Synthesis and evaluation of new difluoromethyl azoles as antileishmanial agents.
Several compounds of great pharmacological interest contain the triazole and imidazole rings. In order to find new drugs with antileishmanial activity we have synthesized and evaluated new imidazole and triazole compounds carrying either the carbaldehyde or the difluoromethylene functionalities against promastigote forms of Leishmania amazonensis. Among the compounds tested difluoromethylene azoles 4b and 8f have inhibited the parasite growth significantly. Our results show that the introduction of the difluoromethylene moieties has turned the inactive carbaldehydes into active antileishmanial compounds.
Ferreira
Sabrina B
SB
Universidade Federal do Rio de Janeiro Departamento de Química Orgânica, Instituto de Química, Cidade Universitária, 21949-900 Rio de Janeiro, RJ, Brazil.
Costa
Marilia S
MS
Boechat
Núbia
N
Bezerra
Rômulo J S
RJ
Genestra
Marcelo S
MS
Canto-Cavalheiro
Marilene M
MM
Kover
Warner B
WB
Ferreira
Vitor F
VF
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001393:Azoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D007894:Leishmania mexicana / Q000187:drug effects*; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D000981:Antiprotozoal Agents; D001393:Azoles; D007093:Imidazoles; D014230:Triazoles; C029899:imidazole