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Molecules 2015, 20(5), 8800-8815;

Design, Synthesis and Antitubercular Activity of Certain Nicotinic Acid Hydrazides

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Egyptian Russian University, Badr City, Cairo 11829, Egypt
The Regional Center for Mycology and Biotechnology, Al-Azhar University, Cairo 11759, Egypt
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia
Department of Applied Organic Chemistry, National Research Center, Dokki, Cairo 12622, Egypt
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 17 April 2015 / Revised: 12 May 2015 / Accepted: 12 May 2015 / Published: 15 May 2015
(This article belongs to the Section Medicinal Chemistry)
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Three series of 6-aryl-2-methylnicotinohydrazides 4ai, N′-arylidene-6-(4-bromophenyl)-2-methylnicotino hydrazides 7af, and N′-(un/substituted 2-oxoindolin-3-ylidene)-6-(4-fluorophenyl)-2-methylnicotinohydrazides 8ac were synthesized and evaluated for their potential in vitro antimycobacterial activity against M. tuberculosis. The results showed that isatin hydrazides 8ac are remarkably more active than the parent hydrazide 4c. Hydrazides 8b and 8c exhibited the highest activity among all the tested compounds (MIC = 12.5 and 6.25 µg/mL, respectively). Compounds 8b and 8c were also devoid of apparent cytotoxicity to HT-29, PC-3, A549, HepG2 and MCF-7 cancer cell lines. Besides, 8b and 8c showed good drug-likeness scores of 0.62 and 0.41, respectively. Those two isatin hydrazides could offer an excellent framework for future development to obtain more potent antitubercular agents. The SAR study suggested that lipophilicity of the synthesized derivatives is a crucial element that accounts for their antimycobacterial activity. Finally, a theoretical kinetic study was established to predict the ADME of the active derivatives. View Full-Text
Keywords: synthesis; nicotinic acid; hydrazides; antimycobacterial; ADME synthesis; nicotinic acid; hydrazides; antimycobacterial; ADME

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Eldehna, W.M.; Fares, M.; Abdel-Aziz, M.M.; Abdel-Aziz, H.A. Design, Synthesis and Antitubercular Activity of Certain Nicotinic Acid Hydrazides. Molecules 2015, 20, 8800-8815.

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