title: Synthesis and structure-activity relationships of lansine analogues as antileishmanial agents.
abstract: Clear and rational thinking: A series of rationally designed, lansine-derived carbazoles was synthesized and evaluated for activity against promastigotes and amastigotes of Leishmania donovani, the causative agent of leishmaniasis. Some structural modifications gave rise to compounds with enhanced activity and selectivity over lansine, allowing structure-activity relationships to be elucidated and providing a foundation for the further development of this pharmacophore.
authors.affiliation: College of Pharmacy, University of Hawai'i at Hilo, Hilo, HI 96720-4029 (USA); Interdepartmental Center Biopharmanet_TEC, Universita' degli Studi di Parma, Via G. P. Usberti 27, Parma (Italy).
authors.forename: Marco
authors.initials: M
authors.lastname: Pieroni
authors.forename: Sisay
authors.initials: S
authors.lastname: Girmay
authors.forename: Dianqing
authors.initials: D
authors.lastname: Sun
authors.forename: Rajnish
authors.initials: R
authors.lastname: Sahu
authors.forename: Babu L
authors.initials: BL
authors.lastname: Tekwani
authors.forename: Ghee T
authors.initials: GT
authors.lastname: Tan
mesh_terms: D000818:Animals; D002460:Cell Line; D002522:Chlorocebus aethiops; D015195:Drug Design; D006801:Humans; D007893:Leishmania donovani / Q000187:drug effects*; D007896:Leishmaniasis / Q000188:drug therapy*; D051379:Mice; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014709:Vero Cells
chemical_list: D014344:Trypanocidal Agents