title: Click reaction based synthesis, antimicrobial, and cytotoxic activities of new 1,2,3-triazoles.
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.
authors.affiliation: Chemistry Department, Faculty of Science, Taif University, Hawyah-Taif, Saudi Arabia; Chemistry Department, Faculty of Applied Science, Port Said University, 42522 Port Said, Egypt. Electronic address: mrea34@hotmail.com.
authors.forename: Mohamed Ramadan
authors.initials: MR
authors.lastname: El Sayed Aly
authors.affiliation: Chemistry Department, Faculty of Science, Taif University, Hawyah-Taif, Saudi Arabia; Chemistry Department, Faculty of Science, Zagazig University, Zagazig 44511, Egypt.
authors.forename: Hosam Ali
authors.initials: HA
authors.lastname: Saad
authors.affiliation: Chemistry Department, Faculty of Science, Taif University, Hawyah-Taif, Saudi Arabia; Chemistry Department, Faculty of Science, Cairo University, Cairo 12613, Egypt.
authors.forename: Mosselhi Abdelnabi Mosselhi
authors.initials: MA
authors.lastname: Mohamed
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001231:Aspergillus flavus / Q000187:drug effects; D001419:Bacteria / Q000187:drug effects*; D002176:Candida albicans / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects*; D002599:Chalcone / Q000737:chemistry; D057930:Click Chemistry; D004926:Escherichia coli / Q000187:drug effects; D005658:Fungi / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D011804:Quinolines / Q000737:chemistry; D013211:Staphylococcus aureus / Q000187:drug effects; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000890:Anti-Infective Agents; D011804:Quinolines; D014230:Triazoles; D002599:Chalcone; C037219:quinoline
keywords: Biological activity; Chalcone; Cholesterol; Click reaction; Quinoline; Theophylline