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

A series of fourteen pyrimido[1,2- ]benzimidazole compounds was prepared by straightforward heterocyclic chemistry and oxidation methods. The new pyrimidobenzimidazole derivative with a 3-fluorophenyl substituent was identified as a new antiparasitic compound showing excellent activities against par...

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Veröffentlicht in:Biomedicines 2023-01, Vol.11 (1), p.219
Hauptverfasser: Nasr, Ibrahim S Al, Koko, Waleed S, Khan, Tariq A, Schobert, Rainer, Biersack, Bernhard
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Sprache:eng
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Zusammenfassung:A series of fourteen pyrimido[1,2- ]benzimidazole compounds was prepared by straightforward heterocyclic chemistry and oxidation methods. The new pyrimidobenzimidazole derivative with a 3-fluorophenyl substituent was identified as a new antiparasitic compound showing excellent activities against parasites. was highly active against promastigotes and amastigotes with EC values in the nanomolar concentration range. Compound was less active than against , but more active against with considerable selectivity. Hence, two promising and selective antiparasitic drug candidates and 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.
ISSN:2227-9059
2227-9059
DOI:10.3390/biomedicines11010219