Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors was written by Chen, Ping;Caldwell, Charles G.;Ashton, Wallace;Wu, Joseph K.;He, Huaibing;Lyons, Kathryn A.;Thornberry, Nancy A.;Weber, Ann E.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Category: isoxazole This article mentions the following:
A series of 4-amino cyclohexanes and 4-substituted piperidines were prepared and evaluated for inhibition of DPP-4. Analog I displayed both good DPP-4 potency and selectivity against other proteases, while derivative II displayed long half life and modest oral bioavailability in rat. The most potent analog, 3-(5-aminocarbonylpyridyl)piperidine III, displayed excellent DPP-4 activity with good selectivity vs. other proline enzymes. In the experiment, the researchers used many compounds, for example, 5-Methyl-4-isoxazolesulfonyl chloride (cas: 321309-26-6Category: isoxazole).
5-Methyl-4-isoxazolesulfonyl chloride (cas: 321309-26-6) belongs to isoxazole derivatives. Isoxazoles also form the basis for a number of drugs, including the COX-2 inhibitor valdecoxib (Bextra) and a neurotransmitter agonist AMPA. Fe(CO)5 efficiently cleaves the N–O bond of fused isoxazolo-1,4-quinones to give the corresponding imines.All the common reducing reagents failed to open the isoxazole ring.Category: isoxazole
Referemce:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem