Rt. Jacobs et al., SUBSTITUTED 2,4-DIAMINOQUINAZOLINES AND 2,4-DIAMINO-8-ALKYLPURINES ASANTAGONISTS OF THE NEUROKININ-2 (NK2) RECEPTOR, Bioorganic & medicinal chemistry letters, 5(23), 1995, pp. 2879-2884
Modification of the heterocyclic nucleus of a lead pyrrolopyrimidine (
1) found to be active as an antagonist at the neurokinin-2 (NK2) recep
tor is described. Compounds based on the purine nucleus (3) were found
to be particularly interesting, and were modified in the C(2), C(4) a
nd C(8) substituents to afford compounds with high potency.