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BioAssay: AID 219819

Inhibition of rabbit lung cAMP Phosphodiesterase

A series of various pyrazolo[1,5-a]-1,3,5-triazines have been prepared and studied as inhibitors of cAMP phosphodiesterase isolated from bovine brain, bovine heart, and rabbit lung. A number of compounds were found to be superior to theophylline. 2-Ethyl-7-phenylpyrazolo[1,5-a]-1,3,5-triazine (35) was found to be 97 times more potent than theophylline as an inhibitor of bovine brain PDE. more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 219819
Data Source: ChEMBL (217158)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-21
Modify Date: 2014-05-19

Data Table ( Complete ):           Active    All
BioActive Compound: 1
Description:
Title: Synthesis and enzymic activity of various substituted pyrazolo[1,5-a]-1,3,5-triazines as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors.

Abstract: A series of various pyrazolo[1,5-a]-1,3,5-triazines have been prepared and studied as inhibitors of cAMP phosphodiesterase isolated from bovine brain, bovine heart, and rabbit lung. A number of compounds were found to be superior to theophylline. 2-Ethyl-7-phenylpyrazolo[1,5-a]-1,3,5-triazine (35) was found to be 97 times more potent than theophylline as an inhibitor of bovine brain PDE. 8-Bromo-2,4-dimethyl-7-phenylpyrazolo[1,5-a]-1,3,5-triazine (52) showed alpha lung = 40 compared to alpha heart = 3.0. Thus, various substituents could increase or decrease the inhibition relative to the type and source of tissue from which the PDE was isolated. The most active compound was 8-bromo-4-(diethylamino)-7-phenylpyrazolo[1,3-a]-1,3,5-triazine (25), which was 185 times more potent than theophylline as an inhibitor of PDE isolated from rabbit lung. The stepwise synthesis via ring-closure procedures of requisite pyrazole intermediates, followed by electrophilic substitution in the pyrazole ring and/or nucleophilic substitution in the 1,3,5-triazine moiety, resulted in the various pyrazolo[1,5-a]1,3,5-triazines listed in Tables I and II. Structure-activity relationships are reviewed.
(PMID: 6279842)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Putative Target:

ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Km*Km PubChem standard valueFloatμM
2Km activity commentKm activity commentString
3Km standard flagKm standard flagInteger
4Km qualifierKm qualifierString
5Km published valueKm published valueFloatμM
6Km standard valueKm standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
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