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KMID : 0043320140370111380
Archives of Pharmacal Research
2014 Volume.37 No. 11 p.1380 ~ p.1393
Synthesis and anti-HIV-1 screening of novel N¡Ç-(1-(aryl)ethylidene)-2-(5,5-dioxido-3-phenylbenzo[e]pyrazolo[4,3-c][1,2]thiazin-4(1H)-yl)acetohydrazides
Aslam Sana

Ahmad Matloob
Zia ur Rehman Muhammad
Montero Catherine
Detorio Mervi
Parvez Masood
Schinazi Raymond F.
Abstract
A novel series of N¡Ç-(1-(aryl)ethylidene)-2-(5,5-dioxido-3-phenylbenzo[e]pyrazolo[4,3-c][1,2]thiazin-4(1H)-yl)acetohydrazides was synthesized. The synthesis was carried out by thermal method as well as ultrasonic bath to reduce reaction time and to enhance product yields. The synthesized compounds were characterized by spectroscopic techniques like NMR, infrared and EIMS. The structure of compound 5w was elucidated by X-ray crystallography. The titled compounds were evaluated for anti-human immunodeficiency virus type 1 (anti-HIV-1) and cytotoxic activities. Biological studies indicated that amongst these compounds, 5a, b, j, h and i showed the activity with median effective concentration (EC50) values less than 20 ¥ìM. Compound 5i exhibited the most potent anti-HIV-1 activity (EC50 = 3.2 ¥ìM) while 5h showed anti-HIV-1 activity (EC50 = 3.8 ¥ìM) with no toxicity at all in primary human lymphocytes, CEM and VERO cells.
KEYWORD
Pyrazolobenzothiazine, Hydrazides, Cytotoxic activity, Anti-HIV-1 activity
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