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. 2020 Nov 1;30(21):127516.
doi: 10.1016/j.bmcl.2020.127516. Epub 2020 Aug 27.

Design, synthesis and SAR study of novel C2-pyrazolopyrimidine amides and amide isosteres as allosteric integrase inhibitors

Manoj Patel  1 , Christopher Cianci  2 , Christopher W Allard  3 , Dawn D Parker  4 , Jean Simmermacher  4 , Susan Jenkins  4 , Brian Mcauliffe  5 , Beatrice Minassian  2 , Linda Discotto  2 , Mark Krystal  5 , Nicholas A Meanwell  3 , B Narasimhulu Naidu  4
Affiliations

Design, synthesis and SAR study of novel C2-pyrazolopyrimidine amides and amide isosteres as allosteric integrase inhibitors

Manoj Patel et al. Bioorg Med Chem Lett. .

Abstract

The design, synthesis and structure-activity relationships associated with a series of C2-substituted pyrazolopyrimidines as potent allosteric inhibitors of HIV-1 integrase (ALLINIs) are described. Structural modifications to these molecules were made in order to examine the effect on potency and, for select compounds, pharmacokinetic properties. We examined a variety of C2-substituted pyrazolopyrimidines and found that the C2-amide derivatives demonstrated the most potent antiviral activity of this class against HIV-1 infection in cell culture.

Keywords: Allosteric integrase inhibitors; HIV; HIV-1 integrase; LEDGF/p75; Pyrazolopyrimidine.

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Conflict of interest statement

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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