The Experts below are selected from a list of 360 Experts worldwide ranked by ideXlab platform
Richard Labaudiniere - One of the best experts on this subject based on the ideXlab platform.
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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
Journal of Medicinal Chemistry, 2003Co-Authors: Alain Claudemarie Daugan, Pascal Grondin, Cecile Ruault, Annecharlotte Le Monnier De Gouville, Herve Coste, Jorge Kirilovsky, Francois Hyafil, Richard LabaudiniereAbstract: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.
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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
Journal of Medicinal Chemistry, 2003Co-Authors: Alain Claudemarie Daugan, Pascal Grondin, Cecile Ruault, Annecharlotte Le Monnier De Gouville, Herve Coste, Jorge Kirilovsky, Francois Hyafil, Richard LabaudiniereAbstract: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.
Alain Claudemarie Daugan - One of the best experts on this subject based on the ideXlab platform.
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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
Journal of Medicinal Chemistry, 2003Co-Authors: Alain Claudemarie Daugan, Pascal Grondin, Cecile Ruault, Annecharlotte Le Monnier De Gouville, Herve Coste, Jorge Kirilovsky, Francois Hyafil, Richard LabaudiniereAbstract: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.
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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
Journal of Medicinal Chemistry, 2003Co-Authors: Alain Claudemarie Daugan, Pascal Grondin, Cecile Ruault, Annecharlotte Le Monnier De Gouville, Herve Coste, Jorge Kirilovsky, Francois Hyafil, Richard LabaudiniereAbstract: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.
Andrei A Gakh - One of the best experts on this subject based on the ideXlab platform.
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antiproliferative 4 1 2 4 oxadiazol 5 yl piperidine 1 carboxamides a new tubulin inhibitor chemotype
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: Mikhail Krasavin, Andrey V Sosnov, Ruben Karapetian, Igor Konstantinov, Olga Soldatkina, Elena Godovykh, Fedor I Zubkov, Ernest Hamel, Andrei A GakhAbstract:We discovered a new Chemical Class of antiproliferative agents, 4-(1,2,4-oxadiazol-5-yl)piperidine-1-carboxamides. SAR-guided optimization of the two distinct terminal fragments yielded a compound with 120 nM potency in an antiproliferative assay. Biological activity profile studies (COMPARE analysis) demonstrated that 4-(1,2,4-oxadiazol-5-yl)piperidine-1-carboxamides act as tubulin inhibitors, and this conclusion was confirmed via bioChemical assays with pure tubulin and demonstration of increased numbers of mitotic cells following treatment of a leukemia cell line.
Jorge Kirilovsky - One of the best experts on this subject based on the ideXlab platform.
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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
Journal of Medicinal Chemistry, 2003Co-Authors: Alain Claudemarie Daugan, Pascal Grondin, Cecile Ruault, Annecharlotte Le Monnier De Gouville, Herve Coste, Jorge Kirilovsky, Francois Hyafil, Richard LabaudiniereAbstract: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.
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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
Journal of Medicinal Chemistry, 2003Co-Authors: Alain Claudemarie Daugan, Pascal Grondin, Cecile Ruault, Annecharlotte Le Monnier De Gouville, Herve Coste, Jorge Kirilovsky, Francois Hyafil, Richard LabaudiniereAbstract: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.
Francois Hyafil - One of the best experts on this subject based on the ideXlab platform.
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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
Journal of Medicinal Chemistry, 2003Co-Authors: Alain Claudemarie Daugan, Pascal Grondin, Cecile Ruault, Annecharlotte Le Monnier De Gouville, Herve Coste, Jorge Kirilovsky, Francois Hyafil, Richard LabaudiniereAbstract: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.
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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
Journal of Medicinal Chemistry, 2003Co-Authors: Alain Claudemarie Daugan, Pascal Grondin, Cecile Ruault, Annecharlotte Le Monnier De Gouville, Herve Coste, Jorge Kirilovsky, Francois Hyafil, Richard LabaudiniereAbstract: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.