title: A natural product inspired hybrid approach towards the synthesis of novel pentamidine based scaffolds as potential anti-parasitic agents.
abstract: A natural product inspired molecular hybridization approach led us to a series of novel pentamidine based pyrimidine and chalcone scaffolds. All the hybrids were evaluated for their anti-leishmanial potential. Most of the screened compounds have showed significant in vitro anti-leishmanial activity with less cytotoxicity in comparison to the standard drugs (pentamidine, sodium stibogluconate, and miltefosine). Additionally, anti-malarial screening of these compounds was also done and four compounds have shown superior activity against chloroquine resistance strain (K1) of Plasmodium falciparum.
authors.affiliation: Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226001, India.
authors.forename: Vikas
authors.initials: V
authors.lastname: Tyagi
authors.forename: Shahnawaz
authors.initials: S
authors.lastname: Khan
authors.forename: Rahul
authors.initials: R
authors.lastname: Shivahare
authors.forename: Khushboo
authors.initials: K
authors.lastname: Srivastava
authors.forename: Suman
authors.initials: S
authors.lastname: Gupta
authors.forename: Saqib
authors.initials: S
authors.lastname: Kidwai
authors.forename: Kumkum
authors.initials: K
authors.lastname: Srivastava
authors.forename: S K
authors.initials: SK
authors.lastname: Puri
authors.forename: Prem M S
authors.initials: PM
authors.lastname: Chauhan
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D001688:Biological Products / Q000737:chemistry*; D002599:Chalcone / Q000737:chemistry; D010419:Pentamidine / Q000737:chemistry*; D010963:Plasmodium falciparum / Q000187:drug effects; D011743:Pyrimidines / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D000981:Antiprotozoal Agents; D001688:Biological Products; D011743:Pyrimidines; D002599:Chalcone; D010419:Pentamidine; C030986:pyrimidine