Design, synthesis, antinociceptive and anti-inflammatory activities of novel piroxicam analogues.
Design, synthesis, antinociceptive and anti-inflammatory activities of novel piroxicam analogues.
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新型吡昔康类似物的设计，合成，抗伤害感受和抗炎活性。
DOI：
10.3390/molecules171214126
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发表时间：
2012-11-28
期刊：
影响因子：
--
通讯作者：
Barreiro EJ
中科院分区：
文献类型：
--
作者：
de Miranda AS;Bispo Júnior W;da Silva YK;Alexandre-Moreira MS;Castro Rde P;Sabino JR;Lião LM;Lima LM;Barreiro EJ
本文报道了通过对非甾体抗炎药吡罗昔康(1)进行结构修饰而设计合成的一系列苯并噻嗪N-酰肼14a-h的设计、合成、抗伤害性和抗炎活性。在合成的类似物中，化合物14F(LASSBio-1637)和14G(LASSBio-1639)被鉴定为新的抗伤害和抗炎原型，通过口服具有活性，其作用机制似乎与吡罗昔康不同，因为它们在10μM时不具有环氧合酶(COX-1和COX-2)的抑制活性。
In this paper we report the design, synthesis, antinociceptive and anti-inflammatory activities of a series of benzothiazine N-acylhydrazones 14a–h, planned by structural modification of piroxicam (1), a non steroidal anti-inflammatory drug. Among the synthesized analogues, compounds 14f (LASSBio-1637) and 14g (LASSBio-1639) were identified as novel antinociceptive and anti-inflammatory prototypes, active by oral administration, acting by a mechanism of action that seems to be different from that of piroxicam, since they were inactive as an inhibitor of cyclooxygenase (COX-1 and COX-2) at concentrations of 10 μM.
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