噻吩-2-甲酰胺的恶二唑基、吡唑基和噻唑基衍生物作为抗菌和抗丙型肝炎病毒剂的合成

Synthesis of Oxadiazolyl, Pyrazolyl and Thiazolyl Derivatives of Thiophene-2-Carboxamide as Antimicrobial and Anti-HCV Agents.

作者信息

Rizk Ola H, Shaaban Omaima G, Abdel Wahab Abeer E

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt.

Department of Analytical and Pharmaceutical Chemistry, Faculty of Pharmacy & Drug Manufacturing, Pharos University, Alexandria, Egypt.

出版信息

Open Med Chem J. 2017 Apr 28;11:38-53. doi: 10.2174/1874104501711010038. eCollection 2017.

DOI:10.2174/1874104501711010038

PMID:28553409

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5427694/

Abstract

INTRODUCTION

Three series of pyrazole, thiazole and 1,3,4-oxadiazole, derivatives were synthesized starting from 5-amino-4-(hydrazinocarbonyl)-3-methylthiophene-2-carboxamide .

METHODS

All compounds were investigated for their preliminary antimicrobial activity. They were proved to exhibit remarkable antimicrobial activity against with insignificant activity towards Gram positive bacterial strains and fungi.

RESULTS

testing of the new compounds on hepatitis-C virus (HCV) replication in hepatocellular carcinoma cell line HepG2 infected with the virus utilizing the reverse transcription polymerase chain reaction technique (RT-PCR) generally showed inhibition of the replication of HCV RNA (-) strands at low concentration, while, eight compounds; , , , , , , and proved to inhibit the replication of HCV RNA (+) and (-) strands at very low concentration range 0.08-0.36 μg/mL.

CONCLUSION

Compounds and displayed the highest anti-HCV and antimicrobial activities in this study.

摘要

引言

以5-氨基-4-(肼基羰基)-3-甲基噻吩-2-甲酰胺为起始原料，合成了吡唑、噻唑和1,3,4-恶二唑的三个系列衍生物。

方法

对所有化合物进行了初步抗菌活性研究。结果表明，它们对革兰氏阳性菌和真菌的活性不显著，但对[此处原文缺失具体对象]具有显著的抗菌活性。

结果

利用逆转录聚合酶链反应技术（RT-PCR），在感染丙型肝炎病毒（HCV）的肝癌细胞系HepG2中，对新化合物进行HCV复制测试，结果显示，在低浓度下，新化合物一般能抑制HCV RNA（-）链的复制，而有8种化合物；[此处原文缺失具体化合物名称]，在0.08-0.36μg/mL的极低浓度范围内，能抑制HCV RNA（+）和（-）链的复制。