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Sana Aslam,Matloob Ahmad,Muhammad Zia-ur-Rehman,Catherine Montero,Mervi Detorio,Masood Parvez,Raymond F. Schinazi 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.11
A novel series of N0-(1-(aryl)ethylidene)-2-(5,5-dioxido-3-phenylbenzo[e]pyrazolo[4,3-c][1,2]thiazin-4(1H)-yl)acetohydrazides was synthesized. The synthesiswas carried out by thermal method as well as ultrasonicbath to reduce reaction time and to enhance product yields. The synthesized compounds were characterized by spectroscopictechniques like NMR, infrared and EIMS. Thestructure of compound 5w was elucidated by X-ray crystallography. The titled compounds were evaluated for antihumanimmunodeficiency virus type 1 (anti-HIV-1) andcytotoxic activities. Biological studies indicated thatamongst these compounds, 5a, b, j, h and i showed theactivity with median effective concentration (EC50) valuesless than 20 lM. Compound 5i exhibited the most potentanti-HIV-1 activity (EC50 = 3.2 lM) while 5h showedanti-HIV-1 activity (EC50 = 3.8 lM) with no toxicity at allin primary human lymphocytes, CEM and VERO cells.