526218-70-2Relevant academic research and scientific papers
Discovery of Benzamidine- And 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists
Prchalová, Eva,Hin, Niyada,Thomas, Ajit G.,Veeravalli, Vijayabhaskar,Ng, Justin,Alt, Jesse,Rais, Rana,Rojas, Camilo,Li, Zhe,Hihara, Hiroe,Aoki, Mika,Yoshizawa, Kyoko,Nishioka, Tomoki,Suzuki, Shuichi,Kopajtic, Theresa,Chatrath, Sheena,Liu, Qin,Dong, Xinzhong,Slusher, Barbara S.,Tsukamoto, Takashi
, p. 8631 - 8641 (2019/10/16)
Mas-related G-protein-coupled receptor X1 (MRGPRX1) is a human sensory neuron-specific receptor and has been actively investigated as a therapeutic target for the treatment of pain. By use of two HTS screening hit compounds, 4-(4-(benzyloxy)-3-methoxybenzylamino)benzimidamide (5a) and 4-(2-(butylsulfonamido)-4-methylphenoxy)benzimidamide (11a), as molecular templates, a series of human MRGPRX1 agonists were synthesized and evaluated for their agonist activity using HEK293 cells stably transfected with human MrgprX1. Conversion of the benzamidine moiety into a 1-aminoisoquinoline moiety carried out in the later stage of structural optimization led to the discovery of a highly potent MRGPRX1 agonist, N-(2-(1-aminoisoquinolin-6-yloxy)-4-methylphenyl)-2-methoxybenzenesulfonamide (16), not only devoid of positively charged amidinium group but also with superior selectivity over opioid receptors. In mice, compound 16 displayed favorable distribution to the spinal cord, the presumed site of action for the MRGPRX1-mediated analgesic effects.
Amidino derivatives, and anticoagulants and thrombosis therapeutic agents containing them
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, (2008/06/13)
Amidino derivatives represented by the following general formula (I): {where X is a group represented by R1SO2NR2— (wherein R1 represents optionally substituted C6-14 aryl, etc. and R2 repr
