title: Identification of novel phenyl butenonyl C-glycosides with ureidyl and sulfonamidyl moieties as antimalarial agents.
abstract: A new series of C-linked phenyl butenonyl glycosides bearing ureidyl(thioureidyl) and sulfonamidyl moieties in the phenyl rings were designed, synthesized, and evaluated for their in vitro antimalarial activities against Plasmodium falciparum 3D7 (CQ sensitive) and K1 (CQ resistant) strains. Among all the compounds screened the C-linked phenyl butenonyl glycosides bearing sulfonamidyl moiety (5a) and ureidyl moiety in the phenyl ring (7d and 8c) showed promising antimalarial activities against both 3D7 and K1 strains with IC50 values in micromolar range and low cytotoxicity offering new HITS for further exploration.
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: K Kumar G
authors.initials: KK
authors.lastname: Ramakrishna
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Sarika
authors.initials: S
authors.lastname: Gunjan
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Akhilesh Kumar
authors.initials: AK
authors.lastname: Shukla
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Venkata Reddy
authors.initials: VR
authors.lastname: Pasam
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Vishal M
authors.initials: VM
authors.lastname: Balaramnavar
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Abhisheak
authors.initials: A
authors.lastname: Sharma
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Swati
authors.initials: S
authors.lastname: Jaiswal
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Jawahar
authors.initials: J
authors.lastname: Lal
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Renu
authors.initials: R
authors.lastname: Tripathi
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.lastname: Anubhooti
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Ravishankar
authors.initials: R
authors.lastname: Ramachandran
authors.affiliation: Academy of Innovative Science and Research, Medicinal and Process Chemistry Division, Parasitology Division, Pharmacokinetics & Metabolism Division, and Molecular and Structural Biology Division, CSIR-Central Drug Research Institute (CSIR-CDRI) , Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.
authors.forename: Rama Pati
authors.initials: RP
authors.lastname: Tripathi
keywords: Antimalarial agent; Plasmodium falciparum; diarylureides; phenyl sulfonamides