期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 6, 期 3, 页码 282-286出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml500463t
关键词
Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazine; PDE2 inhibitor; phosphodiesterase 2 inhibitor; tricycle; selective
A novel series of pyrido[4,3-e][1,2,4]triazolo-[4,3-a]pyrazines is reported as potent PDE2/PDE10 inhibitors with drug-like properties. Selectivity for PDE2 was obtained by introducing a linear, lipophilic moiety on the meta-position of the phenyl ring pending from the triazole. The SAR and protein flexibility were explored with free energy perturbation calculations. Rat pharmacokinetic data and in vivo receptor p or occupancy data are given for two representative compounds 6 and 12.
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