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Updated: Apr 11, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Click reaction based synthesis, antimicrobial, and cytotoxic activities of new 1,2,3-triazoles
Mohamed Ramadan El Sayed Aly1, Hosam Ali Saad2, Mosselhi Abdelnabi Mosselhi Mohamed3
1Chemistry Department, Faculty of Science, Taif University, Hawyah-Taif, Saudi Arabia; Chemistry Department, Faculty of Applied Science, Port Said University, 42522 Port Said, Egypt.
Abstract:
Three-motif pharmacophoric models 20a-e and 21-25 were prepared in good yields by CuAAC of two azido substrates 2 and 11 with seven terminal acetylenic derivatives including chalcones 17a-e, theophylline 18 and cholesterol 19. The structure of these compounds was elucidated by NMR, MS, IR spectroscopy and micro analyses. This series was screened as antimicrobial and cytotoxic agents in vitro. Most derivatives showed appreciable antibacterial activity, but they displayed weak cytotoxic, and antifungal activities. Notably, conjugate 25 (cream of the crop) was found to be more active than Ampicillin against Escherichia coli and Staphylococcus aureus and showed appreciable antifungal and cytotoxic activities as well.
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