Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype was written by Santos, Sofia A.;Lukens, Amanda K.;Coelho, Lis;Nogueira, Fatima;Wirth, Dyann F.;Mazitschek, Ralph;Moreira, Rui;Paulo, Alexandra. And the article was included in European Journal of Medicinal Chemistry in 2015.Application of 17403-09-7 This article mentions the following:
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 antiparasitic activity. The SAR shows that 3-piperidin-4-yl-1H-indole is intolerant to most N-piperidinyl modifications. Nevertheless, the authors were able to identify a new compound 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. The synthesis of the target compounds was achieved using 3-(4-piperidinyl)-1H-indole and 4,6-dichloroquinoline as key reactants. In the experiment, the researchers used many compounds, for example, 3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7Application of 17403-09-7).
3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Application of 17403-09-7
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem