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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis of substituted benzamides as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 but do not cause gastric damage.
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Synthesis of substituted benzamides as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 but do not cause gastric damage.

机译：合成取代的苯甲酰胺作为抗炎剂，可优先抑制环氧合酶1，但不会引起胃部损害。

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摘要

Parsalmide (5-amino-N-butyl-2-(2-propynyloxy) benzamide) (5a), is a non-steroidal anti-inflammatory drug (NSAID), commercialised in Italy until 1985 with the brand name of Synovial(R), that has been widely used to treat arthritic patient. In addition, it was shown to spare gastric mucosa. Here we have synthesised a series of novel substituted benzamides, related to Parsalmide, and have evaluated their activity in vitro on COX-1 and COX-2 as well as in vivo in the carrageenin-induced rat paw edema, a classical in vivo anti-inflammatory assay. Compounds 5b, 11a and 11b, which showed a favourable profile in vitro and in vivo, were screened in comparison with Parsalmide for gastrointestinal (GI) tolerability in vivo in the rat. Results obtained showed that Parsalmide and compound 11b inhibited both COX-1 and COX-2 in vitro as well as they were active in vivo. Both compounds were devoid of gastric effect at the efficacious dose. In addition, both prevented indomethacin-induced gastric damage. Thus, these compounds may guide the definition of a new leading structure with anti-inflammatory activity that may allow designing new safer NSAIDs.
机译：Parsalmide（5-氨基-N-丁基-2-（2-丙炔氧基）苯甲酰胺）（5a）是一种非甾体类抗炎药（NSAID），在意大利一直销售到1985年，商标名为Synovial（R） ，已被广泛用于治疗关节炎患者。另外，它被证明可以保留胃粘膜。在这里，我们合成了一系列与帕萨尔胺有关的新型取代苯甲酰胺，并评估了它们在体外对角叉菜胶诱导的大鼠爪水肿对COX-1和COX-2以及在体内的活性，这是经典的体内抗-炎性测定。与帕萨尔米德相比，对化合物5b，11a和11b在体外和体内均表现出良好的耐受性，从而对大鼠体内的胃肠道（GI）耐受性进行了筛选。所获得的结果表明，帕沙尔胺和化合物11b在体外均抑制COX-1和COX-2，并且它们在体内具有活性。两种化合物在有效剂量下均没有胃作用。另外，两者均防止了消炎痛诱导的胃损伤。因此，这些化合物可以指导具有抗炎活性的新的前导结构的定义，这可以允许设计新的更安全的NSAID。

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