An insight into tetrahydro-β-carboline-tetrazole hybrids: synthesis and bioevaluation as potent antileishmanial agents.

ABSTRACT: A series of 2,3,4,9-tetrahydro-β-carboline tetrazole derivatives (14a-u) have been synthesized utilizing the Ugi multicomponent reaction and were identified as potential antileishmanial chemotypes. Most of the screened derivatives exhibited significant in vitro activity against the promastigote (IC₅₀ from 0.59 ± 0.35 to 31 ± 1.27 μM) and intracellular amastigote forms (IC₅₀ from 1.57 ± 0.12 to 17.6 ± 0.2 μM) of L. donovani, and their activity is comparable with standard drugs miltefosine and sodium stibogluconate. The most active compound 14t was further studied in vivo against the L. donovani/golden hamster model at a dose of 50 mg kg^-1 through the intraperitoneal route for 5 consecutive days, which displayed 75.04

SUBMITTER: Purohit P 

PROVIDER: S-EPMC6084189 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature