2199-92-0Relevant articles and documents
Synthesis of novel triheterocyclic thiazoles as anti-inflammatory and analgesic agents
Kalkhambkar,Kulkarni,Shivkumar,Rao, R. Nagendra
, p. 1272 - 1276 (2007)
Triheterocyclic thiazoles containing coumarin and carbostyril (1-aza coumarin) have been synthesized by the reaction of the in situ generated 4-thioureidomethyl carbostyril and 3-bromoacetyl coumarins. The new compounds have been tested for their in vivo analgesic and anti-inflammatory activities. Qualitative SAR studies indicate that, the chloro substitution at C-7 in carbostyril and 6,8-dibromo substitution in the coumarin ring enhance anti-inflammatory activity. These compounds were also found to provide significant protection against acetic acid writhing in animal models. All the compounds have been characterized by IR, 1H NMR, 13C NMR and mass spectrometry.
Synthesis and anti-acetylcholinesterase activities of novel glycosyl coumarylthiazole derivatives
Cao, Lian-Gong,Cao, Zhi-Ling,Jiang, Kai-Jun,Liu, Shu-Hao,Liu, Wei-Wei,Lu, Xing,Shao, Zhong-Bai,Shi, Da-Hua,Wang, Lei,Wang, You-Xian
, p. 359 - 364 (2020/12/28)
Eleven glycosyl coumarylthiazole derivatives are synthesized by cyclization and condensation of glycosyl thiourea with 3-bromoacetyl coumarins in ethanol. The reaction conditions are optimized and good yields of products (80%–95%) are obtained. The structures of all new products were confirmed by IR, 1H and 13C NMR, and by HRMS (electrospray ionization). The in vitro acetylcholinesterase (AChE) inhibitory activities of these new compounds are tested by Ellman’s method. Among them, N-(2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-β-D-glucopyranosyl)-4-(6-nitrocoumarinyl)-1,3-thiazole-2-amine showed the best activity with an in vitro AChE inhibitory rate of 58% and an IC50 value of 12 ± 0.38 μg/mL.
The effects of bromine atoms on the photophysical and photochemical properties of 3-cinnamoylcoumarin derivatives
Sun, Zhiyuan,Wang, Yu,Fang, De-Cai,Zhao, Yuxia
supporting information, p. 7377 - 7382 (2018/05/07)
Eight coumarin derivatives (T1-T8) with or without modification using one or two bromine atoms were synthesized through the aldol condensation reaction. Their photophysical, photochemical and electrochemical properties were investigated. It was shown that