7‐Chloroquinoline–isatin Conjugates: Antimalarial, Antitubercular, and Cytotoxic Evaluation. (14th March 2014)

• Record Type: Journal Article
• Authors: Raj, Raghu; Biot, Christophe; Carrère‐Kremer, Séverine; Kremer, Laurent; Guérardel, Yann; Gut, Jiri; Rosenthal, Philip J.; Forge, Delphine; Kumar, Vipan
• Is Part Of: Chemical biology & drug design. Volume 83:Number 5(2014:May)
• Page Start: 622
• Page End: 629
• Publication Date: 2014-03-14
• Subjects: Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12273
• Languages: English
• ISSNs: 1747-0277

Abstract

<abstract abstract-type="main" id="cbdd12273-abs-0001"> <title> <x xml:space="preserve">Abstract</x> </title> <p>A series of twenty piperazine‐tethered 7‐chloroquinoline–isatin hybrids have been synthesized <italic>via</italic> either direct nucleophilic substitution or Cu(<italic>Ι</italic>)Cl‐mediated Mannich reaction. These new conjugates were evaluated for their antimalarial and antitubercular efficacy against a chloroquine‐resistant strain of <italic>Plasmodium falciparum</italic> and <italic>Mycobacterium tuberculosis</italic>, respectively, while the cytotoxic profiles were evaluated against 3T6 cell line, a permanent mouse embryonic fibroblast cell line. The most potent of the test compound with IC₅₀ of 0.22 <italic>μ</italic><sc>m</sc> against W2 strain of <italic>P. falciparum</italic> and 31.62 <italic>μ</italic><sc>m</sc> against the embryonic fibroblast cell line (cytotoxicity) displayed a high selective index of 143.73.</p> </abstract>