Synthesis of both enantiomers of 1,2,3,4-tetrahydroisoquinoline derivative IPPAM-1 and enantio-dependency of its positive allosteric modulation of prostacyclin receptor

[Display omitted] We present a practical synthesis of both enantiomers of 1,2,3,4-tetrahydroisoquinoline derivative IPPAM-1 (1), which is a positive allosteric modulator (PAM) of prostacyclin receptor (IP) and a candidate for treatment of pulmonary arterial hypertension without the side effects caus...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2017-06, Vol.27 (11), p.2567-2570
Hauptverfasser:	Yamamoto, Kohki, Suzuki, Toshifumi, Imamura, Riyo, Nagano, Tetsuo, Okabe, Takayoshi, Miyachi, Hiroyuki
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric Regulation Animals Antihypertensive Agents - chemical synthesis Antihypertensive Agents - chemistry Antihypertensive Agents - therapeutic use CHO Cells Cricetinae Cricetulus Cyclic AMP - metabolism Humans Hypertension, Pulmonary - drug therapy Positive allosteric modulator Prostacyclin Prostacyclin receptor Pulmonary arterial hypertension Receptors, Epoprostenol - agonists Receptors, Epoprostenol - genetics Receptors, Epoprostenol - metabolism Stereoisomerism Tetrahydroisoquinolines - chemical synthesis Tetrahydroisoquinolines - chemistry Tetrahydroisoquinolines - therapeutic use Tetrazole derivative
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