2. Academic Validation
  3. Identification of novel phenyl butenonyl C-glycosides with ureidyl and sulfonamidyl moieties as antimalarial agents

Identification of novel phenyl butenonyl C-glycosides with ureidyl and sulfonamidyl moieties as antimalarial agents

  • ACS Med Chem Lett. 2014 Jun 2;5(8):878-83. doi: 10.1021/ml500211c.
K Kumar G Ramakrishna 1,  Sarika Gunjan 1,  Akhilesh Kumar Shukla 1,  Venkata Reddy Pasam 1,  Vishal M Balaramnavar 1,  Abhisheak Sharma 1,  Swati Jaiswal 1,  Jawahar Lal 1,  Renu Tripathi 1,  Anubhooti 1,  Ravishankar Ramachandran 1,  Rama Pati Tripathi 1
Affiliations

Affiliation

  • 1 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.
PMID: 25147607 DOI: 10.1021/ml500211c
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.

Keywords

Antimalarial agent; Plasmodium falciparum; diarylureides; phenyl sulfonamides.

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