title: Chemotherapy of leishmaniasis part X: synthesis and bioevaluation of novel terpenyl heterocycles.
abstract: Some novel α and β ionone based chalcones and their dihydropyrazolidines/pyrazolidines have been synthesized and evaluated for their in vitro and in vivo antileishmanial activities against Leishmania donovani. Amongest all, one compound (4d) exhibited significant in vitro activity against intracellular amastigotes of Leishmania donovani with IC(50) values of 7.49 μM and was found promising as compared to reference drug, miltefosine. On the basis of good Selectivity Index (S.I.), the compound was further tested for its in vivo response against Leishmania donovani/hamster model and has shown significant inhibition of parasite multiplication (81%). The present study has helped us in identifying a new lead that could be exploited as a potential antileishmanial agent.
authors.affiliation: Division of Medicinal Chemistry, CSIR, Central Drug Research Institute, Lucknow 226 001, India.
authors.forename: Avinash
authors.initials: A
authors.lastname: Tiwari
authors.forename: Santosh
authors.initials: S
authors.lastname: Kumar
authors.forename: S N
authors.initials: SN
authors.lastname: Suryawanshi
authors.forename: Monika
authors.initials: M
authors.lastname: Mittal
authors.forename: Preeti
authors.initials: P
authors.lastname: Vishwakarma
authors.forename: Suman
authors.initials: S
authors.lastname: Gupta
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D047188:Chalcones / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D006224:Cricetinae; D004195:Disease Models, Animal; D004353:Drug Evaluation, Preclinical; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D006801:Humans; D007896:Leishmaniasis / Q000188:drug therapy; D007898:Leishmaniasis, Visceral / Q000188:drug therapy; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000981:Antiprotozoal Agents; D047188:Chalcones; D006571:Heterocyclic Compounds; D011720:Pyrazoles