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A series of novel carbazoles were synthesized based on structural modifications to lead carbazole 1 (EC100 = 2.5 µM against Haemonchus contortus in vitro), which was revealed in a small molecule screening program as a potentially promising platform for the development of new anthelmintic drugs. Subsequently, analogues 19, 21, 41, 42 (EC100 = 1.25 µM, all), and 39 (EC100 = 0.625 µM) were demonstrated to exhibit enhanced in vitro anthelmintic activity over the lead structure, with compound 39 also being shown to be active in vivo against Heligmosomoides polygyrus.
Rennison et al. (Sun,) studied this question.