Addressing species specific metabolism and solubility issues in a quinoline series of oral PDE4 inhibitors was written by Lunniss, C.;Eldred, C.;Aston, N.;Craven, A.;Gohil, K.;Judkins, B.;Keeling, S.;Ranshaw, L.;Robinson, E.;Shipley, T.;Trivedi, N.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Related Products of 3528-58-3 This article mentions the following:
Species specific conversion of the lead PDE4 inhibitor 1 to the quinolone 3 was identified as the major route of metabolism in the cynomolgus monkey. Modification of the template to give the cinnoline 9 retained potency and selectivity, and greatly improved the pharmacokinetic profile in the cynomolgus monkey compared with 1. Addnl. SAR studies aimed at improving the solubility of 9 are also described. In the experiment, the researchers used many compounds, for example, 1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3Related Products of 3528-58-3).
1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of both electronegative nitrogen atoms in the pyrazole ring reduces the electron density of the C3- and C5-positions leaving electron density of C4-position unaltered. Thus the C4-position is vulnerable to electrophilic attack. The C3 electrophilic-position may undergo deprotonation in the presence of a strong base leading to ring opening.Related Products of 3528-58-3
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics