Substituted indoles as HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent evaluation (WO2015044928)

ABSTRACT

The invention described in this patent (WO2015044928) is related to compounds based on the substituted indole scaffold, their synthetic process and application to inhibit HIV-1 replication as non-nucleoside reverse transcriptase inhibitors (NNRTIs). Some of the newly claimed compounds presented improved potency against wild-type (WT) HIV-1 strain in comparison to previously disclosed indole-based NNRTIs and were also shown to be effective against common resistant HIV-1 strains. In light of their novel structural characteristics, simple synthetic route and improved anti-HIV activity, these compounds deserve further study as promising NNRTIs.

KEYWORDS:

• HIV
• non-nucleoside reverse transcriptase inhibitors
• substituted indole
• heterocycle
• antiviral activity

Financial and competing interests disclosure

The authors were supported by the financial support from the Key Project of National Natural Science Foundation of China for International Cooperation (No. 81420108027); the National Natural Science Foundation of China (No. 81573347, 81273354); Research Fund for the Doctoral Program of Higher Education of China (No. 20110131130005) and the Science and Technology Development Project of Shandong Province (No. 2014GSF118175). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.