MedChemComm



Discovery of Napabucasin Derivatives for the Treatment of Tuberculosis ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00295B, Research Article Chungen Li, Yun-xiang Tang, Zitai Sang, Yang Yang, Ya-min Gao, Tao Yang, Cui-ting Fang, Tianyu Zhang, Youfu Luo Tuberculosis is the contagious disease responsible for the highest number of deaths worldwide. Here, we screened a commercially available compound library and found napabucasin to possess a moderate anti-tubercular activity... The content of this RSS Feed (c) The Royal Society of Chemistry
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Pursuing DHDPS: an enzyme of unrealised potential as a novel antibacterial target ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00107G, Review Article Rebecca M. Christoff, Chamodi K. Gardhi, Tatiana P. Soares da Costa, Matthew A. Perugini, Belinda M. Abbott DHDPS represents a novel enzyme target for the development of new antibiotics to combat multidrug resistance. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Design of a MUC1-based tricomponent vaccine adjuvanted with FSL-1 for cancer immunotherapy ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00254E, Research Article Mingjing Li, Zhaoyu Wang, Bocheng Yan, Xiaona Yin, Yue Zhao, Fan Yu, Meng Meng, Yonghui Liu, Wei Zhao MUC1 is an attractive target for cancer vaccines as a result of its over-expression and aberrant glycosylation pattern on many tumor cells. However, the low immunogenicity of MUC1 as well... The content of this RSS Feed (c) The Royal Society of Chemistry
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Bivalent AMPA receptor positive allosteric modulators of bis(pyrimidine) series ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00262F, Research Article Anna Nazarova, Kseniya N. Sedenkova, Dmitry S. Karlov, Mstislav Lavrov, Y K. Grishin, Tamara S Kuznetsova, V. L. Zamoyskiy, A A Grigoryev, Elena B. Averina, Vladimir A Palyulin The first examples of novel class of AMPA receptor positive allosteric modulators of bis(pyrimidine) series having a hydroquinone linker have been obtained and showed a potency to increase kainate-induced currents... The content of this RSS Feed (c) The Royal Society of Chemistry
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Non-lethal growth inhibition by arresting the starch utilization system of clinically relevant human isolates of Bacteroides dorei ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00301K, Research Article Anthony D. Santilli, Jordan T. Russell, Eric W. Triplett, Kristi J. Whitehead, Daniel C. Whitehead Acarbose elicits potent, non-microbicidal growth inhibition of clinically relevant Bacteroides dorei strains by arresting the starch utilization system. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Dihydropyrimidine-2-thiones as Eg5 inhibitors and L-type calcium channel blockers: potential antitumour dual agents ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00108E, Research Article Elena González-Hernández, Rubén Aparicio, Mercedes Garayoa, M. José Montero, M. Ángeles Sevilla, Concepción Pérez-Melero 4-Aryldihydropyrimidine-2-thiones are proposed as potential antitumour dual agents, both as Eg5 inhibitors and L-type calcium channel blockers. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Contributors to our ‘New Talent’ Collection ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD90032B, Profile MedChemComm profiles the contributors to the ‘New Talent’ themed collection. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Molecular evolution of peptides by yeast surface display technology ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00252A, Review Article Sara Linciano, Stefano Pluda, Arianna Bacchin, Alessandro Angelini This review provides a detailed analysis of the diverse genetically encoded peptides that have been evolved by using yeast surface display technology. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and anti-cancer activities of glycosides and glycoconjugates of diterpenoid isosteviol ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00242A, Research Article Radmila R. Sharipova, Mayya G. Belenok, Bulat F. Garifullin, Anastasiya S. Sapunova, Alexandra D. Voloshina, Olga V. Andreeva, Irina Yu. Strobykina, Polina V. Skvortsova, Yuriy F. Zuev, Vladimir E. Kataev A series of glycosides and glycoconjugates of diterpenoid isosteviol with various monosaccharide residues were synthesized. Most of them showed moderate to significant cytotoxicity against human cancer cell lines M-HeLa and MCF-7. