Bhattarai, Deepak Lee, Ju-hyeon Seo, Seon Hee Nam, Ghilsoo Choo, Hyunah Kang, Soon Bang Kwak, Jin-Hwan Oh, Taegwon Cho, Sang-Nae Pae, Ae Nim Kim, Eunice Eunkyeong Jeong, Nakcheol Keum, Gyochang 2024-01-20T08:30:36Z 2024-01-20T08:30:36Z 2021-09-02 2014-12 0009-2363 https://pubs.kist.re.kr/handle/201004/126072 A novel series of oxazolidinone-class antimicrobial agents with 5-substituted octahydrocyclopenta[c]pyrrole moieties at the C-ring of linezolid and an acetamide or 1,2,3-triazole ring as the C-5 side chain of the oxazolidinone ring were prepared. The resulting series of compounds were evaluated for in vitro antimicrobial activity against Mycobacterium tuberculosis and a panel of clinically important resistant Gram-positive and -negative bacteria. Among them, endo-alcohol 2a and exo-alcohol 2b showed potent inhibitory activity against M. tuberculosis H(37)Rv, which was superior to that of linezolid. Several analogues in this series showed potent in vitro antibacterial activity against the clinically important vancomycin-resistant bacteria and showed similar or better potency against linezolid-resistant methicillin-resistant Staphylococcus aureus (MASA) strains. The hydroxyl group in the azabicyclic C-ring interacted with the same hydrophobic pocket as linezolid based on a docking study. Selected compounds with high antimicrobial activity showed good human microsomal stability and low CYP isozyme and monoamine oxidase (MAO) inhibition. English PHARMACEUTICAL SOC JAPAN RESISTANT STAPHYLOCOCCUS-AUREUS LINEZOLID RESISTANCE MYCOBACTERIUM-TUBERCULOSIS AGENTS ANTIBIOTICS INFECTIONS OUTBREAK SYSTEM RNA Synthesis and in Vitro Evaluation of the Antitubercular and Antibacterial Activity of Novel Oxazolidinones Bearing Octahydrocyclopenta[c]pyrrol-2-yl Moieties Article 10.1248/cpb.c14-00510 1 CHEMICAL & PHARMACEUTICAL BULLETIN, v.62, no.12, pp.1214 - 1224 CHEMICAL & PHARMACEUTICAL BULLETIN 62 12 1214 1224 scie scopus 000345495500008 2-s2.0-84919903153 Chemistry, Medicinal Chemistry, Multidisciplinary Pharmacology & Pharmacy Pharmacology & Pharmacy Chemistry Article RESISTANT STAPHYLOCOCCUS-AUREUS LINEZOLID RESISTANCE MYCOBACTERIUM-TUBERCULOSIS AGENTS ANTIBIOTICS INFECTIONS OUTBREAK SYSTEM RNA oxazolidinone antibacterial agent Gram-positive bacteria Mycobacterium tuberculosis linezolid