Synthesis of antimicrobial agents of tetra‐substituted thiophenes from ethyl 5‐(2‐bromoacetyl)‐4‐phenyl‐2‐(phenylamino)thiophene‐3‐carboxylate,Journal of Heterocyclic Chemistry

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Synthesis of antimicrobial agents of tetra‐substituted thiophenes from ethyl 5‐(2‐bromoacetyl)‐4‐phenyl‐2‐(phenylamino)thiophene‐3‐carboxylate
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-04-25 , DOI: 10.1002/jhet.3999
Abdulrahman Alsayari ₁ , Abdullatif Bin Muhsinah ₁ , Yahya I. Asiri ₂ , Mohammad Y. Alfaifi ₃ , Serag Eldin I. Elbehairi _{3,

4} , Fatima Alatibi ₅ , Nahed Nasser E. El‐Sayed _{5,

6} , Yahia N. Mabkhot ₇

Affiliation

5‐(2‐Bromoacetyl)‐2,3,4‐trisubstituted‐thiophene was used as a synthetic intermediate to prepare a series of thiophene derivatives and thiophene incorporating oxazole, imidazole, thiazole, pyrrole, and pyridine rings via substitution and cyclo‐condensation reactions. The data were extracted from the spectra of the resulting products confirmed their suggested structures. The newly synthesized compounds were screened to evaluate their in vitro antimicrobial activity vs several positive and negative gram bacteria and fungi. The screening data revealed that the thiophene derivative 7a , incorporating a thiazole ring, displayed strong activity against all tested microorganisms when compared with the antibiotics used.

中文翻译：

由5-（2-溴乙酰基）-4-苯基-2-（苯基氨基）噻吩-3-羧酸乙酯合成四取代噻吩的抗菌剂

5-（2-溴乙酰基）-2-3,4-三取代噻吩被用作合成中间体，以制备一系列噻吩衍生物和噻吩，通过取代和环缩合并入恶唑，咪唑，噻唑，吡咯和吡啶环反应。从所得产物的光谱中提取数据，证实了其建议的结构。筛选了新合成的化合物，以评估其对几种阳性和阴性革兰氏细菌和真菌的体外抗菌活性。筛选数据表明，与所用抗生素相比，掺入噻唑环的噻吩衍生物7a对所有被测微生物表现出较强的活性。

更新日期：2020-04-25

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