Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592892 | Bioorganic & Medicinal Chemistry Letters | 2014 | 6 Pages |
Abstract
A series of pyrazinamide derivatives with alkylamino substitution was designed, synthesized and tested for their ability to inhibit the growth of selected mycobacterial, bacterial and fungal strains. The target structures were prepared from the corresponding 5-chloro (1) or 6-chloropyrazine-2-carboxamide (2) by nucleophilic substitution of chlorine by various non-aromatic amines (alkylamines). To determine the influence of alkyl substitution, corresponding amino derivatives (1a, 2a) and compounds with phenylalkylamino substitution were prepared. Some of the compounds exerted antimycobacterial activity against Mycobacterium tuberculosis H37Rv significantly better than standard pyrazinamide and corresponding starting compounds (1 and 2). Basic structure-activity relationships are presented. Only weak antibacterial and no antifungal activity was detected.
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Authors
Barbora Servusová, Pavla Paterová, Jana MandÃková, VladimÃr KubÃÄek, Radim KuÄera, JiÅà KuneÅ¡, Martin Doležal, Jan Zitko,