Synthesis and Leishmanicidal Activity of Novel Urea, Thiourea, and Selenourea Derivatives of Diselenides.

ABSTRACT: A novel series of thirty-one N-substituted urea, thiourea, and selenourea derivatives containing diphenyldiselenide entities were synthesized, fully characterized by spectroscopic and analytical methods, and screened for their in vitro leishmanicidal activities. The cytotoxic activity of these derivatives was tested against Leishmania infantum axenic amastigotes, and selectivity was assessed in human THP-1 cells. Thirteen of the synthesized compounds showed a significant antileishmanial activity, with 50% effective concentration (EC50) values lower than that for the reference drug miltefosine (EC50, 2.84 μM). In addition, the derivatives 9, 11, 42, and 47, with EC50 between 1.1 and 1.95 μM, also displayed excellent selectivity (selectivity index ranged from 12.4 to 22.7) and were tested ag

SUBMITTER: Diaz M 

PROVIDER: S-EPMC6496061 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature