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Facile synthesis of highly functionalized novel pyrazolopyridones using oxoketene dithioacetal and their anti-HIV activity

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dc.contributor.author Savant, Mahesh M.
dc.contributor.author Ladva, Kartik D.
dc.contributor.author Pandit, Archna B.
dc.date.accessioned 2023-05-03T03:13:59Z
dc.date.available 2023-05-03T03:13:59Z
dc.date.issued 2018-06-08
dc.identifier.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 en_US
dc.identifier.issn 1532-2432
dc.identifier.uri http://10.9.150.37:8080/dspace//handle/atmiyauni/842
dc.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. en_US
dc.description.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. en_US
dc.description.sponsorship UGC-MiRP, New Delhi en_US
dc.language.iso en en_US
dc.publisher Synthetic Communications, Taylor & Francis en_US
dc.subject Anti-HIV activity en_US
dc.subject highly functionalized pyrazolopyridone en_US
dc.subject ketene dithioacetals en_US
dc.subject MTT method en_US
dc.title Facile synthesis of highly functionalized novel pyrazolopyridones using oxoketene dithioacetal and their anti-HIV activity en_US
dc.type Article en_US


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