作为潜在抗菌剂的新型 2-(5-Aryl-1-phenyl-1H-pyrazol-3-yl)-4-aryl 噻唑衍生物的合成与生物筛选,ACS Omega

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作为潜在抗菌剂的新型 2-(5-Aryl-1-phenyl-1H-pyrazol-3-yl)-4-aryl 噻唑衍生物的合成与生物筛选
ACS Omega ( IF 3.7 ) Pub Date : 2023-02-22 , DOI: 10.1021/acsomega.2c08137
Yogesh Nandurkar _{1,

2} , Abhijit Shinde ₁ , Manish R Bhoye _{1,

3} , Shivaji Jagadale ₄ , Pravin Chimaji Mhaske ₁

Affiliation

通过5 - aryl - 1 - phenyl- 1 H -pyrazole-3-carbothioamide ( 7a – d ) 与取代的苯甲酰溴 ( 8a – f )。新合成的 2-(5-aryl-1-phenyl-1 H -pyrazol-3-yl)-4-aryl thiazole ( 10a – ab ) 衍生物的结构通过光谱分析表征。对化合物10a - ab 的体外抗菌活性进行了评估大肠杆菌(NCIM 2574)、奇异变形杆菌(NCIM 2388)、枯草芽孢杆菌(NCIM 2063)、金黄色葡萄球菌(NCIM 2178)，以及对黑曲霉(ATCC 504) 和白色念珠菌(NCIM 3100) 的体外抗真菌活性。在28个吡唑基-噻唑衍生物中，10g、10h、10i、10j、10o和10t这6个化合物对奇异变形杆菌表现出良好的活性；四种化合物10q , 10u ,10y和10z对金黄色葡萄球菌表现出良好的活性；24个衍生物对黑曲霉表现出良好的抗真菌活性。化合物10g、10q、10r、10s和10ab显示出与参考药物 Ravuconazole 相当的活性。因此，2-(5-aryl-1-phenyl- 1H -pyrazol-3-yl)-4-aryl thiazole ( 10a – ab ) 衍生物的显着抗菌活性促使这些支架有助于先导化合物的开发治疗微生物感染。

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Synthesis and Biological Screening of New 2-(5-Aryl-1-phenyl-1H-pyrazol-3-yl)-4-aryl Thiazole Derivatives as Potential Antimicrobial Agents

A new series of 2-(5-aryl-1-phenyl-1H-pyrazol-3-yl)-4-aryl thiazoles (10a–ab) have been synthesized by a cyclocondensation reaction of 5-aryl-1-phenyl-1H-pyrazole-3-carbothioamide (7a–d) with substituted phenacyl bromide (8a–f). The structure of newly synthesized 2-(5-aryl-1-phenyl-1H-pyrazol-3-yl)-4-aryl thiazole (10a–ab) derivatives was characterized by spectroscopic analysis. The compounds 10a–ab were evaluated for in vitro antibacterial activity against Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388), Bacillus subtilis (NCIM 2063), Staphylococcus aureus (NCIM 2178), and in vitro antifungal activity against Aspergillus niger (ATCC 504) and Candida albicans (NCIM 3100). Among the twenty-eight pyrazolyl-thiazole derivatives, six compounds, 10g, 10h, 10i, 10j, 10o, and 10t, showed good activity against P. mirabilis; four compounds 10q, 10u, 10y, and 10z showed good activity against S. aureus; and twenty-four derivatives showed good antifungal activity against A. niger. Compounds 10g, 10q, 10r, 10s, and 10ab showed comparable activity with respect to the reference drug Ravuconazole. Thus, the significant antimicrobial activity of 2-(5-aryl-1-phenyl-1H-pyrazol-3-yl)-4-aryl thiazole (10a–ab) derivatives prompted that these scaffolds could assist in the development of lead compounds to treat microbial infections.

更新日期：2023-02-22

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