| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10596216 | Bioorganic & Medicinal Chemistry Letters | 2013 | 8 Pages |
Abstract
The design and synthesis of novel HIV-1 protease inhibitors (PIs), which display high potency against HIV-1 wild-type and multi-PI-resistant HIV-mutant clinical isolates, is described. Lead optimization was directed towards the discovery of new PIs suitable for a long-acting injectable drug application for treating HIV/AIDS. The two most potent HIV-1 PIs 18 and 22, formulated as nanosuspensions, showed interesting compound release profiles over two months when injected intramuscularly in rats.
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Authors
Bart Kesteleyn, Katie Amssoms, Wim Schepens, Geerwin Hache, Wim Verschueren, Wim Van De Vreken, Klara Rombauts, Greet Meurs, Patrick Sterkens, Bart Stoops, Lieven Baert, Nigel Austin, Jörg Wegner, Chantal Masungi, Inge Dierynck, Stina Lundgren,