AI Article Synopsis
- Researchers developed new indane derivatives to find a CCR5 antagonist that can block HIV-1 entry.
- One of these compounds, 22a (INCB9471), showed strong binding to CCR5 and effectively inhibited HIV-1, along with being safe for use.
- INCB9471 is currently undergoing clinical trials in humans.
Article Abstract
To identify a CCR5 antagonist as an HIV-1 entry inhibitor, we designed a novel series of indane derivatives based on conformational considerations. Modification on the indane ring led to the discovery of compound 22a (INCB9471) that exhibited high affinity for CCR5, potent anti-HIV-1 activity, high receptor selectivity, excellent oral bioavailability, and a tolerated safety profile. INCB9471 has entered human clinical trials.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4007949 | PMC |
| http://dx.doi.org/10.1021/ml1001536 | DOI Listing |
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