Synthesis and in–vitro anti–HIV–1 evaluation of novel pyrazolo[4,3–c]pyridin–4–one derivatives
European Journal of Medicinal Chemistry, ISSN: 0223-5234, Vol: 183, Page: 111714
2019
- 23Citations
- 13Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
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Metrics Details
- Citations23
- Citation Indexes23
- 23
- CrossRef20
- Captures13
- Readers13
- 13
Article Description
In our continuing efforts to find novel anti–HIV compounds, we have synthesized sixteen novel pyrazolo[4,3–c]pyridin–4–one derivatives. All the synthesized compounds were screened for anti–HIV activity against HIV–1 VB59 (R5, subtype C). Compounds 12a–12c and 12e were also tested against HIV–1 UG070 (X4, subtype D) in TZM–bl cell line. Compound 12c was found to be the most active against HIV–1 VB59 and HIV–1 UG070 with IC 50 value 3.67 μM and 2.79 μM, and therapeutic indices 185 and 243, respectively. The lead compound 12c inhibited the HIV-192/BR/018 (R5, subtype B) and drug resistant isolates, NIH-119 (X4/R5, subtype B) and NARI-DR (R5, subtype C) effectively. The activity of the lead compound was further confirmed by PBMC assays. The molecular docking data showed that the most active compound 12c binds in the non-nucleoside binding pocket of HIV-1 reverse transcriptase, which was confirmed by the ToA assay. Thus the study indicated that 12c may be considered as a NNRTI and further explored as a lead for anti-HIV drug development.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0223523419308669; http://dx.doi.org/10.1016/j.ejmech.2019.111714; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85072394098&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/31557609; https://linkinghub.elsevier.com/retrieve/pii/S0223523419308669; https://dx.doi.org/10.1016/j.ejmech.2019.111714
Elsevier BV
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