title: Synthesis of perspicamide A and related diverse analogues: their bioevaluation as potent antileishmanial agents.
abstract: The first protocol for the synthesis of perspicamide A and related diverse analogues has been developed from economical and readily available starting materials. Furthermore, a few synthesized analogues, 24a, 24b, 24c, 24d, and 24l, exhibited potent activity against Leishmania donovani with IC(50) values ranging from 3.75 to 10.37 μM and a selectivity index (SI) ranging from 9.58 to 53.12, which is improved compared to the standard drug Miltefosine (IC(50) 12.4 μM and SI 4.1).
authors.affiliation: Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226001, India.
authors.forename: Anand Kumar
authors.initials: AK
authors.lastname: Pandey
authors.forename: Rashmi
authors.initials: R
authors.lastname: Sharma
authors.forename: Rahul
authors.initials: R
authors.lastname: Shivahare
authors.forename: Ashish
authors.initials: A
authors.lastname: Arora
authors.forename: Neeraj
authors.initials: N
authors.lastname: Rastogi
authors.forename: Suman
authors.initials: S
authors.lastname: Gupta
authors.forename: Prem M S
authors.initials: PM
authors.lastname: Chauhan
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007893:Leishmania donovani / Q000737:chemistry* / Q000187:drug effects; D015394:Molecular Structure; D010767:Phosphorylcholine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000981:Antiprotozoal Agents; D002264:Carboxylic Acids; D011804:Quinolines; C506988:perspicamide A; D010767:Phosphorylcholine; C039128:miltefosine