SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF N-(2-NAPHTHYL)GLYCINE HYDRAZIDE ANALOGS
SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF N-(2-NAPHTHYL)GLYCINE HYDRAZIDE ANALOGS
复制标题
DOI：
10.1021/jm00131a002
复制
发表时间：
1989-11-01
影响因子：
7.3
通讯作者：
BHATT, MV
中科院分区：
文献类型：
--
作者：
RAMAMURTHY, B;BHATT, MV
合成了N-（2-萘基）甘氨酸酰肼类似物，并进行了可能的体外抗结核活性测试。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）在浓度范围为0.5 - 10.0 μ g/mL时显示出对Youman培养基中的结核分枝杆菌H37 Rlv的有效抑制作用。这些化合物对耐异烟酰肼和链霉素的M.结核化合物1和23的生物电子等排体N-6-（喹啉基）甘氨酸酰肼（18）和3-（2-喹啉基氨基）丁酸酰肼（24）在低浓度下表现出抗结核活性的丧失。
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 H37Rlv in Youman''s medium at concentrations ranging from 0.5 to 10.0 .mu.g/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.