Synthesis and enzymic activity of 6-carbethoxy- and 6-ethoxy-3,7-disubstituted pyrazolo[1,5-a]pyrimidines and related derivatives as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors
Publication type: Journal Article
Publication date: 1982-03-01
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
6279841
Drug Discovery
Molecular Medicine
Abstract
A number of 3,7-disubstituted 6-carbethoxypyrazolo [1,5-a] pyrimidines and 3,7-disubstituted 6-ethoxypyrazolo-[1,5-a]pyrimidines have been prepared and evaluated as adenosine cyclic 3',5'-phosphate (cAMP) phosphodiesterase (PDE) inhibitors vs. the low Km enzyme isolated from beef heart, rabbit lung, and kidney preparations. The results were found to be between 0.5 to 13 times as potent as theophylline as inhibitors of PDE, depending on the tissue source. A number of these PDE inhibitors exhibited significant physiological effects in different animal systems, suggesting it should be possible to obtain selective PDE inhibition in various tissues. Several of these heterocycles were found superior to adenosine in inhibiting ADP-induced platelet aggregation in vitro.
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25
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25
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GOST
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Springer R. H. et al. Synthesis and enzymic activity of 6-carbethoxy- and 6-ethoxy-3,7-disubstituted pyrazolo[1,5-a]pyrimidines and related derivatives as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors // Journal of Medicinal Chemistry. 1982. Vol. 25. No. 3. pp. 235-242.
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Springer R. H., Scholten M. B., Obrien D. E., Novinson T., Miller J. P., Robins R. K. Synthesis and enzymic activity of 6-carbethoxy- and 6-ethoxy-3,7-disubstituted pyrazolo[1,5-a]pyrimidines and related derivatives as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors // Journal of Medicinal Chemistry. 1982. Vol. 25. No. 3. pp. 235-242.
Cite this
RIS
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TY - JOUR
DO - 10.1021/jm00345a009
UR - https://doi.org/10.1021/jm00345a009
TI - Synthesis and enzymic activity of 6-carbethoxy- and 6-ethoxy-3,7-disubstituted pyrazolo[1,5-a]pyrimidines and related derivatives as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors
T2 - Journal of Medicinal Chemistry
AU - Springer, Robert H.
AU - Scholten, M B
AU - Obrien, Darrell E
AU - Novinson, Thomas
AU - Miller, Jon P.
AU - Robins, Roland K.
PY - 1982
DA - 1982/03/01
PB - American Chemical Society (ACS)
SP - 235-242
IS - 3
VL - 25
PMID - 6279841
SN - 0022-2623
SN - 1520-4804
ER -
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BibTex (up to 50 authors)
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@article{1982_Springer,
author = {Robert H. Springer and M B Scholten and Darrell E Obrien and Thomas Novinson and Jon P. Miller and Roland K. Robins},
title = {Synthesis and enzymic activity of 6-carbethoxy- and 6-ethoxy-3,7-disubstituted pyrazolo[1,5-a]pyrimidines and related derivatives as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors},
journal = {Journal of Medicinal Chemistry},
year = {1982},
volume = {25},
publisher = {American Chemical Society (ACS)},
month = {mar},
url = {https://doi.org/10.1021/jm00345a009},
number = {3},
pages = {235--242},
doi = {10.1021/jm00345a009}
}
Cite this
MLA
Copy
Springer, Robert H., et al. “Synthesis and enzymic activity of 6-carbethoxy- and 6-ethoxy-3,7-disubstituted pyrazolo[1,5-a]pyrimidines and related derivatives as adenosine cyclic 3',5'-phosphate phosphodiesterase inhibitors.” Journal of Medicinal Chemistry, vol. 25, no. 3, Mar. 1982, pp. 235-242. https://doi.org/10.1021/jm00345a009.