title: Peganine hydrochloride dihydrate an orally active antileishmanial agent.
abstract: Protozoic infections caused by genus Leishmania pose an enormous public health threat in developing countries, compounded by the toxicity and resistance to current therapies. Under the aegis of our ongoing program on drug discovery and development on antileishmanial agents from plants, we carried out bioassay guided fractionation on Peganum harmala seeds which resulted in the isolation of 1 as an antileishmanial agent. 2D-NMR spectral data and single crystal X-ray crystallography data indicated 1 as peganine hydrochloride in dihydrated form. The compound 1 exhibited in-vitro activity against both extracellular promastigotes as well as intracellular amastigotes residing within murine macrophages in Leishmania donovani. Furthermore, 1 also exhibited in-vivo activity, 79.6 (+/-8.07)% against established VL in hamsters at a dose of 100mg/kgb.wt.
authors.affiliation: Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226 001, UP, India.
authors.forename: Tanvir
authors.initials: T
authors.lastname: Khaliq
authors.forename: Pragya
authors.initials: P
authors.lastname: Misra
authors.forename: Swati
authors.initials: S
authors.lastname: Gupta
authors.forename: K Papi
authors.initials: KP
authors.lastname: Reddy
authors.forename: Ruchir
authors.initials: R
authors.lastname: Kant
authors.forename: P R
authors.initials: PR
authors.lastname: Maulik
authors.forename: Anuradha
authors.initials: A
authors.lastname: Dube
authors.forename: T
authors.initials: T
authors.lastname: Narender