title: Synthesis and biological evaluation of arylidene analogues of Meldrum's acid as a new class of antimalarial and antioxidant agents.
abstract: A series of arylidene analogues of Meldrum's acid were synthesized and evaluated for in vitro antimalarial and antioxidant activities for the first time. The influence of various physico-chemical parameters such as dielectric constant (epsilon), donor number (DN), acceptor number (AN), hydrogen bond donor (HBD), hydrogen bond acceptor (HBA), and solubilizing power of the solvents on Meldrum's acid anion generation and thus on promoting the Knoevenagel condensation of Meldrum's acid with aryl aldehydes has been discussed. Five compounds 9l, 9m, 9n, 9r, and 9s were found to be most active against Plasmodiumfalciparum with IC(50) values in the range of 9.68-16.11 microM. Compound 9l exhibited the most potent antimalarial activity (IC(50) 9.68 microM). The compounds were also found to possess antioxidant activity when tested against DPPH and ABTS free radicals.
authors.affiliation: Laboratory for Drug Design and Synthesis, Department of Pharmaceutical Chemistry, Indo-Soviet Friendship (ISF) College of Pharmacy, Moga 142 001, Punjab, India.
authors.forename: Harmeet S
authors.initials: HS
authors.lastname: Sandhu
authors.forename: Sameer
authors.initials: S
authors.lastname: Sapra
authors.forename: Mukesh
authors.initials: M
authors.lastname: Gupta
authors.forename: Kunal
authors.initials: K
authors.lastname: Nepali
authors.forename: Raju
authors.initials: R
authors.lastname: Gautam
authors.forename: Sunil
authors.initials: S
authors.lastname: Yadav
authors.forename: Raj
authors.initials: R
authors.lastname: Kumar
authors.forename: Sanjay M
authors.initials: SM
authors.lastname: Jachak
authors.forename: Manoj
authors.initials: M
authors.lastname: Chugh
authors.forename: Manish K
authors.initials: MK
authors.lastname: Gupta
authors.forename: Om P
authors.initials: OP
authors.lastname: Suri
authors.forename: K L
authors.initials: KL
authors.lastname: Dhar
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000975:Antioxidants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004146:Dioxanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006860:Hydrogen Bonding; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D000975:Antioxidants; D004146:Dioxanes; C076489:Meldrum's acid