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Your search keyword '"M Idrissi"' showing total 5 results
Start Over Author "M Idrissi" Publisher elsevier science ltd
5 results on '"M Idrissi"'

1. Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 2: metabolism-directed optimization studies towards orally bioavailable derivatives.

Author

Vergne F, Bernardelli P, Lorthiois E, Pham N, Proust E, Oliveira C, Mafroud AK, Ducrot P, Wrigglesworth R, Berlioz-Seux F, Coleon F, Chevalier E, Moreau F, Idrissi M, Tertre A, Descours A, Berna P, and Li M

Subjects
3',5'-Cyclic-AMP Phosphodiesterases metabolism, Administration, Oral, Animals, Biological Availability, Cyclic Nucleotide Phosphodiesterases, Type 7, Isoenzymes metabolism, Phosphodiesterase Inhibitors chemical synthesis, Phosphodiesterase Inhibitors chemistry, Rats, Stereoisomerism, Structure-Activity Relationship, Thiadiazoles chemical synthesis, Thiadiazoles chemistry, 3',5'-Cyclic-AMP Phosphodiesterases antagonists & inhibitors, Isoenzymes antagonists & inhibitors, Phosphodiesterase Inhibitors pharmacokinetics, Thiadiazoles pharmacokinetics
Abstract

The synthesis and optimization of pharmacokinetic parameters of structurally novel small PDE7 inhibitors is discussed.

Published
2004
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2. Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.

Author

Lorthiois E, Bernardelli P, Vergne F, Oliveira C, Mafroud AK, Proust E, Heuze L, Moreau F, Idrissi M, Tertre A, Bertin B, Coupe M, Wrigglesworth R, Descours A, Soulard P, and Berna P

Subjects
3',5'-Cyclic-AMP Phosphodiesterases metabolism, Cell Line, Cyclic Nucleotide Phosphodiesterases, Type 7, Drug Evaluation, Preclinical, Humans, Isoenzymes metabolism, Phosphodiesterase Inhibitors chemistry, Phosphodiesterase Inhibitors pharmacology, Quinazolines chemistry, Quinazolines pharmacology, Solubility, Spiro Compounds chemistry, Spiro Compounds pharmacology, Structure-Activity Relationship, 3',5'-Cyclic-AMP Phosphodiesterases antagonists & inhibitors, Isoenzymes antagonists & inhibitors, Phosphodiesterase Inhibitors chemical synthesis, Quinazolines chemical synthesis, Spiro Compounds chemical synthesis
Abstract

The synthesis and SAR studies of spiroquinazolinones as novel PDE7 inhibitors are discussed. The best compounds from the series displayed nanomolar inhibitory affinity and were selective versus other PDE isoenzymes.

Published
2004
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3. Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.

Author

Vergne F, Bernardelli P, Lorthiois E, Pham N, Proust E, Oliveira C, Mafroud AK, Royer F, Wrigglesworth R, Schellhaas J, Barvian M, Moreau F, Idrissi M, Tertre A, Bertin B, Coupe M, Berna P, and Soulard P

Subjects
3',5'-Cyclic-AMP Phosphodiesterases metabolism, Cell Line, Cyclic Nucleotide Phosphodiesterases, Type 4, Cyclic Nucleotide Phosphodiesterases, Type 7, Humans, Isoenzymes metabolism, Phosphodiesterase Inhibitors chemistry, Structure-Activity Relationship, Thiadiazoles chemistry, 3',5'-Cyclic-AMP Phosphodiesterases antagonists & inhibitors, Isoenzymes antagonists & inhibitors, Phosphodiesterase Inhibitors chemical synthesis, Phosphodiesterase Inhibitors pharmacology, Thiadiazoles chemical synthesis, Thiadiazoles pharmacology
Abstract

The synthesis and SAR studies of a series of structurally novel small molecule inhibitors of PDE7 are discussed. The best compounds from the series displayed low nanomolar inhibitory activity and are selective versus PDE4.

Published
2004
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4. Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives.

Author

Bernardelli P, Lorthiois E, Vergne F, Oliveira C, Mafroud AK, Proust E, Pham N, Ducrot P, Moreau F, Idrissi M, Tertre A, Bertin B, Coupe M, Chevalier E, Descours A, Berlioz-Seux F, Berna P, and Li M

Subjects
3',5'-Cyclic-AMP Phosphodiesterases classification, 3',5'-Cyclic-AMP Phosphodiesterases metabolism, Animals, Biological Availability, Cell Line, Cyclic Nucleotide Phosphodiesterases, Type 7, Half-Life, Humans, In Vitro Techniques, Isoenzymes classification, Isoenzymes metabolism, Microsomes drug effects, Microsomes metabolism, Quinazolines chemistry, Quinazolines pharmacology, Rats, Spiro Compounds chemistry, Spiro Compounds pharmacology, Structure-Activity Relationship, 3',5'-Cyclic-AMP Phosphodiesterases antagonists & inhibitors, Isoenzymes antagonists & inhibitors, Phosphodiesterase Inhibitors chemistry, Phosphodiesterase Inhibitors pharmacokinetics, Quinazolines chemical synthesis, Spiro Compounds chemical synthesis
Abstract

The optimization of 5,8-disubstituted spirocyclohexane-quinazolinones into potent, selective, soluble PDE7 inhibitors with acceptable in vivo pharmacokinetic parameters is presented.

Published
2004
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5. New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors.

Author

Devillers I, Pevet I, Jacobelli H, Durand C, Fasquelle V, Puaud J, Gaudillière B, Idrissi M, Moreau F, and Wrigglesworth R

Subjects
3',5'-Cyclic-AMP Phosphodiesterases metabolism, Azulenes, Cyclic Nucleotide Phosphodiesterases, Type 4, Cycloheptanes pharmacology, Phosphodiesterase Inhibitors pharmacology, 3',5'-Cyclic-AMP Phosphodiesterases antagonists & inhibitors, Cycloheptanes chemistry, Phosphodiesterase Inhibitors chemistry
Published
2004
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