title: Antileishmanial activity of benzocycloalkyl azole oximino ethers: the conformationally constraint analogues of oxiconazole.
abstract: Antileishmanial activities of 16 synthetic oximino benzocycloalkyl azoles against Leishmania donovani were evaluated in vitro against extracellular promastigotes and intracellular amastigotes. Based on SI (Selectivity Index), five compounds were tested further in vivo in hamster model. Out of these, three compounds have shown medium activity (53-58%) and one has shown significant inhibition of parasite multiplication (70%). Despite the fact that these compounds were better than the existing antileishmanials in respect to IC(50) and SI values, they were less active than miltefosine in vivo. The present study has helped us in identifying a new lead that could be exploited as a potential antileishmanial agent.
authors.affiliation: Division of Parasitology, Central Drug Research Institute (CSIR), Chattar Manzil Palace, Lucknow 226001 (UP), India.
authors.forename: Aditya
authors.initials: A
authors.lastname: Verma
authors.forename: Saumya
authors.initials: S
authors.lastname: Srivastava
authors.forename: Shraddha A
authors.initials: SA
authors.lastname: Sane
authors.forename: Vijay K
authors.initials: VK
authors.lastname: Marrapu
authors.forename: Nagarapu
authors.initials: N
authors.lastname: Srinivas
authors.forename: Manisha
authors.initials: M
authors.lastname: Yadav
authors.forename: Kalpana
authors.initials: K
authors.lastname: Bhandari
authors.forename: Suman
authors.initials: S
authors.lastname: Gupta
mesh_terms: D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006224:Cricetinae; D004195:Disease Models, Animal; D004987:Ethers / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007893:Leishmania donovani / Q000187:drug effects*; D007898:Leishmaniasis, Visceral / Q000188:drug therapy*; D007928:Lethal Dose 50
chemical_list: D000977:Antiparasitic Agents; D004987:Ethers; D007093:Imidazoles; C022155:oxiconazole