title: Aryloxy cyclohexyl imidazoles: a novel class of antileishmanial agents.
abstract: 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.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, M.G. Marg, Lucknow, UP 226001, India.
authors.forename: Nagarapu
authors.initials: N
authors.lastname: Srinivas
authors.forename: Shraddha
authors.initials: S
authors.lastname: Palne
authors.lastname: Nishi
authors.forename: Suman
authors.initials: S
authors.lastname: Gupta
authors.forename: Kalpana
authors.initials: K
authors.lastname: Bhandari
mesh_terms: 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
chemical_list: D000981:Antiprotozoal Agents; D007093:Imidazoles