Allophenylnorstatine-containing HIV-1 protease inhibitors: design, synthesis and structure-activity relationships for selected P2 ligands was written by Abdel-Rahman, Hamdy M.;El-Koussi, Nawal A.;Alkaramany, Gamal S.;Youssef, Adel F.;Kiso, Yoshiaki. And the article was included in Bulletin of Pharmaceutical Sciences, Assiut University in 2005.Electric Literature of C10H8O4 This article mentions the following:
The design and development of potent HIV protease inhibitors remain an attractive target for antiviral therapy. A novel class of HIV protease inhibitors containing allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4 phenylbutyric acid] as a transition state mimic have been reported. In this work we fixed P2‘ (as tert-butylamino or 2-methylbenzylamino) and changed P2 moiety to provide two series of dipeptide analogs. Preliminary evaluation of the activity of the synthesized derivatives were determined as percentage of enzyme inhibition at 5 μM level. The results showed that the introduction of 2-methylbenzylamino moiety as P2‘ ligands considerably improved HIV inhibitory activity in comparison with the tert-Bu amino analogs. It was found that compounds in both series retained activity still less than the lead compounds KNI-577 and KNI-727. In the experiment, the researchers used many compounds, for example, 7-Methoxybenzofuran-2-carboxylic acid (cas: 4790-79-8Electric Literature of C10H8O4).
7-Methoxybenzofuran-2-carboxylic acid (cas: 4790-79-8) belongs to benzofurans derivatives. Benzofuran derivatives have shown many biological activities, including antifungal and antimicrobial properties, and acting as antagonists of H3 receptors and angiotensin II. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.Electric Literature of C10H8O4
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem