MedChemComm



The Calcium Dependent Lipopeptide Antibiotics: Structure, Mechanism, & Medicinal Chemistry ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00126C, Review Article Thomas Melvin Wood, Nathaniel I. Martin To push back the growing tide of antibacterial resistance the discovery and development of new antibiotics is a must. In recent years the calcium dependent lipopeptide antibiotics (CDAs) have emerged... The content of this RSS Feed (c) The Royal Society of Chemistry
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Connecting iron acquisition and biofilm formation in the ESKAPE pathogens as a strategy for combatting antibiotic resistance ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00032A, Review Article Savannah Post, Justin Shapiro, William Wuest The rise of antibiotic resistant bacteria has become a problem of global concern. Of particular interest are the ESKAPE pathogens, species with high rates of multi-drug resistant infections. Novel antibiotic... The content of this RSS Feed (c) The Royal Society of Chemistry
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Preparation and evaluation of 99mTc-labeled porphyrin complexes prepared using PNP and HYNIC cores: studying the effects of core selection on pharmacokinetics and tumor uptake in a mouse model ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C8MD00559A, Research Article Mohini Guleria, Tapas Das, Kusum Vats, Jeyachitra Amirdhanayagam, Anupam Mathur, Haladhar D. Sarma, Ashutosh Dash Demonstration of the effect of using two different 99mTc-cores for radiolabeling of the same ligand: differential in vivo outcome. 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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Methicillin-resistant Staphylococcus aureus (MRSA): antibiotic-resistance and the biofilm phenotype ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00044E, Review Article Kelly M. Craft, Johny M. Nguyen, Lawrence J. Berg, Steven D. Townsend Staphylococcus aureus (S. aureus) is an asymptomatic colonizer of 30% of all human beings. It is also the most dangerous of all Staphylococcal bacteria. 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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Tridecaptin-inspired antimicrobial peptides with activity against multidrug-resistant Gram-negative bacteria ()
Med. Chem. Commun., 2019, 10,484-487 DOI: 10.1039/C9MD00031C, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Ross D. Ballantine, Conor E. McCallion, Elie Nassour, Sima Tokajian, Stephen A. Cochrane New tridecaptin analogues are cheaper to make and retain strong Gram-negative activity. The content of this RSS Feed (c) The Royal Society of Chemistry
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Isolation and characterization of tambjamine MYP1, a macrocyclic tambjamine analogue from marine bacterium Pseudoalteromonas citrea ()
Med. Chem. Commun., 2019, 10,478-483 DOI: 10.1039/C9MD00061E, Research Article Katherine J. Picott, Julie A. Deichert, Ella M. deKemp, Gabriele Schatte, Françoise Sauriol, Avena C. Ross Identification of a macrocyclic tambjamine natural product, tambjamine MYP1, from a marine bacterium that may enhance bioactivity by restraining bond rotation. The content of this RSS Feed (c) The Royal Society of Chemistry
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Identification and biological evaluation of novel benzothiazole derivatives bearing a pyridine-semicarbazone moiety as apoptosis inducers via activation of procaspase-3 to caspase-3 ()
Med. Chem. Commun., 2019, 10,465-477 DOI: 10.1039/C8MD00624E, Research Article Junjie Ma, Xin Ni, Yali Gao, Kun Huang, Jiaan Liu, Yu Wang, Roufen Chen, Cuifang Wang A series of benzothiazole derivatives bearing a pyridine-semicarbazone moiety were identified as apoptosis inducers via activation of procaspase-3 to caspase-3. The content of this RSS Feed (c) The Royal Society of Chemistry
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Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles ()
Med. Chem. Commun., 2019, 10,450-455 DOI: 10.1039/C8MD00608C, Research Article Henrietta D. Attram, Sergio Wittlin, Kelly Chibale Analogues of a novel class of benzimidazoles with an intramolecular hydrogen bonding motif have been synthesized and evaluated in vitro for their antiplasmodium activity against chloroquine-sensitive (NF54) and multi-drug resistant (K1) strains of the human malaria parasite Plasmodium falciparum. The content of this RSS Feed (c) The Royal Society of Chemistry
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Using 2-aminobenzimidazole derivatives to inhibit Mycobacterium smegmatis biofilm formation ()
Med. Chem. Commun., 2019, 10,456-459 DOI: 10.1039/C9MD00025A, Research Article T. Vu Nguyen, Matthew T. Peszko, Roberta J. Melander, Christian Melander Biofilm formation by mycobacteria can lead to enhanced antibiotic tolerance. The content of this RSS Feed (c) The Royal Society of Chemistry
