Liu, Chunjian et al. published their research in Journal of Medicinal Chemistry in 2005 | CAS: 3528-58-3

1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. The 1H-pyrazole provides an excellent means by which to provide the requisite hydrogen bond acceptor–donor motifs, whether as a monocyclic ring or as a fused indazole ring. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.Recommanded Product: 3528-58-3

5-Cyanopyrimidine Derivatives as a Novel Class of Potent, Selective, and Orally Active Inhibitors of p38α MAP Kinase was written by Liu, Chunjian;Wrobleski, Stephen T.;Lin, James;Ahmed, Gulzar;Metzger, Axel;Wityak, John;Gillooly, Kathleen M.;Shuster, David J.;McIntyre, Kim W.;Pitt, Sidney;Shen, Ding Ren;Zhang, Rosemary F.;Zhang, Hongjian;Doweyko, Arthur M.;Diller, David;Henderson, Ian;Barrish, Joel C.;Dodd, John H.;Schieven, Gary L.;Leftheris, Katerina. And the article was included in Journal of Medicinal Chemistry in 2005.Recommanded Product: 3528-58-3 This article mentions the following:

A novel class of 5-cyanopyrimidine-based inhibitors of p38α MAP kinase has been investigated. Analogs optimized through SAR iterations display low nanomolar enzymic and cellular activity. The in vivo efficacy of this class of p38 inhibitors was demonstrated by 3a and 3b (>50% reduction in TNF levels when orally dosed at 5 mg/kg, 5 h prior to LPS administration in an acute murine model of inflammation). For 3a and 3b, the previously identified N-methoxybenzamide moiety (1) was replaced with N-(isoxazol-3-yl)benzamide, thereby providing increased metabolic stability. Cyanopyrimidine 3a demonstrated 100% oral bioavailability in mouse. High p38 kinase selectivity vs. over 20 kinases was observed for analog 3b. Direct hydrogen bonding of the cyano nitrogen of the 5-cyanopyrimidine core to the backbone NH of Met109 was confirmed by x-ray crystallog. anal. of 3a bound to p38α. In the experiment, the researchers used many compounds, for example, 1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3Recommanded Product: 3528-58-3).

1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. The 1H-pyrazole provides an excellent means by which to provide the requisite hydrogen bond acceptor–donor motifs, whether as a monocyclic ring or as a fused indazole ring. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.Recommanded Product: 3528-58-3

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics