SYNTHESIS OF SOME NOVEL THIOPHENE AND THIAZOLE DERIVATIVES AND THEIR ANTIMICROBIAL EVALUATION

被引：4
|
作者：
Mohamed, Hanan A. [1 ]
Abdel-Wahab, Bakr F. [1 ]
El-Hiti, Gamal A. [2 ]
机构：
[1] Natl Res Ctr, Appl Organ Chem Dept, Giza, Egypt
[2] King Saud Univ, Coll Appl Med Sci, Dept Optometry, Cornea Res Chair, POB 10219, Riyadh 11433, Saudi Arabia
来源：
HETEROCYCLES | 2017年 / 94卷 / 04期
关键词：
Phenyl Isothiocyanate; Thiazole; Thiophene; 1,2,3-Triazole; Antimicrobial Activity; PI3K INHIBITORS; ENAMINONES; KETENE-N; S-ACETALS; PYRIDIN-2(1H)-ONES; LITHIATION; CHEMISTRY; POTENT;
D O I：
10.3987/COM-17-13668
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Reactions of phenyl isothiocyanate with several active methylene compounds 1 (3-oxo-3-phenylpropanenitrile, ethyl 2-cyanoacetate, pentane-2,4-dione and ethyl acetoacetate) and a molar equivalent of potassium hydroxide in dimethylformamide afforded potassium 1-(phenylamino)ethenethiolates as intermediates 2. Reactions of 2 and 2-bromo-1-(5-methyl-1-(4-tolyl)-1H-1,2,3-triazol-4-yl)ethanone (3) afforded novel thiazole and thiophene derivatives 4, 12, 13 and 23a,b in 68-78% yields. The structures of the synthesized products were confirmed using various spectroscopic techniques and single X-ray crystal structures. The novel thiophenes and thiazoles showed good antimicrobial activities against the tested bacteria and fungi.
引用
收藏
页码：716 / +
页数：12
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