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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The winding road of the uvaretin class of natural products: from total synthesis to bioactive agent discovery ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00052F, Research Article Johnathan Dallman, Ashabha Lansakara, Thi Nguyen, Chamitha Weeramange, Wasundara Hulangamuwa, Ryan J. Rafferty Herein, we disclose the development of a synthetic route to gain access to the uvaretin class of chalcone natural products. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Exploration of [2 + 2 + 2] cyclotrimerisation methodology to prepare tetrahydroisoquinoline-based compounds with potential aldo–keto reductase 1C3 target affinity ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00201D, Research Article Ana R. N. Santos, Helen M. Sheldrake, Ali I. M. Ibrahim, Chhanda Charan Danta, Davide Bonanni, Martina Daga, Simonetta Oliaro-Bosso, Donatella Boschi, Marco L. Lolli, Klaus Pors Tetrahydroisoquinoline (THIQ) is a key structural component in many biologically active molecules including natural products and synthetic pharmaceuticals. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis of bicyclic 1,4-thiazepines as novel anti-Trypanosoma brucei brucei agents ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00064J, Research Article Franco Vairoletti, Andrea Medeiros, Pablo Fontán, Jennifer Meléndrez, Carlos Tabárez, Gustavo Salinas, Jaime Franco, Marcelo A. Comini, Jenny Saldaña, Vojtech Jancik, Graciela Mahler, Cecilia Saiz Bicyclic thiazolidinyl-1,4-thiazepines were prepared and evaluated as potential antiparasitic agents. We found thiazepines with low micromolar EC50 against T. b. brucei and high selectivity index. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Benzoazacrown compound: highly effective chelator for therapeutic Bismuth radioisotopes ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00251K, Research Article Ekaterina Matazova, Bayirta Egorova, Ekaterina Konopkina, Gleb Aleshin, Anastasia D. Zubenko, Artem A. Mitrofanov, Kirill Karpov, Olga Fedorova, Yury V. Fedorov, Stepan N. Kalmykov New benzoazacrown ligand H4BATA was synthesized and its complexation ability towards Bismuth cation was evaluated. Binding of cation occurs at room temperature in a few minutes and formed complexes demonstrate... The content of this RSS Feed (c) The Royal Society of Chemistry
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Emerging modes-of-action in drug discovery ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00263D, Review Article Eric Valeur, Frank Narjes, Christian Ottmann, Alleyn T. Plowright An increasing focus on complex biology to cure diseases rather than merely treat symptoms is transforming how drug discovery can be approached, and expands the arsenal of drug modalities and modes-of-actions that can be leveraged to modify diseases. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00264B, Research Article Daniela Passeri, Andrea Carotti, Jose M. Ramos Pittol, Gianmario Ciaccioli, Roberto Pellicciari, Saskia W. C. van Mil, Antimo Gioiello FXR allosteric pockets might act as potential targets for small molecules to selectively interfere with the metabolic action of the receptor. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Development of benzochalcone derivatives as selective CYP1B1 inhibitors and anticancer agents ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00258H, Research Article Jinyun Dong, Jiahua Cui, Yan Wu, S. Li, Qingqing Meng, Qijing Zhang, Zengtao Wang, Guang Huang A series of benzochalcone derivatives has been synthesized and evaluated for CYP1 inhibitory activity and cytotoxic property against wild type cell lines (MCF-7 and MDA-MB-231) and drug resistant cell lines... The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and antitumor activity of fluorouracil – oleanolic acid/ursolic acid/glycyrrhetinic acid conjugates ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00246D, Research Article Chun-Mei Liu, Jia-Yan Huang, Li-Xin Sheng, Xiao-An Wen, Ke-Guang Cheng Due to the obvious adverse effects of 5-fluorouracil and considering the diverse biological activities of pentacyclic triterpenes, twelve pentacyclic triterpene-5-fluorouracil conjugates were synthesized and their antitumor activities were evaluated. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Quinolone Antibiotics ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00120D, Review Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Thu D. M. Pham, Zyta Ziora, Mark Blaskovich The quinolone antibiotics arose in the early 1960s, with the first examples possessing a narrow-spectrum activity with unfavorable pharmacokinetic properties. Over time, the development of new quinolone antibiotics has led... The content of this RSS Feed (c) The Royal Society of Chemistry
