587-95-1Relevant articles and documents
Design, synthesis and anti-HIV-1 activity of modified styrylquinolines
Mahajan, Shivani,Gupta, Shiv,Jariwala, Nisha,Bhadane, Deepali,Bhutani, Late K.K.,Kulkarni, Smita,Singh, Inder Pal
, p. 937 - 944 (2018/08/17)
Background: Drug resistance and reservoirs of latent viral infection have prevented total eradication of the HIV-virus which underlines the need for continuous efforts in the discovery of new anti-HIV agents. The present study deals with the synthesis of novel compounds based on naturally occurring scaffolds and their evaluation as potential anti-HIV agents. Objective: Design and synthesis of styrylquinoline scaffold based new molecules and evaluation of their anti-HIV-1 activity. Methods: A series of forty three new styrylquinolines (SQLs) was designed and synthesized. The newly synthesized compounds were tested for anti-HIV-1 activity against HIV-1VB59 and HIV-1UG070 primary isolates in TZM-bl cell lines. Results: The most active compounds 9 and 34 (IC50 = 0.5-4.0 μM), also exhibited significant inhibition activity against HIV-1VB51 primary isolate in PBMCs (IC50 = 7.3 μM). Compounds 9 and 34 were also found to inhibit HIV-1 entry into host cells and fusion inhibitory activities. The study encourages further exploration of SQL nucleus to design anti-HIV-1 agents. Conclusion: The study encourages further exploration of SQL nucleus to design anti-HIV-1 agents.
A one pot microwave assisted synthesis of 3-acyl-2,4-dihydroxyquinoline followed by synthesis of 7-methyldibenzo[c,f][2,7]naphthyridin-6(5H)-ones via three routes
Pitchai,Uvarani,Gengan,Mohan
, p. 776 - 786 (2013/07/26)
An easy one pot microwave assisted synthesis of 3-acyl-2,4- dihydroxyquinoline from simple precursors followed by convenient synthesis of novel and potential HIV integrase inhibitors 7-methyldibenzo[c,f][2,7] naphthyridin-6(5H)-ones has been achieved through three different routes. Mild reaction conditions and good yields are obtained by applying microwave and photochemical techniques.
Convenient and efficient microwave-assisted synthesis of a methyl derivative of the fused indoloquinoline alkaloid cryptosanguinolentine
Gengan, Robert M.,Pandian, Pitchai,Kumarsamy, Chandraprakash,Mohan, Palathurai S.
experimental part, p. 3171 - 3178 (2010/09/04)
An efficient synthesis of a methyl derivative of the indoloquinoline alkaloid cryptosanguinolentine based on microwave-assisted reactions is described. The microwave-assisted synthesis of an intermediate 4-hydroxy-2-methylquinoline yielded 86% of the desired product and other intermediates prepared yielded high % of products in shorter reaction times, under optimum conditions, as compared to traditional methods.
