Antimicrobial Evaluation and Docking Study of Some 2-Aryl-5-(Pyridin-3-Yl)-1,3,4-Oxadiazole Derivatives

被引:0
|
作者
Alghamdi, Saad [1 ]
Almehmadi, Mazen M. [2 ]
Asif, Mohammad [3 ]
机构
[1] Umm Al Qura Univ, Fac Appl Med Sci, Lab Med Dept, Mecca 21955, Saudi Arabia
[2] Taif Univ, Coll Appl Med Sci, Dept Clin Lab Sci, POB 11099, At Taif 21944, Saudi Arabia
[3] Glocal Univ, Glocal Sch Pharm, Saharanpur 247121, Uttar Pradesh, India
来源
LATIN AMERICAN JOURNAL OF PHARMACY | 2022年 / 41卷 / 04期
关键词
antifungal agents; heterocyclic compounds; in vitro antibacterial agents; oxadiazole; OXADIAZOLE; PYRIDONE;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1,3,4-oxadiazoles are interesting compounds because of their valuable biological effects. A new series of some 2-aryl-5-(pyridin-3-yl)-1,3,4-oxadiazole derivatives (3a-3h) were synthesized and screened for their antimicrobial activity. These compounds (3a-3h) were prepared from the reaction of nicotinic acid with ethyl alcohol converted into ethyl nicotinate (1) by esterification. Compound (1) is converted to nicotinohydrazide (2) by treating with hydrazine hydrate. Compound 2 is converted to compounds 3a-3h by treating with appropriate aromatic carboxylic acids in the presence of POCl3. Confirm of structures of the synthesized compounds by using IR, (HNMR)-H-1, and MS spectroscopy. All the title compounds were tested for in vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis (Gram-positive), Pseudomonas aeruginosa, Escherichia coli (Gram-positive) bacteria, and antifungal activity against Candida albicans and Aspergillus niger. Most of the compounds showed good activity against all the organisms. Compounds 3b, 3d, 3e, 3g, 3j, and 31 showed the highest activity against bacteria strains when compared to the standard ciprofloxacin. Compounds 3b, 3d, 3e, 3g, 3j, 3k, and 3l were showed better antifungal activity against fungal strains as compared to the standard drug griseofulvina.
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页码:772 / 777
页数:6
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