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N-D-醛戊呋喃糖基-N'-[对-(异戊氧基)苯基]-硫脲衍生物:潜在的抗结核治疗药物。

N-D-aldopentofuranosyl-N'-[p-(isoamyloxy)phenyl]-thiourea derivatives: potential anti-TB therapeutic agents.

作者信息

Liav Avraham, Angala Shiva K, Brennan Patrick J, Jackson Mary

机构信息

Department of Microbiology, Immunology and Pathology, Colorado State University, 1682 Campus Delivery, Fort Collins, CO 80523, USA.

出版信息

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2649-51. doi: 10.1016/j.bmcl.2008.03.033. Epub 2008 Mar 14.

Abstract

Thiocarlide (THC; N,N'-bis[p-(isoamyloxy)phenyl]-thiourea; also known as isoxyl) has been used in the past as anti-tuberculosis agent. In an effort to improve the therapeutic value of THC several N-pentofuranosyl-N'-[p-(isoamyloxy)phenyl]-thiourea derivatives were synthesized by coupling of an aniline derivative and pentofuranosyl isothiocyanates. The MIC values of the new products against M.tb indicate that this new approach to the synthesis of potential anti-TB therapeutic agents was successful.

摘要

硫卡利得(THC;N,N'-双[p-(异戊氧基)苯基]-硫脲;也称为异烟肼)过去曾用作抗结核药物。为了提高硫卡利得的治疗价值,通过苯胺衍生物与戊呋喃糖基异硫氰酸酯的偶联反应合成了几种N-戊呋喃糖基-N'-[p-(异戊氧基)苯基]-硫脲衍生物。新产品对结核分枝杆菌的最低抑菌浓度值表明,这种合成潜在抗结核治疗药物的新方法是成功的。

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