title: The synthesis and antibacterial activity of 1,3,4-thiadiazole phenyl oxazolidinone analogues.
abstract: Replacement of the morpholine C-ring of linezolid 1 with a 1,3,4-thiadiazolyl ring leads to oxazolidinone analogues 5 having potent antibacterial activity against both gram-positive and gram-negative organisms. Conversion of the C5 acetamide group to a thioacetamide further increases the potency of these compounds.
authors: Discovery-Chemistry and Discovery-Infectious Diseases, Pharmacia Corporation, 7000 Portage Road, Kalamazoo, MI 49001, USA. lisa.m.thomasco@pfizer.com
authors: Lisa M
authors: LM
authors: Thomasco
authors: Robert C
authors: RC
authors: Gadwood
authors: Elizabeth A
authors: EA
authors: Weaver
authors: Jason M
authors: JM
authors: Ochoada
authors: Charles W
authors: CW
authors: Ford
authors: Gary E
authors: GE
authors: Zurenko
authors: Judith C
authors: JC
authors: Hamel
authors: Douglas
authors: D
authors: Stapert
authors: Judy K
authors: JK
authors: Moerman
authors: Ronda D
authors: RD
authors: Schaadt
authors: Betty H
authors: BH
authors: Yagi
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D000069349:Linezolid; D008826:Microbial Sensitivity Tests; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010636:Phenols / Q000737:chemistry*; D051381:Rats; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000737:chemistry*; D013853:Thioacetamide / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000081:Acetamides; D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D010636:Phenols; D013830:Thiadiazoles; D013853:Thioacetamide; D000069349:Linezolid