N-(4-aminobutyl)-N'-(2-methoxyethyl)guanidine (8a) is as a potent inhibitor targeting the hDDAH-1 active site (Ki = 18 µM) and derived from a series of guanidine- and amidine-based inhibitors. Its non-amino acid nature leads to high selectivities towards other enzymes of the nitric oxide-modulating system. Crystallographic data of 8a-bound hDDAH-1 illuminated a unique binding mode. Together with its developed N-hydroxyguanidine prodrug 11, 8a will serve as a most widely applicable, currently available pharmacological tool to target DDAH-1-associated diseases.

N-(4-aminobutyl)-N'-(2-methoxyethyl)guanidine (8a) is a potent, non-amino acid inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) with high select

Journal of medicinal chemistry

Discovery of N-(4-Aminobutyl)-N'-(2-Methoxyethyl)guanidine as the First Selective, Non-Amino Acid, Catalytic Site Inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1).

Paper

Discovery of N-(4-Aminobutyl)-N'-(2-Methoxyethyl)guanidine as the First Selective, Non-Amino Acid, Catalytic Site Inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1).

References

Citations