MedChemComm



Methyl sulfonamide substituents improve the pharmacokinetic properties of bicyclic 2-pyridone based Chlamydia trachomatis inhibitors ()
Med. Chem. Commun., 2019, 10,1966-1987 DOI: 10.1039/C9MD00405J, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Martina Kulén, Carlos Núñez-Otero, Andrew G. Cairns, Jim Silver, Anders E. G. Lindgren, Emma Wede, Pardeep Singh, Katarina Vielfort, Wael Bahnan, James A. D. Good, Richard Svensson, Sven Bergström, Åsa Gylfe, Fredrik Almqvist Methyl sulfonamide substituents effectively improve the pharmacokinetic properties of bicyclic 2-pyridones, a new class of Chlamydia trachomatis infectivity inhibitors. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Characterization of the genomically encoded fosfomycin resistance enzyme from Mycobacterium abscessus ()
Med. Chem. Commun., 2019, 10,1948-1957 DOI: 10.1039/C9MD00372J, Research Article Skye Travis, Madeline R. Shay, Shino Manabe, Nathaniel C. Gilbert, Patrick A. Frantom, Matthew K. Thompson FosM from Mycobacterium abscessus is a Mn2+-dependent FosX-type hydrase. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Radiosynthesis and preliminary in vivo evaluation of 18F-labelled glycosylated duramycin peptides for imaging of phosphatidylethanolamine during apoptosis ()
Med. Chem. Commun., 2019, 10,1930-1934 DOI: 10.1039/C9MD00354A, Research Article Mohammad B. Haskali, Delphine Denoyer, Peter D. Roselt, Rodney J. Hicks, Craig A. Hutton [18F]-Labelled duramycin derivatives incorporating hydrophilic aminogalacturonic acid moieties were prepared as tracers for in vivo imaging of phosphatidylethanolamine during apoptosis. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Indole compounds with N-ethyl morpholine moieties as CB2 receptor agonists for anti-inflammatory management of pain: synthesis and biological evaluation ()
Med. Chem. Commun., 2019, 10,1935-1947 DOI: 10.1039/C9MD00173E, Research Article Jiaojiao Li, Jing Ji, Ruibo Xu, Zhengfu Li A series of indole compounds were designed and synthesized as CB2 agonist with high efficacy and selectivity. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

A focused structure–activity relationship study of psoralen-based immunoproteasome inhibitors ()
Med. Chem. Commun., 2019, 10,1958-1965 DOI: 10.1039/C9MD00365G, Research Article Eva Shannon Schiffrer, Izidor Sosič, Andrej Šterman, Janez Mravljak, Irena Mlinarič Raščan, Stanislav Gobec, Martina Gobec SAR exploration at a single position of the psoralen ring led to improved selectivity to the chymotrypsin-like (β5i) subunit of the immunoproteasome. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Lipidomic analysis as a tool for identifying susceptibility to various skin diseases ()
Med. Chem. Commun., 2019, 10,1871-1874 DOI: 10.1039/C9MD00364A, Review Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. Valeriy V. Smirnov, Evgenii A. Egorenkov, Tatiana N. Myasnikova, Alexey E. Petukhov, Vladimir I. Gegechkori, Anna M. Sukhanova, Galina V. Ramenskaya This review is about the significance of the use of lipidomic analysis for identifying susceptibility to skin diseases. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Evaluation of anti-inflammatory activity and molecular docking study of new aza-bicyclic isoxazoline acylhydrazone derivatives ()
Med. Chem. Commun., 2019, 10,1916-1925 DOI: 10.1039/C9MD00276F, Research Article Fernanda Virginia Barreto Mota, Marlene Saraiva de Araújo Neta, Eryvelton de Souza Franco, Isla Vanessa Gomes Alves Bastos, Larissa Cardoso Correia da Araújo, Sandra Cabral da Silva, Tatiane Bezerra de Oliveira, Eduarda Karynne Souza, Valderes Moraes de Almeida, Rafael Matos Ximenes, Maria Bernadete de Sousa Maia, Francisco Jaime Bezerra Mendonça Junior, Pascal Marchand, Antônio Rodolfo de Faria, Teresinha Gonçalves da Silva The aim of this study was to investigate the anti-inflammatory effects of two new isoxazoline-acylhydrazone derivatives. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands ()
Med. Chem. Commun., 2019, 10,1926-1929 DOI: 10.1039/C9MD00379G, Research Article Lars Stank, Annika Frank, Stefanie Hagenow, Holger Stark We linked 5,6,7,8-tetrahydro-4H-thiazoloazepine scaffolds with phenylpiperazine pharmacophores to generate bitopic dopamine receptor ligands. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Structural modification of azolylacryloyl derivatives yields a novel class of covalent modifiers of hemoglobin as potential antisickling agents ()
Med. Chem. Commun., 2019, 10,1900-1906 DOI: 10.1039/C9MD00291J, Research Article Open Access Open Access Creative Commons Licence  This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence. A. M. Omar, T. David, P. P. Pagare, M. S. Ghatge, Q. Chen, A. Mehta, Y. Zhang, O. Abdulmalik, A. H. Naghi, M. E. El-Araby, M. K. Safo The intracellular polymerization and the concomitant sickling processes, central to the pathology of sickle cell disease, can be mitigated by increasing the oxygen affinity of sickle hemoglobin (HbS). The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

