Synthesis and biological evaluation of new 3-substituted indole derivatives as potential anti-inflammatory and analgesic agents
Synthesis and biological evaluation of new 3-substituted indole derivatives as potential anti-inflammatory and analgesic agents
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DOI：
10.1016/j.bmc.2007.03.024
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发表时间：
2007-06-01
影响因子：
3.5
通讯作者：
El-Shenawy, Siham M.
中科院分区：
文献类型：
--
作者：
Radwan, Mohamed A. A.;Ragab, Eman A.;El-Shenawy, Siham M.
用3-苯基-5-氨基吡唑和2-氨基苯并咪唑的重氮盐处理3-氰基乙酰基吲哚1，得到相应的腙4和5。3-氰基乙酰基吲哚与异硫氰酸苯酯反应，得到相应的硫代乙酰苯胺衍生物7。用腙酰处理7例。氯化物得到相应的1，3，4-噻二唑衍生物8a-f和9。此外，硫代乙酰苯胺与α-卤代酮反应，得到噻吩衍生物10a、B（替尼达普类似物）或噻唑烷-4-酮衍生物11。新合成的化合物具有潜在的抗炎镇痛活性。(c)2007爱思唯尔有限公司保留所有权利。
Treatment of 3-cyanoacetyl indole 1 with the diazonium salts of 3-phenyl-5-aminopyrazole and 2-aminobenzimidazole afforded the corresponding hydrazones 4 and 5. 3-Cyanoacetyl indole reacted with phenylisothiocyanate to give the corresponding thioacetanilide derivative 7. Treatment of 7 with hydrazonoyl. chlorides afforded the corresponding 1,3,4-thiadiazole derivatives 8a-f and 9. Also, the thioacetanilide reacted with alpha-haloketones to afford thiophene derivatives 10a,b (tenidap analogues), or thiazolidin-4-one derivative 11. The newly synthesized compounds were found to possess potential anti-inflammatory and analgesic activities. (c) 2007 Elsevier Ltd. All rights reserved.