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Messenger RNA delivery by hydrazone-activated polymers ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00231F, Research Article Marisa Juanes, Oliver Creese, Paco Fernández-Trillo, Javier Montenegro Here we present the intracellular delivery of mRNA using polyhydrazones prepared in situ under physiological conditions, demonstrating the versatility and adaptability of this technology to more sensitive and therapeutically relevant nucleic acids. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Binding site characterization – similarity, promiscuity, and druggability ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00102F, Research Article Christiane Ehrt, Tobias Brinkjost, Oliver Koch Promiscuity as key to drug repurposing, off-target prediction, polypharmacology: What can be learned based on the comparison of binding sites and the description of their properties? Herein, we discuss binding site similarities with a special focus on medicinal chemistry. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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FgaPT2, a biocatalytic tool for alkyl-diversification of indole natural products ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00177H, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Chandrasekhar Bandari, Erin M. Scull, Tejaswi Bavineni, Susan L. Nimmo, Eric D. Gardner, Ryan C. Bensen, Anthony W. Burgett, Shanteri Singh Demonstration of FgaPT2 catalyzed alkyl-diversification of indole containing natural products. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Drug-resistance in Mycobacterium tuberculosis: where we stand ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00057G, Review Article Amanda Mabhula, Vinayak Singh Tuberculosis (TB), an infectious disease caused by the bacterium Mycobacterium tuberculosis (Mtb), has burdened vulnerable populations in modern day societies for decades. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Correction: From linked open data to molecular interaction: studying selectivity trends for ligands of the human serotonin and dopamine transporter ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD90031D, Correction Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Barbara Zdrazil, Eva Hellsberg, Michael Viereck, Gerhard F. Ecker To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Repositioning salirasib as new antimalarial agent ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00298G, Research Article Exequiel Oscar Jesús Porta, Ignasi Bofill Verdaguer, Consuelo Pérez, Claudia Banchio, Mauro Ferreira de Azevedo, Alejandro Katzin, Guillermo R Labadie Malaria is a neglected disease that kills thousands of people every year, mainly in Africa, due to Plasmodium falciparum infections. Salirasib is a promising cancer drug candidate that interferes with... The content of this RSS Feed (c) The Royal Society of Chemistry
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The global antibiotic research and development partnership (GARDP): researching and developing new antibiotics to meet global public health needs ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD90010A, Editorial Laura J. V. Piddock To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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On the road to structure-based development of anti-virulence therapeutics targeting the type III secretion system injectisome ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00146H, Review Article Bronwyn J. E. Lyons, Natalie C. J. Strynadka Targeting the T3SS injectisome using the anti-virulence strategy offers an alternative to antibiotic therapeutic approaches when dealing with resistance. