- N - 4 - trifluoromethyl phenyl salicylic amide derivatives of preparation method and application
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The invention discloses a preparation method and use of N-4-trifluoromethylphenylsalicylamide derivatives shown in a general formula (I). The preparation method of the N-4-trifluoromethylphenylsalicylamide derivatives or pharmaceutically acceptable salt t
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Paragraph 0063-0071
(2019/06/11)
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- Identification and synthesis of low-molecular weight cholecystokinin B receptor (CCKBR) agonists as mediators of long-term synaptic potentiation
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Recently, He et al. reported that CCKB receptors located in the neocortex of the brain when bound to their bound natural ligand, CCK peptides, enhance memory, bringing up the possibility that agonists targeting the CCKB receptor may act as therapeutic agents in diseases in which memory loss is marked as observed in dementia and Alzheimer’s. In this report, we describe the synthesis of novel low-molecular weight benzoamine CCKB receptor agonists. The compounds made in this series were determined to be mostly partial agonists, although some antagonists were identified, as well, capable of triggering calcium release in a cell line that overexpresses the CCKB receptor. Compound 35 demonstrated an EC50 of 0.15 μM in the cell-based assay, but more importantly, several of the compounds, including 35, demonstrated a physiological effect, inducing long-term potentiation in rat brains comparable to the CCK-8 peptide albeit at much higher concentrations. Based on these findings, benzoamines may be the basis for a new series of CCKB receptor agonists in drug-discovery efforts that seek to develop therapeutics to prevent memory loss.
- Zhang, Yanmei,Wang, Yican,Guo, Yiping,Liao, Jinxi,Tu, Zhengchao,Lu, Yongzhi,Ding, Ke,Tortorella, Micky D.,He, Jufang
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p. 387 - 393
(2019/02/01)
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- Novel derivatives of nitro-substituted salicylic acids: Synthesis, antimicrobial activity and cytotoxicity
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Inspired by the high antituberculous activity of novel nitro-substituted derivatives and based on promising predicted ADMET properties we have synthesized a series of 33 salicylanilides containing nitro-group in their salicylic part and evaluated them for
- Paraskevopoulos, Georgios,Krátky, Martin,Mandíková, Jana,Trejtnar, Franti?ek,Stola?íková, Ji?ina,Pávek, Petr,Besra, Gurdyal,Vin?ová, Jarmila
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p. 7292 - 7301
(2015/11/16)
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- Design and Synthesis of Novel Cyclooxygenase-1 Inhibitors as Analgesics: 5-Amino-2-ethoxy-N-(substituted-phenyl)benzamides
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We previously found that N-(4-aminophenyl)-4-trifluoromethylbenzamide (TFAP), a COX-1 inhibitor, exhibits an analgesic effect without causing gastric damage. Unfortunately, TFAP causes reddish purple coloration of urine, and its analgesic effect is less potent than that of indomethacin. Herein we describe our study focusing on the development of 4- and 5-amino-2-alkoxy-N-phenylbenzamide scaffolds, designed on the basis of the structures of TFAP and parsalmide, another known COX-1 inhibitory analgesic agent. 5-Amino-2-ethoxy-N-(2- or 3-substituted phenyl)benzamide derivatives exhibited analgesic activity in a murine acetic acid induced writhing test. Among these compounds, 5-amino-2-ethoxy-N-(2-methoxyphenyl)benzamide (9v) possesses potent COX-1 inhibitory and analgesic activities, similar to those of indomethacin. In addition, 5-amino-2-ethoxy-N-(3-trifluoromethylphenyl)benzamide (9g) showed a more potent analgesic effect than indomethacin or 9v without causing apparent gastric damage or coloration of urine, although its COX-1 inhibitory activity was weaker than that of indomethacin or 9v. Thus, 9g and 9v appear to be promising candidates for analgesic agents and are attractive lead compounds for further development of COX-1 inhibitors.
- Fukai, Ryosuke,Zheng, Xiaoxia,Motoshima, Kazunori,Tai, Akihiro,Yazama, Futoshi,Kakuta, Hiroki
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experimental part
p. 550 - 560
(2011/12/22)
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