Synthesis, Antiprotozoal Activity, and Physicochemical Evaluation of Benzamido-Menadione Derivatives.

ABSTRACT: The naphthoquinone skeleton is known for broad biological applications and, in particular, for antiparasitic efficacy. As part of our ongoing search for new antiprotozoal naphthoquinone derivatives, we incorporated computer-aided optimization models utilizing physicochemical parameters into our approach. Herein, we report on the synthesis of 21 new benzamido-menadione and naphthoquinone derivatives via the Kochi-Anderson reaction. The antiprotozoal activity of all the synthesized compounds was evaluated against Plasmodium falciparum NF54 and Trypanosoma brucei rhodesiense STIB900. Cytotoxicity towards L6 cells was also determined, and the respective selectivity indices (SI) were calculated. Several ligand efficiency metrics, such as LLE, SILE, and FQ, were calculated, and the

SUBMITTER: Presser A 

PROVIDER: S-EPMC12652484 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature