title: Chemotherapy of leishmaniasis. Part XII: design, synthesis and bioevaluation of novel triazole integrated phenyl heteroterpenoids as antileishmanial agents.
abstract: A novel series of triazole integrated phenyl heteroterpenoids have been synthesized and screened for their in vitro activity against intracellular amastigote form of Leishmania donovani. Among all tested compounds, compound 3a was found to be the most active with IC50 6.4μM and better selectivity index (SI) 18 as compared to reference drugs, miltefosine and miconazole. When evaluated in vivo in L. donovani/hamster model, 3a has exhibited 79±11% inhibition of parasite multiplication at 50mgkg(-1)×5days on day 7 post treatment.
authors.affiliation: Division of Medicinal Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 001, India.
authors.forename: S N
authors.initials: SN
authors.lastname: Suryawanshi
authors.forename: Avinash
authors.initials: A
authors.lastname: Tiwari
authors.forename: Santosh
authors.initials: S
authors.lastname: Kumar
authors.forename: Rahul
authors.initials: R
authors.lastname: Shivahare
authors.forename: Monika
authors.initials: M
authors.lastname: Mittal
authors.forename: Padam
authors.initials: P
authors.lastname: Kant
authors.forename: Suman
authors.initials: S
authors.lastname: Gupta
mesh_terms: D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D007893:Leishmania donovani / Q000187:drug effects*; D007898:Leishmaniasis, Visceral / Q000188:drug therapy*; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D013729:Terpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014709:Vero Cells
chemical_list: D000977:Antiparasitic Agents; D013729:Terpenes; D014230:Triazoles