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Kaolin alleviates the toxicity of graphene oxide for mammalian cells ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C8MD00633D, Research Article Elvira Rozhina, Svetlana Batasheva, Anna Danilushkina, Marina Kryuchkova, Marina Gomzikova, Yuliya Cherednichenko, Läysän Nigamatzyanova, Farida Akhatova, Rawil Fakhrullin Toxicity of graphene oxide to cells reduced by almost 20% after its incubation with kaolin, most likely because of its adhesion to the platy clay nanoparticles, which was detected by atomic force microscopy. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Non-covalent albumin-binding ligands for extending the circulating half-life of small biotherapeutics ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00018F, Review Article Alessandro Zorzi, Sara Linciano, Alessandro Angelini This review provides a detailed examination and comparison of the diverse non-covalent albumin-binding ligands developed until now to extend the half-life of different small biotherapeutics. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Derivatives of a new heterocyclic system – pyrano[3,4-c][1,2,4]triazolo[4,3-a]pyridines: synthesis, docking analysis and neurotropic activity ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00187E, Research Article Ervand G. Paronikyan, Anthi Petrou, Maria Fesatidou, Athina Geronikaki, Shushanik Sh. Dashyan, Suren S. Mamyan, Ruzanna G. Paronikyan, Ivetta M. Nazaryan, Hasmik H. Hakopyan 8-Hydrazino derivatives of pyrano[3,4-c]pyridines and derivatives of new heterocyclic system 3-thioxopyrano[3,4-c][1,2,4]triazolo[4,3-a]pyridines were synthesized and evaluated for their neurotropic activity. The most active compound in all tests appeared to be 5g. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Novel zafirlukast derivatives exhibit selective antibacterial activity against Porphyromonas gingivalis ()
Med. Chem. Commun., 2019, 10,926-933 DOI: 10.1039/C9MD00074G, Research Article Nishad Thamban Chandrika, Marina Y. Fosso, Yelena Alimova, Abigail May, Octavio A. Gonzalez, Sylvie Garneau-Tsodikova Eleven new zafirlukast derivatives selective and bactericidal against Porphyromonas gingivalis. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and biological evaluation of structurally diverse α-conformationally restricted chalcones and related analogues ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00127A, Research Article Casey J. Maguire, Graham J. Carlson, Jacob W. Ford, Tracy E. Strecker, Ernest Hamel, Mary Lynn Trawick, Kevin G. Pinney Cyclic chalcones and structural analogues evaluated as cytotoxic agents. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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A MedChem toolbox for cereblon-directed PROTACs ()
Med. Chem. Commun., 2019, 10,1037-1041 DOI: 10.1039/C9MD00185A, Research Article Christian Steinebach, Izidor Sosič, Stefanie Lindner, Aleša Bricelj, Franziska Kohl, Yuen Lam Dora Ng, Marius Monschke, Karl G. Wagner, Jan Krönke, Michael Gütschow A modular chemistry toolbox was developed for cereblon-directed PROTACs. The content of this RSS Feed (c) The Royal Society of Chemistry
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New N-phenyl-4,5-dibromopyrrolamides as DNA gyrase B inhibitors ()
Med. Chem. Commun., 2019, 10,1007-1017 DOI: 10.1039/C9MD00224C, Research Article Nace Zidar, Helena Macut, Tihomir Tomašič, Lucija Peterlin Mašič, Janez Ilaš, Anamarija Zega, Päivi Tammela, Danijel Kikelj A new series of N-phenyl-4,5-dibromopyrrolamides was developed as inhibitors of bacterial DNA gyrase B with IC50 in the low nanomolar range. The content of this RSS Feed (c) The Royal Society of Chemistry
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Fluoroquinolone-derived fluorescent probes for studies of bacterial penetration and efflux ()
Med. Chem. Commun., 2019, 10,901-906 DOI: 10.1039/C9MD00124G, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. M. Rhia L. Stone, Muriel Masi, Wanida Phetsang, Jean-Marie Pagès, Matthew A. Cooper, Mark A. T. Blaskovich Fluorescent probes derived from the fluoroquinolone antibiotic ciprofloxacin were synthesised using a Cu(I)-catalysed azide–alkyne cycloaddition (CuAAC) to link a ciprofloxacin azide derivative with alkyne-substituted green and blue fluorophores. The content of this RSS Feed (c) The Royal Society of Chemistry
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Scaffold hybridization strategy towards potent hydroxamate-based inhibitors of Flaviviridae viruses and Trypanosoma species ()
