Aryloxy cyclohexyl imidazoles: a novel class of antileishmanial agents.
Thirteen novel aryloxy cyclohexane-based mono and bis imidazoles were synthesized and evaluated in vitro as antileishmanials against Leishmania donovani and cytotoxicity assessed. These compounds were better than the existing drugs, sodium stibogluconate and pentamidine in respect to IC(50) and SI values. Promising compounds were tested further in vivo. Among all, the bis methylimidazole with 2-fluoro, 4-nitro aryloxy group (9) exhibited significant in vivo inhibition of 77.9%, thus providing new structural lead for antileishmanials.
Srinivas
Nagarapu
N
Medicinal and Process Chemistry Division, Central Drug Research Institute, M.G. Marg, Lucknow, UP 226001, India.
Palne
Shraddha
S
Nishi
Gupta
Suman
S
Bhandari
Kalpana
K
D000818:Animals; D030801:Animals, Genetically Modified; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007893:Leishmania donovani / Q000187:drug effects*; D009682:Magnetic Resonance Spectroscopy
D000981:Antiprotozoal Agents; D007093:Imidazoles