Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1, 4-naphthoquinones. Issue 13 (1st July 2019)

• Record Type: Journal Article
• Authors: Olawode, Emmanuel O.; Tandlich, Roman; Prinsloo, Earl; Isaacs, Michelle; Hoppe, Heinrich; Seldon, Ronnett; Warner, Digby F.; Steenkamp, Vanessa; Kaye, Perry T.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 29:Issue 13(2019)
• Page Start: 1572
• Page End: 1575
• Publication Date: 2019-07-01
• Subjects: 2-Chloro-3-[(thiazol-2-yl)amino]-1, 4-naphthoquinones -- Anti-malarial -- Anti-bacterial -- Anti-tuberculosis -- Cytotoxicity -- HeLa cells; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.05.001
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of novel, substituted 2-chloro-3-[(thiazol-2-yl)amino]-1, 4-naphthoquinones have been prepared and shown to exhibit promising concentration-dependent activity against human SH-SY5Y cells, Plasmodium falciparum, Mycobacterium tuberculosis and P. aeruginosa . Substituent effects on observed bioactivity have been explored; the para- fluorophenyl derivative3d exhibited activity across the range of the bioassays employed, indicating the potential of the 2-chloro-3-[(4-arylthiazol-2-yl)amino]-1, 4-naphthoquinone scaffold in the development of novel, broad spectrum therapeutics.