Med. Chem. Commun., 2019, 10,991-1006 DOI: 10.1039/C9MD00200F, Research Article Erofili Giannakopoulou, Vasiliki Pardali, Efseveia Frakolaki, Vasileios Siozos, Vassilios Myrianthopoulos, Emmanuel Mikros, Martin C. Taylor, John M. Kelly, Niki Vassilaki, Grigoris Zoidis Design and synthesis of potent inhibitors with dual activity by successfully merging two distinct scaffolds into a single chemical entity. The content of this RSS Feed (c) The Royal Society of Chemistry
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Fungal natural alkaloid schizocommunin activates the aryl hydrocarbon receptor pathway ()
Med. Chem. Commun., 2019, 10,985-990 DOI: 10.1039/C9MD00138G, Research Article Roxana Filip, Tyler A. Shaw, Atsushi Nishida, John Paul Pezacki Activation of AhR by schizocommunin is linked to increased expression of xenobiotic metabolizing enzymes associated with immune and allergic responses. The content of this RSS Feed (c) The Royal Society of Chemistry
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Aminopyrimidine–galactose hybrids are highly selective galectin-3 inhibitors ()
Med. Chem. Commun., 2019, 10,913-925 DOI: 10.1039/C9MD00183B, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Alexander Dahlqvist, Fredrik R. Zetterberg, Hakon Leffler, Ulf J. Nilsson Galactopyranosides with aryl-aminopyrimidine moieties at O3 inhibit the tumor and immunity-related galectin-3 with high selectivity over other galectins. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and antitumor activity of aza-brazilan derivatives containing imidazolium salt pharmacophores ()
Med. Chem. Commun., 2019, 10,1027-1036 DOI: 10.1039/C9MD00112C, Research Article Mingqin Huang, Shengzu Duan, Xueqiong Ma, Bicheng Cai, Dongmei Wu, Yan Li, Liang Li, Hongbin Zhang, Xiaodong Yang A series of novel aza-brazilan derivatives containing imidazolium salt pharmacophores were synthesized and their antitumor structure–activity relationship studies were reported. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis, molecular docking, and biological evaluation of novel 2-pyrazoline derivatives as multifunctional agents for the treatment of Alzheimer's disease ()
Med. Chem. Commun., 2019, 10,1018-1026 DOI: 10.1039/C9MD00030E, Research Article Oya Unsal-Tan, Tuba Tüylü Küçükkılınç, Beyza Ayazgök, Ayla Balkan, Keriman Ozadali-Sari A novel series of 2-pyrazoline derivatives were designed, synthesized, and evaluated for cholinesterase (ChE) inhibitory, Aβ anti-aggregating and neuroprotective activities. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and direct comparison of the anticancer activities of phomopsolides D and E and two 7-oxa-/7-aza-analogues ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00121B, Research Article Alhanouf Z. Aljahdali, Seth A. Freedman, Jana Scott, Miaosheng Li, George A. O'Doherty The synthesis and biological evaluation of two phomopsolide natural products (D and E) and two analogues is presented. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
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Revitalizing antifolates through understanding mechanisms that govern susceptibility and resistance ()
Med. Chem. Commun., 2019, 10,880-895 DOI: 10.1039/C9MD00078J, Review Article Shannon Lynn Kordus, Anthony David Baughn Mechanisms of antifolate resistance in bacterial and mammalian cells. The content of this RSS Feed (c) The Royal Society of Chemistry
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Discovery of (aza)indole derivatives as novel respiratory syncytial virus fusion inhibitors ()
Med. Chem. Commun., 2019, 10,970-973 DOI: 10.1039/C9MD00178F, Research Article Xiufang Zheng, Chungen Liang, Lisha Wang, Kun Miao, Baoxia Wang, Weixing Zhang, Dongdong Chen, Guolong Wu, Wei Zhu, Lei Guo, Song Feng, Lu Gao, Hong C. Shen, Hongying Yun A new class of (aza)indole derivatives have been identified as potent RSV fusion inhibitors. The content of this RSS Feed (c) The Royal Society of Chemistry
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Anthranilic amide and imidazobenzothiadiazole compounds disrupt Mycobacterium tuberculosis membrane potential ()
Med. Chem. Commun., 2019, 10,934-945 DOI: 10.1039/C9MD00088G, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Jake Smith, Heather Wescott, Julie Early, Steven Mullen, Junitta Guzman, Joshua Odingo, Jason Lamar, Tanya Parish Compounds 1 and 2 disrupt M. tuberculosis membrane potential and demonstrate bactericidal activity against non-replicating M. tuberculosis in pH 4.5 buffer. The content of this RSS Feed (c) The Royal Society of Chemistry
