title: Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents. Part II.
abstract: The synthesis and antibacterial activity of 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinones is reported. Compound 3e with a 2,4-disubstituted thiophene ring was found to be a potent inhibitor of Gram-positive pathogens and was 4-16-fold more potent than Linezolid.
authors.affiliation: Department of Medicinal Chemistry, New Drug Discovery Research, Ranbaxy Laboratories Limited, R&D III, Plot No. 20, Sector-18, Udyog Vihar Industrial Area, Gurgaon 122001, India. manoj.khera.c4@dsin.co.in
authors.forename: Manoj Kumar
authors.initials: MK
authors.lastname: Khera
authors.forename: Ian A
authors.initials: IA
authors.lastname: Cliffe
authors.forename: Om
authors.initials: O
authors.lastname: Prakash
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D004305:Dose-Response Relationship, Drug; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008958:Models, Molecular; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D011743:Pyrimidines; D014230:Triazoles