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2,2-Dimethyl-3,4-dihydro-2H-1,4-benzoxazines as isosteres of 2,2-dimethylchromans acting as inhibitors of insulin release and vascular smooth muscle relaxants ()
Med. Chem. Commun., 2019, 10,431-438 DOI: 10.1039/C8MD00593A, Research Article Bernard Pirotte, Xavier Florence, Eric Goffin, Philippe Lebrun The present study describes the synthesis and biological evaluation of 4-phenylureido/thioureido-substituted 2,2-dimethyl-3,4-dihydro-2H-1,4-benzoxazines as isosteres of corresponding 2,2-dimethylchromans reported as KATP channel openers. The content of this RSS Feed (c) The Royal Society of Chemistry
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Diversity of PEGylation methods of liposomes and their influence on RNA delivery ()
Med. Chem. Commun., 2019, 10,369-377 DOI: 10.1039/C8MD00515J, Review Article A. S. Nosova, O. O. Koloskova, A. A. Nikonova, V. A. Simonova, V. V. Smirnov, D. Kudlay, M. R. Khaitov A brief review and comparison of the methods of PEGylation of liposomal particles and their influence on the delivery of RNA. The content of this RSS Feed (c) The Royal Society of Chemistry
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Fluorine substituted methoxyphenylalkyl amides as potent melatonin receptor agonists ()
Med. Chem. Commun., 2019, 10,460-464 DOI: 10.1039/C8MD00604K, Research Article Andrew Tsotinis, Rodanthi Kompogennitaki, Ioannis Papanastasiou, Peter J. Garratt, Alina Bocianowska, David Sugden A series of fluorine substituted methoxyphenylalkyl amides were prepared with different orientations of the fluorine and methoxy groups with respect to the alkylamide side chain and with alkyl sides of differing lengths (n = 1–3). The content of this RSS Feed (c) The Royal Society of Chemistry
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Thiosemicarbazones with tyrosinase inhibitory activity ()
Med. Chem. Commun., 2019, 10,378-389 DOI: 10.1039/C9MD00005D, Review Article Katarzyna Hałdys, Rafał Latajka Thiosemicarbazones reveal strong anti-tyrosinase activity. The content of this RSS Feed (c) The Royal Society of Chemistry
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Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation ()
Med. Chem. Commun., 2019, 10,413-420 DOI: 10.1039/C8MD00556G, Research Article Xiaodong Ma, Fang Fang, Qiangqiang Tao, Li Shen, Guochen Zhong, Tao Qiao, Xiaoqing Lv, Jiaming Li A series of structurally novel quinazolone-based PI3Kδ-selective inhibitors were designed and synthesized via the approach of conformational restriction. The content of this RSS Feed (c) The Royal Society of Chemistry
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Rationally synthesized coumarin based pyrazolines ameliorate carrageenan induced inflammation through COX-2/pro-inflammatory cytokine inhibition ()
Med. Chem. Commun., 2019, 10,421-430 DOI: 10.1039/C8MD00457A, Research Article Priyanka Chandel, Anoop Kumar, Nishu Singla, Anshul Kumar, Gagandeep Singh, Rupinder Kaur Gill In the present work, coumarin based pyrazolines (7a–g) have been synthesized and investigated for their in vitro and in vivo anti-inflammatory potential. The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and X-ray study of dispiro 8-nitroquinolone analogues and their cytotoxic properties against human cervical cancer HeLa cells ()
Med. Chem. Commun., 2019, 10,439-449 DOI: 10.1039/C8MD00482J, Research Article Selvaraj Shyamsivappan, Raju Vivek, Arjunan Saravanan, Thangaraj Arasakumar, Gopalan Subashini, Thangaraj Suresh, Ramasamy Shankar, Palathurai Subramaniam Mohan A series of unique dispiro 8-nitroquinolone analogues has been obtained through a one pot three-component reaction. The content of this RSS Feed (c) The Royal Society of Chemistry
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Amide linked redox-active naphthoquinones for the treatment of mitochondrial dysfunction ()
Med. Chem. Commun., 2019, 10,399-412 DOI: 10.1039/C8MD00582F, Research Article Krystel L. Woolley, Monila Nadikudi, Mitra N. Koupaei, Monika Corban, Paul McCartney, Alex C. Bissember, Trevor W. Lewis, Nuri Gueven, Jason A. Smith Naphthoquinones have been investigated as potential therapeutic molecules for neurodegenerative disorders, which is largely based on their anti-oxidative potential. The content of this RSS Feed (c) The Royal Society of Chemistry
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Isatin and its derivatives: a survey of recent syntheses, reactions, and applications ()
Med. Chem. Commun., 2019, 10,351-368 DOI: 10.1039/C8MD00585K, Review Article Varun, Sonam, Rita Kakkar Isatin (1H-indole-2,3-dione) and its derivatives represent an important class of heterocyclic compounds that can be used as precursors for drug synthesis. The content of this RSS Feed (c) The Royal Society of Chemistry
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Potent antiviral activity of carbohydrate-specific algal and leguminous lectins from the Brazilian biodiversity ()
