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Arylazolyl(azinyl)thioacetanilide. Part 9: Synthesis and Biological Investigation of Thiazolylthioacetamides Derivatives as a Novel Class of Potential Antiviral Agents
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  • Arylazolyl(azinyl)thioacetanilide. Part 9: Synthesis and Biological Investigation of Thiazolylthioacetamides Derivatives as a Novel Class of Potential Antiviral Agents
  • Arylazolyl(azinyl)thioacetanilide. Part 9: Synthesis and Biological Investigation of Thiazolylthioacetamides Derivatives as a Novel Class of Potential Antiviral Agents
저자명
Zhan. Peng,Wang. Liu,Liu. Hong,Chen. Xuwang,Li. Xiao,Jiang. Xin,Zhang. Qiangqiang,Liu. Xinyong,Pannecouque. Christophe,Naesens.
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2012년|35권 6호|pp.975-986 (12 pages)
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대한약학회
파일정보
정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

In continuation of our endeavor to develop new, potent, selective and less toxic antiviral agents, a novel series of 2-(2-amino/chloro-4-(2,4-dibromophenyl) thiazol-5-ylthio)acetamide derivatives was synthesized via an expeditious route and evaluated for their anti-HIV activities against wild-type virus and clinically relevant mutant strains, and for their anti-influenza virus activities against influenza A (H1N1 and H3N2) and influenza B in cellular assays. The selected active compounds were also assayed for their enzymic inhibitory activities. The results showed that some 2-chloro substituted thiazolylthioacetamide derivatives possessed potent activity against wild type HIV-1 and several key mutant strains (E138K, K103N, L100I) of HIV-1 in MT-4 cells with $EC_{50}$ values in micromolar range. Two 2-amino substituted thiazole derivatives 8a7 and 8a8 displayed significant potency against influenza A/H1N1 in MDCK cells with $EC_{50}$ values much lower than that of oseltamivir carboxylate, ribavirin, amantadine and rimantadine. Though the mechanism of actions is still unclear, these novel thiazolylthioacetamides might serve as original leads for further pharmacological investigations as potential therapeutic agents against HIV-1 or influenza virus.