title: Effects of varied substituents on the antibacterial activity of triazolylmethyl oxazolidinones.
abstract: A number of 1,2,3-triazolylmethyl piperazino oxazolidinone derivatives with optionally varied substituents at the 4N-piperazine position were synthesized and their antibacterial activity evaluated against a panel of susceptible and resistant Gram-positive and selected Gram-negative bacteria. Substitution with 5-membered heteroaroyl and dinitrobenzoyl moieties potentiated activity against staphylococci and enterococci strains. Furthermore, the compounds having dinitrobenzoyl 7n, 7o, and 5-nitrofuroyl 7t substitutions were four- to eightfold more potent than linezolid against M. catarrhalis. However, substitution of guanidino and other water-solubilizing functionalities at the 4N-piperazine position resulted in compounds that are devoid of antibacterial activity.
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Kuwait University, Safat, Kuwait. dphillips@hsc.edu.kw
authors.forename: Oludotun A
authors.initials: OA
authors.lastname: Phillips
authors.forename: Edet E
authors.initials: EE
authors.lastname: Udo
authors.forename: Mohammed E
authors.initials: ME
authors.lastname: Abdel-Hamid
authors.forename: Reny
authors.initials: R
authors.lastname: Varghese
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D024881:Drug Resistance, Bacterial; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D001936:Moraxella catarrhalis / Q000187:drug effects; D023303:Oxazolidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012995:Solubility; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D023303:Oxazolidinones