TY - JOUR AU - Amin, Kamilia M. AU - Abou-seri, Sahar M. AU - Abdelnaby, Rana M. AU - Rateb, Heba S. AU - Khalil, Mahmoud A. F. AU - Hussein, Mohamed M. PY - 2016/04/01 Y2 - 2024/03/29 TI - SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL COUMARIN DERIVATIVES AS POTENTIAL ANTIMICROBIAL AGENTS JF - International Journal of Pharmacy and Pharmaceutical Sciences JA - Int J Pharm Pharm Sci VL - 8 IS - 4 SE - Original Article(s) DO - UR - https://journals.innovareacademics.in/index.php/ijpps/article/view/10652 SP - 109-116 AB - <p><strong>Objective: </strong>Synthesize new series of 7-hydroxy-4-methylcoumarin and 7-alkoxy-4-methylcoumarin derivatives featuring thiosemicarbazone or thiazolidin-4-one moieties and to evaluate their antimicrobial activity against two strains of Gram-positive bacteria<em> (Staphylococcus aureus</em> and <em>Bacillus subtilis)</em>, two Gram-negative bacteria<em> (Escherichia Coli</em> and <em>Pseudomonas aeruginosa)</em>, and <em>Candida albicans</em>.</p><p><strong>Methods: </strong>Preparation of the new coumarin derivatives was done by adopting Pechmann condensation and attaching different isothiocyanates to give coumarin-thiosemicarbazone hybrids. Thiosemicarbazones were cyclized into thiazolidine-4-ones using chloroacetic acid or diethyl bromo malonate.</p><p><strong>Results: </strong>Compounds VIb, Xb, XIVb, and XVc gave the highest inhibition zones (&gt;20 mm) against <em>Staphylococcus aureus. </em>Their MIC (minimum inhibitory concentration) values ranging from 0.19-0.36 µg/ml were better than the reference drug tobramycin with MIC= 2µg/ml.</p><p><strong>Conclusion: </strong>The newly synthesized compounds with the 7-hydroxyl group showed better antimicrobial activity than those with the 7-alkoxy groups.</p><p><strong>Keywords: </strong>Coumarin, Thiosemicarbazones, Thiazolidin-4-ones, Antimicrobial activity</p> ER -