RESUMO
A series of amino-pyridines were synthesized and evaluated for androgen antagonist activities. Among these compounds, (R)-(+)-6-[methyl-(1-phenyl-ethyl)-amino]-4-trifluoromethyl-nicotinonitrile was the most active example of this class. This compound displayed potent androgen receptor antagonist activity as well as favorable pharmacokinetic characteristics for a potential topical agent. It also demonstrated remarkable potency for stimulating hair growth in a male C3H mouse model as well as reducing sebum production in the male Syrian hamster ear model.
Assuntos
Aminopiridinas/química , Aminopiridinas/farmacologia , Antagonistas de Receptores de Andrógenos , Cabelo/efeitos dos fármacos , Cabelo/crescimento & desenvolvimento , Sebo/efeitos dos fármacos , Sebo/metabolismo , Aminopiridinas/síntese química , Animais , Relação Dose-Resposta a Droga , Masculino , Camundongos , Camundongos Endogâmicos C3H , Modelos Moleculares , Estrutura Molecular , Receptores Androgênicos/metabolismo , Relação Estrutura-AtividadeRESUMO
Synthesis, pharmacology, and pharmacokinetic profiles of (1R, 2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile are reported. This compound demonstrated remarkable potency for stimulating hair growth in a male C3H mouse model as well as reducing sebum production in the male Syrian hamster ear model.
