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Literature summary extracted from
- A new therapeutic approach in Parkinsons disease: some novel quinazoline derivatives as dual selective phosphodiesterase 1 inhibitors and anti-inflammatory agents (2009), Bioorg. Med. Chem., 17, 6796-6802.
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 3.1.4.1 | pharmacology | phosphodiesterase plays an important role in regulating cAMP and cGMP, und thus becomes an important site for the pharmacological intervention, i.e. Parkinson's disease, inhibition studies with theinopyrimidine fused quinazolines and pyridopyrimidine fused quinazolinones | Rattus norvegicus |
| 3.1.4.1 | pharmacology | phosphodiesterase plays an important role in regulating cAMP and cGMP, und thus becomes an important site for the pharmacological intervention, i.e. Parkinson's disease, inhibition studies with thienopyrimidine fused quinazolines and pyridopyrimidine fused quinazolinones | Bos taurus |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.1.4.1 | 1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one | - |
Bos taurus |  |
| 3.1.4.1 | 1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10,12-dibromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10,12-dibromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10,12-dibromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10,12-dibromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10,12-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10,12-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10,12-dibromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10,12-dibromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10,12-dibromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10,12-dibromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10,12-dibromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10,12-dibromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10,12-dibromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10,12-dibromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10-bromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10-bromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10-bromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10-bromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10-bromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10-bromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10-bromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10-bromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10-bromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10-bromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10-bromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10-bromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 10-bromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 10-bromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 11,13-dibromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one | - |
Bos taurus | |
| 3.1.4.1 | 11,13-dibromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 11-bromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one | - |
Bos taurus | |
| 3.1.4.1 | 11-bromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 3-(4-methoxy-phenyl)-1-(3-nitro-phenyl)-8Hpyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Rattus norvegicus | |
| 3.1.4.1 | 3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Bos taurus | |
| 3.1.4.1 | 3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 3-isobutyl-1-methylxanthine | i.e. IBMX | Rattus norvegicus | |
| 3.1.4.1 | 9,11-dibromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 9,11-dibromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 9,11-dibromo-1-(2-furyl)-3-(4-tolyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Rattus norvegicus | |
| 3.1.4.1 | 9,11-dibromo-1-(4-chlorophenyl)-3-(4-tolyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Rattus norvegicus | |
| 3.1.4.1 | 9,11-dibromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 9,11-dibromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 9,11-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Rattus norvegicus | |
| 3.1.4.1 | 9,11-dibromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 9,11-dibromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 9,11-dibromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 9,11-dibromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 9-bromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 9-bromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 9-bromo-1-(4-chlorophenyl)-3-(4-tolyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | - |
Rattus norvegicus | |
| 3.1.4.1 | 9-bromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 9-bromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 9-bromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 9-bromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | 9-bromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | - |
Bos taurus | |
| 3.1.4.1 | 9-bromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | IBMX | - |
Bos taurus | |
| 3.1.4.1 | IBMX | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intra peritoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | indomethacin | - |
Bos taurus | |
| 3.1.4.1 | indomethacin | PDE1 inhibitor for anti-inflammatory activity assays, the compound is suspended in 0.5% aqueous carboxy methyl cellulose solution and administered orally as well as intraperitoneal to the rats | Rattus norvegicus | |
| 3.1.4.1 | additional information | synthesis of 1,2,9,11-tetrasubstituted 7H-thieno[2',3':4,5]pyrimido[6,1-b]-quinazolin-7-one and 1,3,10,12-tetrasubstituted 8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one inhibitors, synthesis and evaluation, overview | Rattus norvegicus | |
| 3.1.4.1 | rolipram | a PDE 4 inhibitor | Rattus norvegicus | |
| 3.1.4.1 | trequinsin | a PDE 3 inhibitor | Rattus norvegicus | |
| 3.1.4.1 | vinpocetine | a PDE 1 inhibitor | Rattus norvegicus | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.1.4.1 | Bos taurus | - |
- |
- |
| 3.1.4.1 | Rattus norvegicus | - |
- |
- |
| 3.1.4.1 | Rattus norvegicus | - |
Sprague-Dawley rats | - |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 3.1.4.1 | brain | - |
Bos taurus | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.1.4.1 | cyclic 3',5'-mononucleotides + H2O | PDE1 inhibitory activity assays | Bos taurus | mononucleoside 5'-phosphate | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.1.4.1 | PDE | - |
Rattus norvegicus |
| 3.1.4.1 | PDE1 | - |
Rattus norvegicus |
| 3.1.4.1 | PDE1 | - |
Bos taurus |
| 3.1.4.1 | phosphodiesterase | - |
Rattus norvegicus |
| 3.1.4.1 | phosphodiesterase 1 | - |
Rattus norvegicus |
| 3.1.4.1 | phosphodiesterase 1 | - |
Bos taurus |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 3.1.4.1 | 37 | - |
assay at | Bos taurus |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 3.1.4.1 | additional information | - |
not tested | Bos taurus | indomethacin | |
| 3.1.4.1 | 0.02 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | IBMX | |
| 3.1.4.1 | 0.03 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10,12-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.0399 | - |
- |
Rattus norvegicus | 3-(4-methoxy-phenyl)-1-(3-nitro-phenyl)-8Hpyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.04 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.05 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10,12-dibromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.06 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 9,11-dibromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.06 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 9,11-dibromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.06 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.06 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10,12-dibromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.07 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.07 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.07 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10,12-dibromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.07 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10,12-dibromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.07 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10,12-dibromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.07 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10-bromo-1-(furan-2-ylmethyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.07 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10-bromo-1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.08 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 9,11-dibromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.08 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 9-bromo-1-(4-methoxyphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.08 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.08 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.08 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10,12-dibromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.08 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10-bromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.08 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10-bromo-1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.09 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 9-bromo-1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.09 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 9-bromo-1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.09 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 1-(4-methylphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.1 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 11,13-dibromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one | |
| 3.1.4.1 | 0.1 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 9,11-dibromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.1 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 1-(4-chlorophenyl)-3-(4-methylphenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.1 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10-bromo-3-(4-chlorophenyl)-1-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.1 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10-bromo-3-(4-methoxyphenyl)-1-(3-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.1 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 10-bromo-1,3-bis(4-nitrophenyl)-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
| 3.1.4.1 | 0.12 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 1-(4-chlorophenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.13 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 11-bromo-1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one | |
| 3.1.4.1 | 0.15 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 9-bromo-1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.23 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 1,2,3,4-tetrahydro-9H-[1]benzothieno[2',3':4,5]pyrimido[6,1-b]quinazolin-9-one | |
| 3.1.4.1 | 0.23 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 1-(4-methylphenyl)-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.3 | - |
60 min at 37°C, 10 mM cAMP substrate, pH not specified in the publication | Bos taurus | 1,2-dimethyl-7H-thieno[2',3':4,5]pyrimido[6,1-b]quinazolin-7-one | |
| 3.1.4.1 | 0.337 | - |
- |
Rattus norvegicus | 9,11-dibromo-1-(4-methoxyphenyl)-3-phenyl-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one | |
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Release 2023.1 (January 2023)
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