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Antiparasitic Activity of Fluorophenyl-Substituted Pyrimido[1,2-a]benzimidazoles.

ABSTRACT: A series of fourteen pyrimido[1,2-a]benzimidazole compounds was prepared by straightforward heterocyclic chemistry and oxidation methods. The new pyrimidobenzimidazole derivative 2a with a 3-fluorophenyl substituent was identified as a new antiparasitic compound showing excellent activities against Leishmania major parasites. 2a was highly active against L. major promastigotes and amastigotes with EC₅₀ values in the nanomolar concentration range. Compound 3b was less active than 2a against L. major, but more active against Toxoplasma gondii with considerable selectivity. Hence, two promising and selective antiparasitic drug candidates 2a and 3b for the treatment of two parasitic diseases were identified, which can be prepared by green chemistry methods using simple one-pot reactions and oxidation procedures, respectively.

SUBMITTER: Nasr ISA

PROVIDER: S-EPMC9855371 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature

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Antiparasitic Activity of Fluorophenyl-Substituted Pyrimido[1,2-a]benzimidazoles.

Nasr Ibrahim S Al ISA Koko Waleed S WS Khan Tariq A TA Schobert Rainer R Biersack Bernhard B

Biomedicines 20230114 1

A series of fourteen pyrimido[1,2-a]benzimidazole compounds was prepared by straightforward heterocyclic chemistry and oxidation methods. The new pyrimidobenzimidazole derivative 2a with a 3-fluorophenyl substituent was identified as a new antiparasitic compound showing excellent activities against Leishmania major parasites. 2a was highly active against L. major promastigotes and amastigotes with EC50 values in the nanomolar concentration range. Com ...[more]

PMID: 36672727

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