Synthesis and NOS regulative effect of 2-arylacylated amino pteridines

Aim:To synthesize a series of 2-arylacylated amino pteridine compounds in order to find the NOS regulators.Methods:2-amino of 2-amino-4-dimethylamino-4-arylpteridines were modified by arylacylation and their effects on iNOS activity were evalued.Results and Conclusion:A series of 2-arylacylated amino pteridine compounds(P-1～P-16) have been synthesized and their structures were confirmed by IR,UV,()~(1)H NMR,MS and EA.Pharmacological evaluation showed that arylacylation of 2-amino of mother compounds(5a～c)could lead to inhibition or activation of iNOS activity.Three compounds,P-2,P-7 and P-9 on the setting concentrations had the same effect on iNOS as BH_(4) and their minimum effective concentrations were 83.32 μmol/L,81.98 μmol/L and 79.70 μmol/L respectively.