Bhattarai, Deepak Lee, Sun H. Seo, Seon H. Nam, Ghilsoo Kang, Soon B. Pae, Ae N. Kim, Eunice E. Oh, Taegwon Cho, Sang-Nae Keum, Gyochang 2024-01-20T14:03:20Z 2024-01-20T14:03:20Z 2021-09-05 2012-09 1747-0277 https://pubs.kist.re.kr/handle/201004/128932 We synthesized a series of oxazolidinone-type antibacterials in which morpholine C-ring of linezolid has been modified by substituted 3-azabicyclo[3.3.0]octanyl rings. Acetamide or 1,2,3-triazole heterocycle was used as C-5 side chain of oxazolidinone. The resulting series of compounds was then screened in vitro against panel of susceptible and resistant Gram-positive, Gram-negative bacteria, and Mycobacterium tuberculosis (Mtb). Several analogs in this series exhibited potent in vitro antibacterial activity comparable or superior to linezolid against the tested bacteria. Compounds 10a, 10b, 11a, and 15a displayed highly potent activity against M.similar to tuberculosis. Selected compound 10b showed good human microsomal stability and CYP-profile, and showed low activity against hERG channel. English WILEY RESISTANT STAPHYLOCOCCUS-AUREUS LINEZOLID-RESISTANT MYCOBACTERIUM-TUBERCULOSIS MULTIDRUG-RESISTANT MURINE MODEL AGENTS INFECTIONS EPIDERMIDIS SYSTEM GENE Synthesis and In Vitro Antibacterial Activity of Novel 3-Azabicyclo[3.3.0]octanyl Oxazolidinones Article 10.1111/j.1747-0285.2012.01404.x 1 CHEMICAL BIOLOGY & DRUG DESIGN, v.80, no.3, pp.388 - 397 CHEMICAL BIOLOGY & DRUG DESIGN 80 3 388 397 scie scopus 000306664800006 2-s2.0-84864135918 Biochemistry & Molecular Biology Chemistry, Medicinal Biochemistry & Molecular Biology Pharmacology & Pharmacy Article RESISTANT STAPHYLOCOCCUS-AUREUS LINEZOLID-RESISTANT MYCOBACTERIUM-TUBERCULOSIS MULTIDRUG-RESISTANT MURINE MODEL AGENTS INFECTIONS EPIDERMIDIS SYSTEM GENE antibacterial agents drug design drug discovery Mycobacterium tuberculosis oxazolidinone