Solubility-Driven Optimization of Phosphodiesterase-4 Inhibitors Leading to a Clinical Candidate was written by Press, Neil J.;Taylor, Roger J.;Fullerton, Joseph D.;Tranter, Pamela;McCarthy, Clive;Keller, Thomas H.;Arnold, Nicola;Beer, David;Brown, Lyndon;Cheung, Robert;Christie, Julie;Denholm, Alastair;Haberthuer, Sandra;Hatto, Julia D. I.;Keenan, Mark;Mercer, Mark K.;Oakman, Helen;Sahri, Helene;Tuffnell, Andrew R.;Tweed, Morris;Tyler, John W.;Wagner, Trixie;Fozard, John R.;Trifilieff, Alexandre. And the article was included in Journal of Medicinal Chemistry in 2012.Recommanded Product: 5912-35-6 This article mentions the following:
The solubility-driven optimization of a series of 1,7-naphthyridine phosphodiesterase-4 inhibitors is described. Directed structural changes resulted in increased aqueous solubility, enabling superior pharmacokinetic properties with retention of PDE4 inhibition. A range of potent and orally bioavailable compounds with good in vivo efficacy in animal models of inflammation and reduced emetic potential compared to previously described drugs were synthesized. Compound 2d (I) was taken forward as a clin. candidate for the treatment of COPD. In the experiment, the researchers used many compounds, for example, 6-Amino-8-bromo-1,7-naphthyridine (cas: 5912-35-6Recommanded Product: 5912-35-6).
6-Amino-8-bromo-1,7-naphthyridine (cas: 5912-35-6) belongs to naphthyridine derivatives. The naphthyridines have 10 delocalized π-electrons located in five molecular orbitals, each of which is distorted by the presence of the nitrogen atoms causing an electron drift in that direction. Halogen atoms attached to the naphthyridine moiety can be easily replaced by other nucleophiles such as alkoxides and amines.Recommanded Product: 5912-35-6
Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem