Desideri N, Stein M L, Conti S, Sestili I, Bucchi F, Cerletti C
Arzneimittelforschung. 1986 Nov;36(11):1561-3.
3-Pyridyloxyacetaldehyde guanylhydrazone and the guanylhydrazones of pyridine-2- and -4-aldehydes substituted at the 3-position with the omega-carboxypentyloxy chain were synthesized in order to evaluate their activity as thromboxane synthase inhibitors in vitro. The tested compounds inhibit thromboxane B2 biosynthesis in human serum. The first appears to be a selective inhibitor of thromboxane synthase, since there was a concomitant rise in Prostaglandin E2 (PGE2) level. The derivative of 4-pyridinealdehyde was the more active one of the other two compounds but it also markedly lowered PGE2 biosynthesis proving to be an inhibitor of cyclooxygenase.
合成了3-吡啶氧基乙醛胍腙以及在3位被ω-羧基戊氧基链取代的吡啶-2-醛和 -4-醛的胍腙,以评估它们在体外作为血栓素合酶抑制剂的活性。所测试的化合物抑制人血清中血栓素B2的生物合成。第一种化合物似乎是血栓素合酶的选择性抑制剂,因为同时前列腺素E2(PGE2)水平有所升高。4-吡啶醛的衍生物是另外两种化合物中活性更强的一种,但它也显著降低了PGE2的生物合成,证明是一种环氧化酶抑制剂。