19514-92-2Relevant articles and documents
Structure based design, synthesis, and biological evaluation of imidazole derivatives targeting dihydropteroate synthase enzyme
Daraji, Drashti G.,Rajani, Dhanji P.,Rajani, Smita D.,Pithawala, Edwin A.,Jayanthi, Sivaraman,Patel, Hitesh D.
supporting information, (2021/02/16)
In this study, we have designed and synthesized 2-((5-acetyl-1-(phenyl)-4-methyl-1H-imidazol-2-yl)thio)-N-(4-((benzyl)oxy)phenyl) acetamide derivatives. Antimicrobial activities of all the imidazole derivatives have been examined against Gram-positive and Gram-negative bacteria and results showed that the conjugates have appreciable antibacterial activity. Besides, several analogous were evaluated for their in vitro antiresistant bacterial strains such as Extended-spectrum beta-lactamases (ESBL), Vancomycin-resistant Enterococcus (VRE), and Methicillin-resistant Staphylococcus aureus (MRSA). The SAR revealed that the 12l compound resulted in potency against all bacterial strains as well as ESBL, VRE, and MRSA strains. Lipinski's rule of five, and ADME studies were preformed for all the synthesized compounds with Staphylococcus aureus dihydropteroate synthase (saDHPS) protein (PDB ID: 6CLV) and were found standard drug-likeness properties of conjugates. Moreover, the binding mode of the ligands with the protein study has been examined by molecular docking and results are quite promising. Besides, all the analogous were tested for their in vitro antituberculosis, antimalarial, and antioxidant activity.
Synthesis and biological evaluation of 1H-benzimidazol-5-ols as potent HBV inhibitors
Zhao, Yanfang,Liu, Yajing,Chen, Dong,Wei, Zengquan,Liu, Wenzhao,Gong, Ping
scheme or table, p. 7230 - 7233 (2011/01/03)
A new series of 1-methyl-1H-benzimidazol-5-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. Some of the analogues in this series displayed inhibitory activity superior to lamivudine. Of them, compound 13b was the most potent one, showing an IC50 value of 7.8 μM and a SI value of 13.0. 2010 Published by Elsevier Ltd. All rights reserved.
4-Acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists
Procopiou, Panayiotis A.,Ancliff, Rachael A.,Bamford, Mark J.,Browning, Christopher,Connor, Helen,Davies, Susannah,Fogden, Yvonne C.,Hodgson, Simon T.,Holmes, Duncan S.,Looker, Brian E.,Morriss, Karen M. L.,Parr, Christopher A.,Pickup, Elizabeth A.,Sehmi, Sanjeet S.,White, Gemma V.,Watts, Clarissa J.,Wilson, David M.,Woodrow, Michael D.
, p. 6706 - 6717 (2008/09/17)
A series of ketopiperazines were prepared and evaluated for their activity as histamine H3 antagonists. From investigation of the tertiary basic center in the aminopropyloxyphenyl template, the 2(R)-methylpyrrolidine was identified as the most
