Synthesis, antimicrobial and anti-inflammatory activities of some novel 5-substituted imidazolone analogs

• Published in: Chinese chemical letters Vol. 27; no. 5; pp. 707 - 710
• Main Authors: Dhingra, Ashwani Kumar, Chopra, Bhawna, Dass, Rameshwar, Mittal, Sanjeev Kumar
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.05.2016
• Subjects: Anti-inflammatory activity; Antimicrobial activity; Imidazolones; Oxazolones; 反应合成; 合成化合物; 咪唑啉酮衍生物; 抗炎活性; 抗菌; 白色念珠菌; 类似物; 革兰氏阴性细菌; Anti-inflammatory activity; Antimicrobial activity; Oxazolones; Imidazolones
• ISSN: 1001-8417; 1878-5964
• DOI: 10.1016/j.cclet.2016.01.049

In view of potent antimicrobial and anti-inflammatory activities exhibited by S-substituted imidazolones, a variety of novel imidazolone analogs 3a-I were synthesized by the condensation of different substituted oxazolones I with various aromatic amines 2. All the synthesized compounds were screened for in vitro activities against a panel of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. Several analogs produced good or moderate activities particularly against the tested Gram-positive bacteria Micrococcus luteus and Gram-negative bacteria Pseudornonas aeruginosa and, Meanwhile, compounds 3b and 3c displayed marked antifungal activity against C. albicans. In addition, the in vivo anti-inflammatory activity of the synthesized compounds was determined using the carrageenin-induced paw oedema method in rats. Two of S-substituted imidazo/one derivatives, 3k and 3d show good anti-inflammatory activity. The structures of all the newly svnthesized compounds were elucidated using IR, 1H NMR and 13C NMR.