European Journal of Medicinal Chemistry p. 320 - 333 (2015)
Update date:2022-08-17
Topics:
Santos, Sofia A.
Lukens, Amanda K.
Coelho, Lis
Nogueira, Fátima
Wirth, Dyann F.
Mazitschek, Ralph
Moreira, Rui
Paulo, Alexandra
A series of 3-piperidin-4-yl-1H-indoles with building block diversity was synthesized based on a hit derived from an HTS whole-cell screen against Plasmodium falciparum. Thirty-eight compounds were obtained following a three-step synthetic approach and evaluated for anti-parasitic activity. The SAR shows that 3-piperidin-4-yl-1H-indole is intolerant to most N-piperidinyl modifications. Nevertheless, we were able to identify a new compound (10d) with lead-like properties (MW = 305; cLogP = 2.42), showing antimalarial activity against drug-resistant and sensitive strains (EC50 values ~ 3 μM), selectivity for malaria parasite and no cross-resistance with chloroquine, thus representing a potential new chemotype for further optimization towards novel and affordable antimalarial drugs.
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Doi:10.1016/0040-4039(95)00331-6
(1995)Doi:10.1039/DT9890001477
(1989)Doi:10.1021/acs.orglett.7b03076
(2017)Doi:10.1021/jo01029a520
(1964)Doi:10.1039/d0cc01934h
(2020)Doi:10.1021/ja01477a049
(1961)