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Effects of Varied Substituents on the Antibacterial Activity of Triazolylmethyl Oxazolidinones
Author(s) -
Phillips Oludotun A.,
Udo Edet E.,
AbdelHamid Mohammed E.,
Varghese Reny
Publication year - 2012
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201100332
Subject(s) - piperazine , chemistry , antibacterial activity , stereochemistry , antibacterial agent , bacteria , bicyclic molecule , structure–activity relationship , chemical synthesis , biological activity , organic chemistry , biochemistry , antibiotics , in vitro , biology , genetics
A number of 1,2,3‐triazolylmethyl piperazino oxazolidinone derivatives with optionally varied substituents at the 4 N ‐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 4 N ‐piperazine position resulted in compounds that are devoid of antibacterial activity.