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Using Drosophila as a platform for drug discovery from natural products in Parkinson's disease ()
Med. Chem. Commun., 2019, 10,867-879 DOI: 10.1039/C9MD00099B, Review Article Urmila Maitra, Lukasz Ciesla The review provides an overview of discovery of new drug leads from natural extracts using Drosophila as a screening platform to evaluate the therapeutic potential of phytochemicals against Parkinson's disease. The content of this RSS Feed (c) The Royal Society of Chemistry
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Recent advances in the genome mining of Aspergillus secondary metabolites (covering 2012–2018) ()
Med. Chem. Commun., 2019, 10,840-866 DOI: 10.1039/C9MD00054B, Review Article Jillian Romsdahl, Clay C. C. Wang This review covers advances made in genome mining SMs produced by Aspergillus nidulans, Aspergillus fumigatus, Aspergillus niger, and Aspergillus terreus in the past six years (2012–2018). Genetic identification and molecular characterization of SM biosynthetic gene clusters, along with proposed biosynthetic pathways, is discussed in depth. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis, ribosomal selectivity, and antibacterial activity of netilmicin 4′-derivatives ()
Med. Chem. Commun., 2019, 10,946-950 DOI: 10.1039/C9MD00153K, Research Article Amr Sonousi, Dimitri Shcherbakov, Andrea Vasella, Erik C. Böttger, David Crich We describe the synthesis and evaluation of 4′-subsituted netilmicin derivatives by selective functionalization at the 4′-position of the endocyclic enolether function. The content of this RSS Feed (c) The Royal Society of Chemistry
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Construction of a hybrid gene cluster to reveal coupled ring formation–hydroxylation in the biosynthesis of HSAF and analogues from Lysobacter enzymogenes ()
Med. Chem. Commun., 2019, 10,907-912 DOI: 10.1039/C9MD00154A, Research Article Xue Li, Haoxin Wang, Yaoyao Li, Liangcheng Du HSAF and analogues are polycyclic tetramate macrolactams (PoTeMs) isolated from Lysobacter enzymogenes. The content of this RSS Feed (c) The Royal Society of Chemistry
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Stereoselective semi-synthesis of the neuroprotective natural product, serofendic acid ()
Med. Chem. Commun., 2019, 10,951-960 DOI: 10.1039/C9MD00145J, Research Article Dimitri Perusse, Michael J. Smanski Our synthesis of neuroprotectant serofendic acid from biosourced ent-atis-16-en-19-oic acid represents the best route to date. The content of this RSS Feed (c) The Royal Society of Chemistry
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Controlling cellular distribution of drugs with permeability modifying moieties ()
Med. Chem. Commun., 2019, 10,974-984 DOI: 10.1039/C8MD00412A, Research Article Paul L. Richardson, Violeta L. Marin, Stormy L. Koeniger, Aleksandra Baranczak, Julie L. Wilsbacher, Peter J. Kovar, Patricia E. Bacon-Trusk, Min Cheng, Todd A. Hopkins, Sandra T. Haman, Anil Vasudevan Anionic moieties can be used to control the cell-permeability of drugs and used to select the appropriate target identification method for phenotypic screening hits. The content of this RSS Feed (c) The Royal Society of Chemistry
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Novel antimycobacterial C-21 amide derivatives of the antibiotic fusidic acid: synthesis, pharmacological evaluation and rationalization of media-dependent activity using molecular docking studies in the binding site of human serum albumin ()
Med. Chem. Commun., 2019, 10,961-969 DOI: 10.1039/C9MD00161A, Research Article Godwin Akpeko Dziwornu, Stephanie Kamunya, Tando Ntsabo, Kelly Chibale Fusidic acid is a natural product antibiotic used clinically, primarily against staphylococcal infections. The content of this RSS Feed (c) The Royal Society of Chemistry
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Rational design of novel amphipathic antimicrobial peptides focused on the distribution of cationic amino acid residues ()
Med. Chem. Commun., 2019, 10,896-900 DOI: 10.1039/C9MD00166B, Research Article Takashi Misawa, Chihiro Goto, Norihito Shibata, Motoharu Hirano, Yutaka Kikuchi, Mikihiko Naito, Yosuke Demizu Amphipathic helical peptide Stripe showed high antimicrobial activity, low hemolytic activity, and low human cell cytotoxicity. The content of this RSS Feed (c) The Royal Society of Chemistry
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