新型2,4-二取代-7-甲基-1,1,3-三氧代-2H,4H-吡唑并[4,5-e][1,2,4]噻二嗪衍生物的合成及其抗HIV活性

Synthesis and anti-HIV activity of novel 2,4-disubstituted-7-methyl-1,1,3-trioxo-2H,4H-pyrazolo[4,5-e][1,2,4]thiadiazine derivatives.

作者信息

Zhan P, Yan R Z, Liu X Y, Pannecouque C, Witvrouw M, De Clercq E, Molina M T, Vega S

机构信息

Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Ji'nan, China.

出版信息

Drug Discov Ther. 2011 Dec;5(6):279-85.

PMID:22466438

Abstract

A series of novel 2,4-disubstituted-7-methyl-1,1,3-trioxo-2H,4H-pyrazolo[4,5-e][1,2,4]thiadiazines (PTDs) was prepared starting from a ring of pyrazolo[4,5-e][1,2,4]thiadiazine nuclei with two different alkyl halides obtained by a facile one-pot reaction. The structures of all synthesized compounds were confirmed by H- and C-NMR, infrared spectra (IR), and mass spectra (MS) spectroscopic analysis. Anti-HIV activity was evaluated and none of the compounds were found to inhibit HIV replication in human T-lymphocyte (MT-4) cell culture.

摘要

从吡唑并[4,5-e][1,2,4]噻二嗪核环出发，通过简便的一锅法反应，用两种不同的卤代烃制备了一系列新型的2,4-二取代-7-甲基-1,1,3-三氧代-2H,4H-吡唑并[4,5-e][1,2,4]噻二嗪（PTDs）。所有合成化合物的结构均通过氢核磁共振（H-NMR）、碳核磁共振（C-NMR）、红外光谱（IR）和质谱（MS）光谱分析得以确认。对其抗HIV活性进行了评估，结果发现所有化合物在人T淋巴细胞（MT-4）细胞培养中均未抑制HIV复制。