Pyrazolo-[1,5-a]-1,3,5-triazine corticotropin-releasing factor (CRF) receptor ligands

Paul J Gilligan¹, Beverly K Folmer, Richard A Hartz

¹Bristol-Myers Squibb Co., Discovery Chemistry Department and E.I. DuPont de Nemours and Co., Central Research and Development Department, Experimental Station, Wilmington, DE 19880-0500, USA. paul.j.gilligan@bms.squibb

|August 21, 2003

Abstract:

The syntheses and rat CRF receptor binding affinities of 'retro-pyrazolotriazine' corticotropin-releasing factor (CRF) ligands 4 are reported. Some have high affinity for rat CRF receptors (K(i)< or =10 nM). The data provide additional support for the hypothesis that it is possible to interchange isosteric cores with similar electronic properties in the design of high-affinity CRF receptor ligands, provided the peripheral pharmacophore elements are maintained in the same three-dimensional array.

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Pyrazolo-[1,5-a]-1,3,5-triazine corticotropin-releasing factor (CRF) receptor ligands

Abstract:

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