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近期研究结果表明,抗溃疡性结肠炎药物柳氮磺吡啶(SASP)在体外具有抑制前列腺素失活的作用,这一作用可以通过非竞争性地与前列腺素15-羟基脱氢酶(PGDH)相互作用,也可通过离体肺灌注试验证实。据此,作者制备了一系列不具磺胺吡啶(B环)结构的SASP类似物,并且对这些PGDH抑制剂作了结构与活性关系的研究,初步发现在A环水杨酸基处插入亚甲基所得的化合物例如homosalazine(2-羟基-5-苯偶氮基苯乙酸),活性得以很大提高。本文作者通过纯PGDH试验、大鼠结肠细胞质悬液以及离体肺灌注
Recent studies have shown that anti-ulcerative colitis drug sulfasalazine (SASP) has the effect of inhibiting prostaglandin inactivation in vitro and that this effect can be mediated by non-competitive association with prostaglandin 15-hydroxydehydrogenase (PGDH) Interactions can also be confirmed by isolated lung perfusion tests. Accordingly, the authors prepared a series of SASP analogues without sulfapyridine (B ring) structure and studied the relationship between structure and activity of these PGDH inhibitors. It was found that insertion of methylene The resulting compound, such as homosalazine (2-hydroxy-5-phenylazo phenylacetic acid), shows a dramatic increase in activity. The authors pass pure PGDH test, rat cytoplasmic suspension and isolated lung perfusion