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

页码：716 / +

页数：12

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