Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype
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.
Santos, Sofia A.,Lukens, Amanda K.,Coelho, Lis,Nogueira, Fátima,Wirth, Dyann F.,Mazitschek, Ralph,Moreira, Rui,Paulo, Alexandra
p. 320 - 333
(2015/09/01)
Synthesis of piperidine derivatives with a quinazoline ring system as potential antihypertensive agent
-
Takai,Obase,Teranishi
p. 1907 - 1916
(2007/10/02)
More Articles about upstream products of 56361-85-4