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Novel Antiprotozoal Products: Imidazole and Benzimidazole N ‐Oxide Derivatives and Related Compounds
Author(s) -
Aguirre Gabriela,
Boiani Mariana,
Cerecetto Hugo,
Gerpe Alejandra,
González Mercedes,
Sainz Yolanda Fernández,
Denicola Ana,
de Ocáriz Carmen Ochoa,
Nogal Juan José,
Montero David,
Escario José Antonio
Publication year - 2004
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200300840
Subject(s) - antiprotozoal , benzimidazole , imidazole , chemistry , anthelmintic , combinatorial chemistry , stereochemistry , organic chemistry , biochemistry , in vitro , medicine , veterinary medicine
The syntheses and biological evaluation of the first anti‐protozoa imidazole N ‐oxide and benzimidazole N ‐oxide and their derivatives are reported. They were tested in vitro against two different protozoa, Trypanosoma cruzi and Trichomonas vaginalis . Derivative 7c , ethyl‐1‐( i ‐butyloxycarbonyloxy)‐6‐nitrobenzimid‐azole‐2‐carboxylate, displayed activity on both protozoa. Lipophilicity and redox potential were experimentally determined in order to study the relationship with activity of the compounds. These properties are well related with the observed bioactivity. Imidazole and benzimidazole N ‐oxide derivatives are becoming leaders for further chemical modifications and advanced biological studies.