Department of Pharmaceutical Chemistry, KLES' College of Pharmacy, Vidyanagar, Hubli, Karnataka, India.
Arch Pharm (Weinheim). 2009 Dec;342(12):723-31. doi: 10.1002/ardp.200900001.
A novel series of 14 new isonicotinyl hydrazide derivatives 2a-g, 3a-g containing a 4-thiazolidinone / 2-azetidinone nucleus were synthesized by reacting N'-substituted arylidene / heteroarylidene isonicotinyl hydrazide 1a-g with thioglycollic acid in the presence of dry benzene and with chloroacetyl chloride in the presence of triethylamine, respectively. Structures of all newly synthesized compounds were characterized on the basis of elemental analyses and spectral data (IR and (1)H-NMR). All the title compounds were tested for their in-vitro antimycobacterial activity against Mycobacterium tuberculosis H(37)Rv using Alamar-Blue susceptibility test, and the activity is expressed as the minimum inhibitory concentration (MIC) in microg/mL. Among the series, compounds 2b, 2g, 3b, and 3g displayed an encouraging antimycobacterial activity profile as compared to that of the reference drugs isoniazid / rifampicin.
通过 N’-取代的芳基/杂芳基亚肼基异烟酰肼 1a-g 与巯基乙酸在无水苯中的反应，以及氯乙酰氯在三乙胺存在下的反应，合成了一系列 14 种新型异烟酰肼衍生物 2a-g、3a-g，其中包含 4-噻唑烷酮/2-氮杂环丁酮核。所有新合成的化合物的结构均基于元素分析和光谱数据（IR 和 1H-NMR）进行了表征。使用 Alamar-Blue 药敏试验对所有标题化合物进行了体外抗结核分枝杆菌活性测试，并以微克/毫升为单位表示最小抑菌浓度（MIC）。在该系列中，与参考药物异烟肼/利福平相比，化合物 2b、2g、3b 和 3g 显示出令人鼓舞的抗结核分枝杆菌活性。
