Please use this identifier to cite or link to this item: http://10.9.150.37:8080/dspace//handle/atmiyauni/841
Title: Facile synthesis of highly functionalized novel pyrazolopyridones using oxoketene dithioacetal and their anti-HIV activity
Authors: Savant, Mahesh M.
Ladva, Kartik D.
Pandit, Archna B.
Keywords: Anti-HIV activity
highly functionalized pyrazolopyridone
ketene dithioacetals
MTT method
Issue Date: 8-Jun-2018
Publisher: Synthetic Communications, Taylor & Francis
Citation: Mahesh M. Savant, Kartik D. Ladva & Archna B. Pandit (2018) Facile synthesis of highly functionalized novel pyrazolopyridones using oxoketene dithioacetal and their anti-HIV activity, Synthetic Communications, 48:13, 1640-1648, DOI: 10.1080/00397911.2018.1458239
Abstract: A series of novel 3-amino-4,5-dihydro-6-methyl-4-oxo-N-aryl-1H pyrazolo[4,3-c]pyridine-7-carboxamide have been synthesized starting from various oxoketene dithioacetals. The cyclocondensation reaction of 2-(bis(methylthio)methylene)-3-oxo-N-arylbutanamide 2a–w with cyanoacetamide using NaOiPr as base under reflux condition afforded novel highly functionalized pyridone 3a–w derivatives. Further, [3 þ 2] cyclocondensation reaction of pyridones with hydrazine in the presence of alcohol was yielded pyrazolopyridones (23 nos) 4a–w with excellent yields. All newly synthesized compounds were evaluated for in vitro anti-HIV activity using MTT method. Most of these compounds have showed moderate to potent activity against HIV-1 (IIIB) and HIV-2 (ROD) strains with an IC50 ranging from >18 IC50 [µg/ml] to <100 IC50[µg/ml]. Among them, compounds 4j and 4v were identified as the most promising compound for both types of HIV strains. (IC50 ¼ 18 µg/ml). Three compounds 4l, 4m, and 4p have been found potent anti-HIV 1 and 2 activity against MT-4 cells.
Description: Authors are thankful for financial assistance given under UGC-MiRP, New Delhi, Sanction No.: 47-605/13(WRO); Dated: 20/05/2014 and Shree M. & N. Virani Science College, Rajkot for providing central instrumentation & laboratory facilities and Prof. Pannecouque Rega Institute for Medical Research, KU Leuven, Belgium for providing Anti-HIV analysis.
URI: http://10.9.150.37:8080/dspace//handle/atmiyauni/841
ISSN: 1532-2432
Appears in Collections:01. Journal Articles

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