Nandurkar Yogesh, Shinde Abhijit, Bhoye Manish R, Jagadale Shivaji, Mhaske Pravin Chimaji
Post-Graduate Department of Chemistry, S. P. Mandali's Sir Parashurambhau College, Tilak Road, Pune 411030, India.
Department of Chemistry, Nowrosjee Wadia College, Pune 411001, India.
ACS Omega. 2023 Feb 22;8(9):8743-8754. doi: 10.1021/acsomega.2c08137. eCollection 2023 Mar 7.
A new series of 2-(5-aryl-1-phenyl-1-pyrazol-3-yl)-4-aryl thiazoles (-) have been synthesized by a cyclocondensation reaction of 5-aryl-1-phenyl-1-pyrazole-3-carbothioamide (-) with substituted phenacyl bromide (-). The structure of newly synthesized 2-(5-aryl-1-phenyl-1-pyrazol-3-yl)-4-aryl thiazole (-) derivatives was characterized by spectroscopic analysis. The compounds - were evaluated for antibacterial activity against (NCIM 2574), (NCIM 2388), (NCIM 2063), (NCIM 2178), and antifungal activity against (ATCC 504) and (NCIM 3100). Among the twenty-eight pyrazolylthiazole derivatives, six compounds, , , , , , and , showed good activity against ; four compounds , , , and showed good activity against ; and twenty-four derivatives showed good antifungal activity against . Compounds , , , , and showed comparable activity with respect to the reference drug Ravuconazole. Thus, the significant antimicrobial activity of 2-(5-aryl-1-phenyl-1-pyrazol-3-yl)-4-aryl thiazole (-) derivatives prompted that these scaffolds could assist in the development of lead compounds to treat microbial infections.
通过5-芳基-1-苯基-1-吡唑-3-碳硫酰胺（-）与取代苯甲酰溴（-）的环缩合反应，合成了一系列新的2-（5-芳基-1-苯基-1-吡唑-3-基）-4-芳基噻唑（-）。通过光谱分析对新合成的2-（5-芳基-1-苯基-1-吡唑-3-基）-4-芳基噻唑（-）衍生物的结构进行了表征。评估了这些化合物对金黄色葡萄球菌（NCIM 2574）、大肠杆菌（NCIM 2388）、枯草芽孢杆菌（NCIM 2063）、铜绿假单胞菌（NCIM 2178）的抗菌活性，以及对白色念珠菌（ATCC 504）和热带念珠菌（NCIM 3100）的抗真菌活性。在28种吡唑基噻唑衍生物中，6种化合物，即[具体化合物名称未给出]，对金黄色葡萄球菌表现出良好的活性；4种化合物[具体化合物名称未给出]对大肠杆菌表现出良好的活性；24种衍生物对白色念珠菌表现出良好的抗真菌活性。化合物[具体化合物名称未给出]与参考药物瑞伏康唑表现出相当的活性。因此，2-（5-芳基-1-苯基-1-吡唑-3-基）-4-芳基噻唑（-）衍生物的显著抗菌活性表明，这些支架可有助于开发用于治疗微生物感染的先导化合物。
