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首页> 外文期刊>Archiv der Pharmazie >Further evaluation of a series of anti-inflammatory N-pyrrolylcarboxylic acids: effects on the nociception in rats.
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Further evaluation of a series of anti-inflammatory N-pyrrolylcarboxylic acids: effects on the nociception in rats.

机译:一系列抗炎N-吡咯烷基羧酸的进一步评估:对大鼠伤害感受的影响。

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摘要

The analgesic activity of nine substituted N-pyrrolylcarboxylic acids, previously reported as anti-inflammatory agents, has been evaluated. The effects on nociception were examined in male Wistar rats by the Randall-Selitto paw-pressure test. The compounds were administrated in doses 10, 20, and 40 mg/kg both i.p. and p.o. As a whole, the activities of 3-(N-pyrrolyl)propanoic acids 3e-3h and 2-[3-(ethoxycarbonyl)-2-methyl-5-phenyl-1H-1-pyrrolyl]-3-methylpentanoic acid 3i were comparable with or superior to that of metamizole used as a reference (200 mg/kg, i.p.), whereas only 3a from among the N-pyrrolyl-acetic acids 3a-3d showed analgesic activity on the inflamed paw. The compounds found most promising to increase the pain threshold significantly were the same ones with the higher anti-inflammatory activity registered in our previous study: 3-[3-(ethoxycarbonyl)-2-methyl-5-(3-nitrophenyl)-1H-1-pyrrolyl]propanoic acid 3e, together with its 5-(4-nitrophenyl)- 3f, 5-phenyl- 3g, and 5-(4-methylphenyl)- 3hanalogs. Certain parallels between the analgesic activities and some physicochemical properties were observed.
机译:已经评估了九种取代的N-吡咯烷基羧酸的镇痛活性,以前报道它们是抗炎药。通过Randall-Selitto爪压试验检查了雄性Wistar大鼠对伤害感受的影响。分别以10、20和40mg / kg的剂量腹膜内给药。和p.o.总体上,3-(N-吡咯基)丙酸3e-3h和2- [3-(乙氧基羰基)-2-甲基-5-苯基-1H-1-吡咯基] -3-甲基戊酸3i的活性为与作为参考的间苯二甲醚相当或优于后者(200 mg / kg,腹腔注射),而N-吡咯基乙酸3a-3d中只有3a对发炎的爪有镇痛作用。发现最有希望显着提高疼痛阈值的化合物与我们先前研究中记录的具有更高抗炎活性的化合物相同:3- [3-(乙氧羰基)-2-甲基-5-(3-硝基苯基)-1H -1-吡咯基]丙酸3e及其5-(4-硝基苯基)-3f,5-苯基-3g和5-(4-甲基苯基)-3hanalog。观察到止痛活性和某些理化性质之间存在某些相似之处。

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