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  • Title: Effects of varied substituents on the antibacterial activity of triazolylmethyl oxazolidinones.
    Author: Phillips OA, Udo EE, Abdel-Hamid ME, Varghese R.
    Journal: Arch Pharm (Weinheim); 2012 Oct; 345(10):790-803. PubMed ID: 22886578.
    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.
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