354764-98-0Relevant academic research and scientific papers
Exploration of TRPM8 Binding Sites by β-Carboline-Based Antagonists and Their in Vitro Characterization and in Vivo Analgesic Activities
Bertamino, Alessia,Ostacolo, Carmine,Medina, Alicia,Di Sarno, Veronica,Lauro, Gianluigi,Ciaglia, Tania,Vestuto, Vincenzo,Pepe, Giacomo,Basilicata, Manuela Giovanna,Musella, Simona,Smaldone, Gerardina,Cristiano, Claudia,Gonzalez-Rodriguez, Sara,Fernandez-Carvajal, Asia,Bifulco, Giuseppe,Campiglia, Pietro,Gomez-Monterrey, Isabel,Russo, Roberto
, p. 9672 - 9694 (2020/10/19)
Transient receptor potential melastatin 8 (TRPM8) ion channel represents a valuable pharmacological option for several therapeutic areas. Here, a series of conformationally restricted derivatives of the previously described TRPM8 antagonist N,N′-dibenzyl
A class of 3 S -2-aminoacyltetrahydro-β-carboline-3-carboxylic acids: Their facile synthesis, inhibition for platelet activation, and high in vivo anti-thrombotic potency
Liu, Jiawang,Jiang, Xueyun,Zhao, Ming,Zhang, Xiaoyi,Zheng, Meiqing,Peng, Li,Peng, Shiqi
experimental part, p. 3106 - 3116 (2010/09/05)
3S-Tetrahydro-β-carboline-3-carboxylic acid (TCCA) effectively inhibits ADP-induced platelet activation. This paper used TCCA as a lead, modified its 2-position with amino acids, and provided 20 novel 3S-2-aminoacyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acids (5a-t). With the in vitro assay, it was demonstrated that this modification diminished the IC50 values from 701 nM of TCCA to 10 nM of 5a-t. With the in vivo assay, it was demonstrated that this modification reduced the efficacious dose from 5.0 μmol/kg of TCCA to 0.1 μmol/kg of 5a-t. Comparing the Cerius2 based conformation of them with that of their analogues, the 3-position modified TCCA, it was suggested that the comparatively unfolded conformation was one of the important factors of enhancing the in vivo antithrombotic potency.
Toward breast cancer resistance protein (BCRP) inhibitors: design, synthesis of a series of new simplified fumitremorgin C analogues
Wu, Guofeng,Liu, Jiawang,Bi, Lanrong,Zhao, Ming,Wang, Chao,Baudy-Floc'h, Miche?le,Ju, Jingfang,Peng, Shiqi
, p. 5510 - 5528 (2008/02/07)
In this study, we report the design and synthesis of a series of new simplified fumitremorgin C analogues. The preliminary biological study indicated some of these simplified fumitremorgin C might be developed into breast cancer resistance inhibitors.
Microwave assisted stereospecific synthesis of (S)-3-substituted 2,3,6,7,12,12a-hexahydropyrazino[1′,2′:1,6]pyrido [3,4-b]indole-1,4-diones
Pandey, Suresh K.,Awasthi, Keshav K.,Saxena, Anil K.
, p. 4437 - 4442 (2007/10/03)
A new easy way of preparing (S)-3-substituted 2,3,6,7,12,12a-hexahydropyrazino[1′,2′:1,6]pyrido[3,4-b] indole-1,4-diones, an important intermediate compound, is described using microwave irradiation supported on silica gel. The reaction is generalised and good to excellent yields of enantiomerically pure products are obtained.
