首页> 外文OA文献 >Analgesic and anti-inflammatory activities of salicylaldehyde 2-chlorobenzoyl hydrazone (H2LASSBio-466), salicylaldehyde 4-chlorobenzoyl hydrazone (H 2LASSBio-1064) and their zinc(II) complexes
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Analgesic and anti-inflammatory activities of salicylaldehyde 2-chlorobenzoyl hydrazone (H2LASSBio-466), salicylaldehyde 4-chlorobenzoyl hydrazone (H 2LASSBio-1064) and their zinc(II) complexes

机译:水杨醛2-氯苯甲酰(H2LASSBio-466),水杨醛4-氯苯甲酰((H 2LASSBio-1064)及其锌(II)络合物的镇痛和抗炎活性

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摘要

Salicylaldehyde 2-chlorobenzoyl hydrazone (H 2LASSBio-466), salicylaldehyde 4-chlorobenzoyl hydrazone (H 2LASSBio-1064) and their complexes [Zn(LASSBio- 466)H 2O] 2 (1) and [Zn(HLASSBio-1064)Cl] 2 (2) were evaluated in animal models of peripheral and central nociception, and acute inflammation. All studied compounds significantly inhibited acetic acid-induced writhing response. Upon coordination the antinociceptive activity was favored in the complex 1. H 2LASSBio-466 inhibited only the first phase of the formalin test, while 1 was active in the second phase, like indomethacin, indicating its ability to inhibit nociception associated with the inflammatory response. Hence coordination to zinc(II) altered the pharmacological profile of H 2LASSBio-466. H2LASSBio-1064 inhibited both phases but this effect was not improved by coordination. The studied compounds did not increase the latency of response in the hot plate model, indicating their lack of central anti-nociceptive activity. All compounds showed levels of inhibition of zymosan-induced peritonitis comparable or superior to indomethacin, indicating an expressive anti-inflammatory profile.
机译:水杨醛2-氯苯甲酰(H 2LASSBio-466),水杨醛4-氯苯甲酰(H 2LASSBio-1064)及其配合物[Zn(LASSBio- 466)H 2O] 2(1)和[Zn(HLASSBio-1064)Cl] 2(2)在周围和中枢伤害感受和急性炎症的动物模型中进行了评估。所有研究的化合物均显着抑制乙酸诱导的扭体反应。经配位后,复合物1的抗伤害感受活性受到支持。H2LASSBio-466仅抑制福尔马林测试的第一阶段,而第二阶段则像吲哚美辛一样活跃,表明其抑制与炎症反应相关的伤害感受的能力。因此,与锌(II)的配位改变了H 2LASSBio-466的药理特性。 H2LASSBio-1064抑制了两个阶段,但这种作用并未通过协调得到改善。所研究的化合物在热板模型中并未增加应答潜伏期,表明它们缺乏中枢的抗伤害感受活性。所有化合物均表现出与吲哚美辛相当或更高的对酵母聚糖诱导的腹膜炎的抑制水平,表明其具有表达性的消炎作用。

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