Singh J, Seth M, Fatma N, Sharma S, Bhaduri A P, Chatterjee R K
Central Drug Research Institute, Lucknow, India.
Z Naturforsch C J Biosci. 1990 Nov-Dec;45(11-12):1210-4. doi: 10.1515/znc-1990-11-1221.
The design and synthesis of a series of alkyl 5(6)-substituted benzimidazole-2-carbamates (1-13), 7-chloro-4-(4-substituted phenyl)aminoquinolines (14-16), 1,2-dimethyl-3-methoxy-carbonyl-4,5-disubstituted pyrroles (17-19) and some compounds belonging to the class pimelonitrile (20), dihydroquinoline (21), pyridine (22), pyridoquinoline (23) and tetrahydro-pyrimidine (24) have been carried out as possible antifilarial agents. All these compounds have been evaluated for their activity against male and female adult worms of Litomosoides carinii in cotton rats. The effect of these compounds was also observed on the reproductive system (condition of developing microfilariae and their release from uterus) of adult female worms. In this study, three types of compounds were discovered: (a) those which showed activity on both the male and female adult worms and also had sterilizing effects on surviving adult females (1-3, 6-9, 13, 19), (b) those which only sterilized the adult females (14-16, 21, 24), and (c) those which had no effect on female reproduction but killed only adult worms (4, 5, 11, 12, 17, 18, 20, 22, 23). This tends to open up a new avenue in the chemotherapy of filariasis and the future scope of work on chemosterilization of adult females has been discussed.
已开展了一系列5(6)-烷基取代苯并咪唑-2-氨基甲酸酯（1-13）、7-氯-4-(4-取代苯基)氨基喹啉（14-16）、1,2-二甲基-3-甲氧基羰基-4,5-二取代吡咯（17-19）以及一些属于庚二腈（20）、二氢喹啉（21）、吡啶（22）、吡啶并喹啉（23）和四氢嘧啶（24）类化合物的设计与合成，将其作为潜在的抗丝虫病药物。已对所有这些化合物针对棉鼠体内卡里尼丝虫的雌雄成虫的活性进行了评估。还观察了这些化合物对成年雌虫生殖系统（发育中的微丝蚴状况及其从子宫中的释放）的影响。在本研究中，发现了三种类型的化合物：(a) 对雌雄成虫均有活性且对存活的成年雌虫有绝育作用的化合物（1-3、6-9、13、19），(b) 仅使成年雌虫绝育的化合物（14-16、21、24），以及(c) 对雌虫生殖无影响但仅杀死成虫的化合物（4、5、11、12、17、18、20、22、23）。这倾向于为丝虫病化疗开辟一条新途径，并且已讨论了成年雌虫化学绝育未来的工作范围。
