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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >N-Pyridinyl-indole-3-(alkyl)carboxamides and derivatives as potential systemic and topical inflammation inhibitors.
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N-Pyridinyl-indole-3-(alkyl)carboxamides and derivatives as potential systemic and topical inflammation inhibitors.

机译：N-吡啶基-吲哚-3-（烷基）羧酰胺及其衍生物作为潜在的全身和局部炎症抑制剂。

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摘要

N-substituted-(indol-3-yl)carboxamides 10-15 and alkanamides 16-18 were prepared starting from the corresponding acids and submitted to screening for evaluation of their anti-inflammatory activity. None of the considered carboxamides exhibited significant inhibitory effect in the carrageenin-induced rat paw oedema after oral administration of 0.1 mMkg(-1); nevertheless introduction of an alkyl chain, leading to alkanamides 16-18, induced moderate to high activity: 46-95% inhibition. The efficacy of these compounds in the inhibition of topical inflammation was confirmed by measuring reduction of ear thickness in the acute tetradecanoyl phorbol acetate (TPA)-induced mouse ear swelling assay. Preliminary pharmacomodulation brought to the fore that toxic effects induced, at 0.4 mMkg(-1), by N-(pyridin-4-yl)(indol-3-yl)propanamide (17) could be attenuated or suppressed by 5-fluorination or introduction of a methoxycarbonylborane moiety, leading to 18 and 21.
机译：从相应的酸开始制备N-取代的（吲哚-3-基）羧酰胺10-15和烷酰胺16-18，并进行筛选以评估其抗炎活性。口服0.1 mMkg（-1）后，没有一种认为的羧酰胺在角叉菜胶诱导的大鼠爪水肿中显示出明显的抑制作用。然而，引入烷基链导致烷酰胺16-18诱导了中等至高活性：抑制46-95％。通过在急性十四烷酰佛波醋酸酯（TPA）诱导的小鼠耳朵肿胀试验中测量耳厚度的减少，证实了这些化合物抑制局部炎症的功效。初步的药物调节作用脱颖而出，N-（吡啶-4-基）（吲哚-3-基）丙酰胺（17）在0.4 mMkg（-1）诱导的毒性作用可以通过5-氟化或引入甲氧基羰基硼烷部分，导致18和21。

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