Ramakrishna K Kumar G, Gunjan Sarika, Shukla Akhilesh Kumar, Pasam Venkata Reddy, Balaramnavar Vishal M, Sharma Abhisheak, Jaiswal Swati, Lal Jawahar, Tripathi Renu, Ramachandran Ravishankar, Tripathi Rama Pati
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.
ACS Med Chem Lett. 2014 Jun 2;5(8):878-83. doi: 10.1021/ml500211c. eCollection 2014 Aug 14.
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.
设计、合成了一系列新型的在苯环上带有脲基（硫脲基）和磺酰胺基部分的C-连接苯基丁烯酰基糖苷，并评估了它们对恶性疟原虫3D7（氯喹敏感）和K1（氯喹耐药）菌株的体外抗疟活性。在所有筛选的化合物中，在苯环上带有磺酰胺基部分（5a）以及脲基部分（7d和8c）的C-连接苯基丁烯酰基糖苷对3D7和K1菌株均表现出有前景的抗疟活性，IC50值在微摩尔范围内且细胞毒性低，为进一步探索提供了新的活性化合物。
