title: Design and synthesis of novel tetrahydronaphthyl azoles and related cyclohexyl azoles as antileishmanial agents.
abstract: A novel series of trans-2-aryloxy-1,2,3,4,-tetrahydronaphthyl azoles and related cyclohexyl azoles were synthesized and evaluated in vitro against Leishmania donovani. Compound 9 identified as most active analog with IC(50) value of 0.64 μg/mL and SI value of 34.78 against amastigotes, and is several folds more potent than the reference drugs sodium stilbogluconate and paromomycin. It also exhibited significant in vivo inhibition of 83.33%, and provided a new structural scaffold for antileishmanials.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow, India.
authors.forename: Vijay K
authors.initials: VK
authors.lastname: Marrapu
authors.forename: Nagarapu
authors.initials: N
authors.lastname: Srinivas
authors.forename: Monika
authors.initials: M
authors.lastname: Mittal
authors.forename: Nishi
authors.initials: N
authors.lastname: Shakya
authors.forename: Suman
authors.initials: S
authors.lastname: Gupta
authors.forename: Kalpana
authors.initials: K
authors.lastname: Bhandari
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001393:Azoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects; D015394:Molecular Structure
chemical_list: D000981:Antiprotozoal Agents; D001393:Azoles