Synthesis of novel pyrazolobenzothiazine 5,5-dioxide derivatives as potent anti-HIV-1 agents

被引：30

作者：

Ahmad, Matloob ^{[1
]}

Aslam, Sana ^{[2
,3
]}

Bukhari, Mujahid Hussain ^{[2
]}

Montero, Catherine ^{[4
]}

Detorio, Mervi ^{[4
]}

Parvez, Masood ^{[5
]}

Schinazi, Raymond F. ^{[4
]}

机构：

[1] Govt Coll Univ, Dept Chem, Faisalabad 38000, Pakistan

[2] Univ Punjab, Inst Chem, Lahore 54590, Pakistan

[3] Govt Coll Women Univ, Dept Chem, Faisalabad, Pakistan

[4] Emory Univ, Sch Med, Vet Affairs Med Ctr, Biochem Pharmacol Lab, Atlanta, GA 30322 USA

[5] Univ Calgary, Dept Chem, Calgary, AB T2N 1N4, Canada

来源：

MEDICINAL CHEMISTRY RESEARCH | 2014年 / 23卷 / 03期

关键词：

Heterocyclic compounds; Biological activity; 1,2-Benzothiazine 1,1-dioxide; Pyrazolobenzothiazines; Anti-HIV-1; activity; Cytotoxic studies; ANTIBACTERIAL ACTIVITIES; 1,1-DIOXIDE; TENOFOVIR; VIRUS; EMTRICITABINE; ANTIOXIDANT; EFAVIRENZ; ANALOGS; HIV;

D O I：

10.1007/s00044-013-0718-x

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of pyrazolobenzothiazine-based carbohydrazides was prepared in a facile way, starting with commercially available sodium saccharine. The final products were sufficiently characterized by spectroscopic techniques. In addition, compound 5k was confirmed with X-ray crystallography as well. All the compounds were screened for anti-HIV-1 and cytotoxicity activities. Overall, out of 15 compounds, seven exhibited good activity with EC50 values < 20 mu M. Compounds 5c, 5d, 5g, 5j and 5k appeared as the potent anti-HIV-1 agents with EC50 values < 5.0 mu M. The structure-activity relationship would facilitate the discovery of new molecules with better profile of HIV inhibition activity.

引用

页码：1309 / 1319

页数：11

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