Preparation and in‐vitro Evaluation of 4‐Benzylsulfanylpyridine‐2‐carbohydrazides as Potential Antituberculosis Agents |
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| Authors: | Petra Herzigová Vera Klime?ová Karel Palát Jarmila Kaustová Hans‐Martin Dahse Ute Möllmann |
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| Institution: | 1. Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Králové, Czech Republic. Fax: +420 495 067 166;2. Laboratory of Mycobacterial Diagnostics, Regional Institute of Public Health, Ostrava, Czech Republic;3. Lebniz‐Institut für Naturstoff‐Forschung und Infektionsbiologie e.V. – Hans‐Kn?ll‐Institut, Germany |
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| Abstract: | A set of 4‐benzylsulfanylpyridine‐2‐carbohydrazides was synthesized and evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, non‐tuberculous mycobacteria, and multidrug‐resistant M. tuberculosis. The activities expressed as the minimum inhibitory concentration (MIC) fall into a range of 2 to 125 μmol/L, most often 4 to 32 μmol/L. The results revealed that the substituents on the benzyl moiety do not influence the antimycobacterial efficacy. The substances exhibited similar activities against sensitive and resistant strains of M. tuberculosis. Furthermore, compounds show low antiproliferative effect and cytotoxicity. |
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| Keywords: | 4‐Benzylsulfanyl derivatives Multidrug‐resistant M tuberculosis Mycobacterium tuberculosis Non‐tuberculous mycobacteria Pyridine‐2‐carbohydrazides |
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