119377-08-1Relevant articles and documents
The discovery of tadalafil: A novel and highly selective PDE5 inhibitor. 1: 5,6,11,11a-Tetrahydro-1H-imidazo[1′,5′ :1,6]pyrido[3,4-b]indole-1,3(2H)-dione analogues
Daugan, Alain,Grondin, Pascal,Ruault, Cécile,Le Monnier De Gouville, Anne-Charlotte,Coste, Hervé,Kirilovsky, Jorge,Hyafil, Fran?ois,Labaudinière, Richard
, p. 4525 - 4532 (2007/10/03)
Starting from ethyl β-carboline-3-carboxylate (β-CCE), 1, a modest inhibitor of type 5 phosphodiesterase (PDE5), a series of functionalized tetrahydro-β-carboline derivatives has been identified as a novel chemical class of potent and selective PDE5 inhibitors. Optimization of the side chain on the hydantoin ring of initial lead compound 2 and of the aromatic ring on position 5 led to the identification of compound 6e, a highly potent and selective PDE5 inhibitor, with greater selectivity for PDE5 vs PDE1-4 than sildenafil. Compound 6e demonstrated a long-lasting and significant blood pressure lowering effect after iv administration in the spontaneously hypertensive rat model but showed only moderate oral in vivo efficacy.
Synthese der Ester der 1-Pyridyl-β-carbolin-3-carbonsaeure
Cegla, M.,Duszynska, Beata,Misztal, S.
, p. 510 (2007/10/02)
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