The cytotoxic potential of cationic triangulenes against tumour cells ()
Med. Chem. Commun., 2019, 10,1881-1891 DOI: 10.1039/C9MD00305C, Research Article Euphemia Leung, Lisa I. Pilkington, Mohinder M. Naiya, David Barker, Ayesha Zafar, Chatchakorn Eurtivong, Jóhannes Reynisson Close-shelled carbocations DNA intercalators Pr-ADOTA and Pr-DAOTA are very cytotoxic against the cancer cell lines MDA-MB-231 (breast) and HCT116 (colon). The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study ()
Med. Chem. Commun., 2019, 10,1892-1899 DOI: 10.1039/C9MD00286C, Research Article Pasquale Linciano, Barbara De Filippis, Alessandra Ammazzalorso, Pasquale Amoia, Felisa Cilurzo, Marialuigia Fantacuzzi, Letizia Giampietro, Cristina Maccallini, Charlotte Petit, Rosa Amoroso PPAR agonists represent a new therapeutic opportunity for the prevention and treatment of neurodegenerative disorders, but their pharmacological success depends on favourable pharmacokinetic properties and capability to cross the BBB. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Post-PKS enzyme complexes ()
Med. Chem. Commun., 2019, 10,1855-1866 DOI: 10.1039/C9MD00066F, Review Article Redding Gober, Ryan Wheeler, Jürgen Rohr This review highlights the protein–protein interactions between type II post-PKS tailoring enzymes with an emphasis on gilvocarcin and mithramycin. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Different solid forms for optimizing route of administration of the herpes drug Pritelivir ()
Med. Chem. Commun., 2019, 10,1867-1870 DOI: 10.1039/C9MD00233B, Review Article Helga Ruebsamen-Schaeff, Helmut Buschmann In depth knowledge of the physicochemical properties of different salt forms and respective solvates/hydrates has a significant impact on the pharmaceutical dosage form. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Small antibacterial molecules highly active against drug-resistant Staphylococcus aureus ()
Med. Chem. Commun., 2019, 10,1907-1915 DOI: 10.1039/C9MD00329K, Research Article Rajib Dey, Kathakali De, Riya Mukherjee, Sreyan Ghosh, Jayanta Haldar The rapid growth of antibiotic resistance in Staphylococcus aureus coupled with their biofilm forming ability has made the infections difficult to treat with conventional antibiotics. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Non-lethal growth inhibition by arresting the starch utilization system of clinically relevant human isolates of Bacteroides dorei ()
Med. Chem. Commun., 2019, 10,1875-1880 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. The content of this RSS Feed (c) The Royal Society of Chemistry
>> Read More

Synthesis of new lophine–carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00358D, Research Article João Paulo Bizarro Lopes, Luana Silva, Marco Antonio Ceschi, Diogo Seibert Lüdtke, Aline Rigon Zimmer, Thais Carine Ruaro, Rafael Ferreira Dantas, Cristiane Martins Cardoso de Salles, Floriano Paes Silva-Jr, Mario Roberto Senger, Gisele Barbosa, Lídia Moreira Lima, Isabella Alvim Guedes, Laurent Emmanuel Dardenne A series of selective butyrylcholinesterase inhibitors were obtained. The absence of in vitro cytotoxicity and good ADME-Tox profile make these compounds new promising prototypes for the treatment of Alzheimer's disease. 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
>> Read More

Overcoming synthetic challenges in targeting coenzyme A biosynthesis with the antimicrobial natural product CJ-15,801 ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00312F, Research Article Riyad Domingo, Renier van der Westhuyzen, Anton R. Hamann, Konrad J. Mostert, Leanne Barnard, Tanya Paquet, Erick T. Tjhin, Kevin J. Saliba, Willem A. L. van Otterlo, Erick Strauss Presenting an optimised synthesis of the fungus-derived antibiotic CJ-15,801 which shows selective activity against Staphylococcus aureus and Plasmodium falciparum. 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
>> Read More

Current and emerging therapeutic targets of alzheimer's disease for the design of multi-target directed ligands ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00337A, Review Article Laura Blaikie, Graeme Kay, Paul Kong Thoo Lin Alzheimer's disease (AD) is the most prevalent neurodegenerative disease, and a major cause of death worldwide. Since AD is a multi-factorial disease, a MTDL approach to drug discovery is discussed. 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
>> Read More

Aurantiamide-related dipeptide derivatives are formyl peptide receptor 1 antagonists ()
Med. Chem. Commun., 2019, Advance Article DOI: 10.1039/C9MD00336C, Research Article Margherita Mastromarino, Liliya N. Kirpotina, Igor A. Schepetkin, Mark T. Quinn, Enza Lacivita, Marcello Leopoldo Aurantiamide is a useful scaffold to develop promising FPR1 antagonists capable of inhibiting neutrophil chemotaxis. 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
>> Read More