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Synthesis and antitubercular activity of N-(2-naphthyl)glycine hydrazide analogues.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 1989-11-01 , DOI: 10.1021/jm00131a002
B Ramamurthy 1 , M V Bhatt
Affiliation  

N-(2-Naphthyl)glycine hydrazide analogues were synthesized and tested for possible in vitro antitubercular activity. N-(2-Naphthyl)alanine hydrazide (3), N-methyl-N-(2-naphthyl)glycine hydrazide (5), N-(6-methoxy-2-naphthyl)glycine hydrazide (7), and 3-(2-naphthylamino)butyric acid hydrazide (23) showed potent inhibitory action against Mycobacterium tuberculosis H37Rv in Youman's medium at concentrations ranging from 0.5 to 10.0 micrograms/mL. These compounds showed significant inhibitory action against isonicotinic acid hydrazide and streptomycin-resistant strains of M. tuberculosis. N-(6-Quinolyl)glycine hydrazide (18) and 3-(2-quinolylamino)butyric acid hydrazide (24), which are bioisosteres of compounds 1 and 23, showed loss of antitubercular activity at low concentrations.

中文翻译:

N-(2-萘基)甘氨酸酰肼类似物的合成和抗结核活性。

合成了N-(2-萘基)甘氨酸酰肼类似物,并测试了其可能的体外抗结核活性。N-(2-萘基)丙氨酸酰肼(3),N-甲基-N-(2-萘基)甘氨酸酰肼(5),N-(6-甲氧基-2-萘基)甘氨酸酰肼(7)和3- (2-萘基氨基)丁酸酰肼(23)在Youman培养基中对结核分枝杆菌H37Rv表现出有效的抑制作用,浓度范围为0.5至10.0微克/ mL。这些化合物对异烟酸酰肼和结核分枝杆菌的抗链霉素菌株具有明显的抑制作用。作为化合物1和23的生物等排体的N-(6-喹啉基)甘氨酸酰肼(18)和3-(2-喹啉基氨基)丁酸酰肼(24)在低浓度下显示出抗结核活性的丧失。
更新日期:2019-11-01
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