Ozagrel sodium

Inhibition of thromboxane synthase (TXAS), especially in human platelets, has been a clinical objective for many years. 1-Alkyl (N-alkyl)-imidazole derivatives have been recognized as TXAS inhibitors since the early 1980s.^1,2,3 Ozagrel is a 1-alkyl imidazole derivative that acts as a selective inhibitor of TXAS with an IC₅₀ of 11 nM. The beneficial effects of TXAS inhibition by ozagrel include improved motor coordination after experimental stroke,⁴ and antihypertensive effects in spontaneously hypertensive rats.⁵

1.Iizuka, K., Akahane, K., Momose, D., et al.Highly selective inhibitors of thromboxane synthase. 1. Imidazole derivativesJ. Med. Chem.241139-1148(1981) 2.Wright, W.B., Tomcufcik, A.S., Chan, P.S., et al.Thromboxane synthase inhibitors and antihypertensive agents. 4,N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-onesJ. Med. Chem.302277-2283(1987) 3.Wright, W.B., Jr., Press, J.B., Chan, P.S., et al.Thromboxane synthetase inhibitors and antihypertensive agents. 1. N-[(1H-imidazol-1-yl)alkyl]aryl amides and N-[(1H-imidazol-1,2,4-triazol-1-yl)alkyl]aryl amidesJ. Med. Chem.29523-530(1986) 4.Ichikawa, K., Tazawa, S., Hamano, S., et al.Effect of ozagrel on locomotor and motor coordination after transient cerebral ischemia in experimental animal modelsPharmacology59257-265(1999) 5.Press, J.B., Wright, W.B., Jr., Chan, P.S., et al.Thromboxane synthetase inhibitors and antihypertensive agents. 2. N-[(1H-Imidazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones and N-[(1H-1,2,4-triazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones as unique antihypertensive agentsJ. Med. Chem.29(5)816-819(1986)