4.5 Article

Synthesis and characterization of novel benzothiazole amide derivatives and screening as possible antimitotic and antimicrobial agents

Journal

RESEARCH ON CHEMICAL INTERMEDIATES
Volume 43, Issue 1, Pages 361-378

Publisher

SPRINGER
DOI: 10.1007/s11164-016-2627-3

Keywords

Benzothiazole; Amide; HATU; Antimitotic activity; Allium assay

Funding

  1. Department of Science and Technology, New Delhi, India [IF130464]

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A new series of benzothiazole amide derivatives (9a-l) were synthesized and characterized by Fourier-transform infrared (FT-IR), mass, and H-1 and C-13 nuclear magnetic resonance (NMR) spectroscopic techniques. The antimitotic activity of the newly synthesized compounds was determined by the Allium assay method, from which mitotic index values were calculated. Here, 9g (14.0 %) and 9l (14.5 %) showed mitotic index values most comparable to that of standard drug (14.4 %), while the remaining compounds showed lower mitotic index values; hence, these compounds inhibit the regular cell division process and are the most promising antimitotic agents. Based on the structural activity relationship, the maximum percentage inhibition was observed for compounds containing electron-withdrawing group, revealing enhanced antimitotic activity, while compounds with electron-donating groups such as furan (9g) and methyl (9l) were comparable to standard. The newly synthesized compounds were also screened for antimicrobial activity, with some of them showing remarkable activity. [GRAPHICS] .

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