Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists.

Autor: Corbett JW; Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA. jeffrey.w.corbett@pfizer.com, Rauckhorst MR, Qian F, Hoffman RL, Knauer CS, Fitzgerald LW
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Nov 15; Vol. 17 (22), pp. 6250-6. Date of Electronic Publication: 2007 Sep 07.
DOI: 10.1016/j.bmcl.2007.09.008
Abstrakt: Low nanomolar corticotropin releasing factor type-1 (CRF(1)) receptor antagonists containing unique indanylamines were identified from the heteroatom-linked pyrazine chemotype. The most potent indanylpyrazine had a K(i)=11+/-1 nM. The oxygen-linked pyrazinyl derivatives were prepared through a copper-catalyzed coupling of a pyridinone to a bromo- or iodopyrazine.
Databáze: MEDLINE