@article{Shafiq_Eldeen_Al-kaissi_Al-adham_2016, title={SYNTHESIS, STRUCTURAL ELUCIDATION AND ANTIMICROBIAL EVALUATION OF 2-{4-(T-AMINO)-2-(BUT-2-YN-1-YL)}-1, 3 BENZOTHIAZOLE DERIVATIVES}, volume={8}, url={https://journals.innovareacademics.in/index.php/ijpps/article/view/10414}, abstractNote={<p><strong>Objective</strong>:<strong> </strong>A new series of 2-{4-(t-amino)-2-(but-2-yn-1-yl)}-1,3-benzothiazole<em> </em>derivatives, 2-[4-(pyrrolidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ2), 2-[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ3), 2-[4-(piperidin-1-yl) but-2-yn-1-yl]-1,3-benzothiazole (BZ4), 2-[4-(azepan-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ5), 2-[4-(4-methylpiperazin-1-yl) but-2-yn-1-yl]-1,3-benzothiazole (BZ6), 2-[4-(2, 6-dimethylpiperidin-1-yl) but-2-yn-1-yl]-1, 3-benzothiazole (BZ7) were synthesized and screened <em>in vitro </em>as potential antimicrobial agents.</p><p><strong>Methods</strong>:<strong> </strong><em>In-vitro </em>antimicrobial activity evaluation was done, by agar diffusion method and broth dilution test against <em>Staphylococcus aureus</em> ATCC 6538p, <em>Candida albicans</em> ATCC 10231, <em>Pseudomonas aeruginosa</em> ATCC 9027, <em>Escherichia coli </em>ATCC 8739, and <em>Bacillus subtilis</em> ATCC 6633. Minimum inhibitory concentration (MIC) and Minimum bactericidal concentration (MBC) were determined. The results of antimicrobial testing were compared to two positive control drugs ciprofloxacin (5 µg/ml) and fluconazole (500µg/ml).</p><p><strong>Results</strong>:<strong> </strong>Compound 2-[4-(azepan-1-yl) but-2-yn-1-yl]-1,3-benzothiazole<em> </em>(BZ5)<strong> </strong>showed the highest antibacterial activity against <em>S. aureus</em> with MIC value of 15.62 µg/ml while; Compound 2-[4-(2,6-dimethylpiperidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ7) exhibited the highest antibacterial activity against <em>P. aeruginosa</em> with MIC value of 31.25 µg/ml. Compounds<strong> </strong>2-[4-(pyrrolidin-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ2) and 2-[4-(azepan-1-yl)but-2-yn-1-yl]-1,3-benzothiazole (BZ5) showed the highest antifungal activity against <em>C. albicans</em> with MIC value of 15.62 µg/ml (for both).</p><p><strong>Conclusion</strong>:<strong> </strong>The results obtained showed variation in the antibacterial and antifungal activity based on the structure of the cyclic amines in these amino acetylenic benzothiazole derivatives.<em> </em><em></em></p><p dir="RTL"><strong>Keywords</strong>:<strong> </strong>Benzothiazole, Aminoacetylenic, Antibacterial, Antifungal, Mannich reaction</p>}, number={4}, journal={International Journal of Pharmacy and Pharmaceutical Sciences}, author={Shafiq, Bahaa and Eldeen, Zuhair Muhi and Al-kaissi, Elham and Al-adham, Ibrahim S}, year={2016}, month={Apr.}, pages={189–193} }