title: Synthesis and biological evaluation of adamantane-based aminophenols as a novel class of antiplasmodial agents.
abstract: A series of adamantane based aminophenol derivatives were synthesized and evaluated for their antiplasmodial activity in vitro against Plasmodium falciparum (Pf_NF54) and resistant strain (Pf_K1). Herein, we report compounds resulting from this work that show excellent potency against both strains. Additionally, this series displayed excellent cytotoxicity selectivity index against THP1 cell line and had acceptable in vitro DMPK properties.
authors.affiliation: Department of Medicinal Chemistry, AstraZeneca India Pvt. Ltd, Bellary Road, Hebbal, Bangalore 560024, India; Chemistry Division, School of Advanced Sciences, VIT University, Vellore 632014, India.
authors.forename: Murugan
authors.initials: M
authors.lastname: Chinnapattu
authors.affiliation: Chemistry Division, School of Advanced Sciences, VIT University, Vellore 632014, India. Electronic address: sathiya_kuna@hotmail.com.
authors.forename: Kulathu Iyer
authors.initials: KI
authors.lastname: Sathiyanarayanan
authors.affiliation: Department of Medicinal Chemistry, AstraZeneca India Pvt. Ltd, Bellary Road, Hebbal, Bangalore 560024, India. Electronic address: praviniyer@yahoo.com.
authors.forename: Pravin S
authors.initials: PS
authors.lastname: Iyer
mesh_terms: D000218:Adamantane / Q000138:chemical synthesis* / Q000494:pharmacology*; D000627:Aminophenols / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects
chemical_list: D000627:Aminophenols; D000962:Antimalarials; D000218:Adamantane
keywords: Adamantane; Antiplasmodial agents; Plasmodium falciparum; Structure activity relationship