Med. Chem. Commun., 2019, 10,390-398 DOI: 10.1039/C8MD00508G, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Ana C. S. Gondim, Suzete Roberta da Silva, Leen Mathys, Sam Noppen, Sandra Liekens, Alexandre Holanda Sampaio, Celso S. Nagano, Cintia Renata Costa Rocha, Kyria S. Nascimento, Benildo S. Cavada, Peter J. Sadler, Jan Balzarini Brazilian legumes and algae contain potent antiviral lectins. The content of this RSS Feed (c) The Royal Society of Chemistry
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Targeting S. mutans biofilms: a perspective on preventing dental caries ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00015A, Review Article Amber M. Scharnow, Amy E. Solinski, William M. Wuest This review aims to provide an overview of the current small molecule strategies used for targeting S. mutans biofilms, and a perspective of the future for the field. 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 biological evaluation of zinc chelating compounds as metallo-β-lactamase inhibitors ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C8MD00578H, Research Article Geir Kildahl-Andersen, Christian Schnaars, Anthony Prandina, Sylvie Radix, Marc Le Borgne, Lars Petter Jordheim, Tor Gjøen, Adriana Magalhães Santos Andresen, Silje Lauksund, Christopher Fröhlich, Ørjan Samuelsen, Pål Rongved, Ove Alexander Høgmoen Åstrand New MBL inhibitor renders resistant Gram negative bacteria susceptible to carbapenems. 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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Astemizole-based turn-on fluorescent probes for imaging hERG potassium channel ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C8MD00562A, Research Article Xiaomeng Zhang, Tingting Liu, Beilei Wang, Yuqi Gao, Pan Liu, Minyong Li, Lupei Du Based on the scaffold of astemizole, three novel turn-on fluorescent probes (N1–N3) for human ether-a-go-go-related gene (hERG) potassium channel were developed herein. 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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Selective modulation of the cannabinoid type 1 (CB1) receptor as an emerging platform for the treatment of neuropathic pain ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C8MD00595H, Review Article Samuel Banister, Kaavya Krishna Kumar, Vineet Kumar, Brian K Kobilka, Sanjay V. Malhotra Neuropathic pain is caused by a lesion or dysfunction in the nervous system, and it may arise from illness, be drug-induced or caused by toxin exposure. Since the discovery of... The content of this RSS Feed (c) The Royal Society of Chemistry
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New Methods to Assess 6-Thiopurine Toxicity and Expanding its Therapeutic Application to Pancreatic Cancer Via Small Molecule Potentiators ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00010K, Research Article Chamitha Weeramange, Ashabha Lansakara, Johnathan Dallman, Thi Nguyen, Wasundara Hulangamuwa, Ryan J. Rafferty 6-Thiopurine (6TP) is a potent cytotoxic agent that is a clinically prescribed anti-metabolite employed in the treatment of numerous blood cancers since 1952. However, its reported severe toxicities limit its... The content of this RSS Feed (c) The Royal Society of Chemistry
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Polybasic peptide–levofloxacin conjugates potentiate fluoroquinolones and other classes of antibiotics against multidrug-resistant Gram-negative bacteria ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00051H, Research Article Liam Berry, Ronald Domalaon, Marc Brizuela, George G. Zhanel, Frank Schweizer To address the rising threat of multidrug-resistant (MDR) bacteria, new therapeutic strategies must be developed. 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 endolides A and B: naturally occurring N-methylated cyclic tetrapeptides ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00050J, Research Article Emma K. Davison, Alan J. Cameron, Paul W. R. Harris, Margaret A. Brimble The first syntheses of the bioactive cyclic tetrapeptide natural products, endolides A and B, were accomplished using a solution-phase macrocyclisation reaction; the stereoselectivity of which was found to be reagent-controlled. 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 carbohydrate modified berberine derivatives: synthesis and in vitro anti-diabetic investigation ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00036D, Research Article Liwen Han, Wenlong Sheng, Xiaobin Li, Attila Sik, Houwen Lin, Kechun Liu, Lizhen Wang Berberine is a bioactive alkaloid used in Chinese medicine and has numerous positive effects on biological systems. 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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Photophysical properties and application in live cell imaging of B,B-fluoro-perfluoroalkyl BODIPYs ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00011A, Research Article Atsuhiko Taniguchi, Taka Sawazaki, Yusuke Shimizu, Youhei Sohma, Motomu Kanai The photophysical properties of newly identified B,B-fluoro-perfluoroalkyl BODIPYs (2 and 3), which possess a fluoro group and a trifluoromethyl or pentafluoroethyl group at the boron center, were investigated. B,B-Fluoro-perfluoroalkyl BODIPYs... The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis of DNA-coupled isoquinolones and pyrrolidines by solid phase ytterbium- and silver-mediated imine chemistry ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00042A, Research Article Marco Potowski, Verena B. K. Kunig, Florian Losch, Andreas Brunschweiger A solid phase-based strategy gave access to DNA-tagged heterocycles by metal-mediated imine chemistry, exemplified by Cushman- and 1,3-dipolar cycloaddition reactions. 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 Saccharocin from Apramycin and Evaluation of its Ribosomal Selectivity ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C9MD00093C, Research Article Vikram Sarpe, Michael Pirrone, Klara Haldimann, Sven Hobbie, Andrea Vasella, D Crich We describe a straightforward synthesis of the apramycin biosynthetic precursor saccharocin from apramycin by regioselective partial azidation followed by stereoretentive oxidative deamination. Saccharocin was found to exhibit excellent selectivity for... The content of this RSS Feed (c) The Royal Society of Chemistry
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Design of 5-fluorouracil (5-FU) loaded, folate conjugated peptide linked nanoparticles, a potential new drug carrier for selective targeting of tumor cells ()
Med. Chem. Commun., 2019, Accepted Manuscript DOI: 10.1039/C8MD00565F, Research Article Julekha Kazi, Ria Mukhopadhyay, Ramkrishna Sen, Tarun Jha, Shantanu Ganguly, MITA CHATTERJEE Chatterjee DEBNATH In the present investigation folate peptide (FA-Pep) conjugated 5-fluorouracil (5-FU) loaded nanoparticles were synthesized and tumor targeting potentiality was monitored by different in vitro and in vivo techniques. FA-Pep-1 and... The content of this RSS Feed (c) The Royal Society of Chemistry
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Synthesis and discovery of asiatic acid based 1,2,3-triazole derivatives as antitumor agents blocking NF-κB activation and cell migration ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C8MD00620B, Research Article Ri-Zhen Huang, Gui-Bin Liang, Mei-Shan Li, Yi-Lin Fang, Shi-Feng Zhao, Mei-Mei Zhou, Zhi-Xin Liao, Jing Sun, Heng-Shan Wang Asiatic acid based 1,2,3-triazole derivatives as potential inhibitors of NF-κB with high binding affinity and apoptotic induction effects. 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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Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines to develop functionalized ligands to target adenosine receptors: fluorescent ligands as an example ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00014C, Research Article Stephanie Federico, Enrico Margiotta, Silvia Paoletta, Sonja Kachler, Karl-Norbert Klotz, Kenneth A. Jacobson, Giorgia Pastorin, Stefano Moro, Giampiero Spalluto A series of adenosine receptor antagonists bearing a reactive linker was developed. 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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Eradicating uropathogenic Escherichia coli biofilms with a ciprofloxacin–dinitroxide conjugate ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00062C, Research Article Anthony D. Verderosa, Jessica Harris, Rabeb Dhouib, Makrina Totsika, Kathryn E. Fairfull-Smith Biofilm-related UTIs are problematic infectious diseases worldwide; here we have developed a novel ciprofloxacin–dinitroxide conjugate with potent UPEC biofilm-eradication activity. 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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Computation of protein–ligand binding free energies using quantum mechanical bespoke force fields ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00017H, Research Article Daniel J. Cole, Israel Cabeza de Vaca, William L. Jorgensen A quantum mechanical bespoke molecular mechanics force field is derived for the L99A mutant of T4 lysozyme and used to compute absolute binding free energies of six benzene analogs to the protein. 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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Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C8MD00548F, Review Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. James P. Holt-Martyn, Anthony Tumber, Mohammed Z. Rahman, Kerstin Lippl, William Figg, Michael A. McDonough, Rasheduzzaman Chowdhury, Christopher J. Schofield Structure–activity relationship and crystallographic studies on HIF prolyl hydroxylase inhibitors reveal spiro[4.5]decanones as useful templates for generation of potent and selective 2OG oxygenase inhibitors. 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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