Acylhydrazones as M1/M3 selective muscarinic agonists
Тип публикации: Journal Article
Дата публикации: 1996-11-01
SCImago Q2
WOS Q2
БС2
SJR: 0.426
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
To improve receptor binding affinity and to investigate functional selectivity of 2,8-dimethyl-1-oxa-8-azaspiro[4.5]decan-3-one acetylhydrazone 2 at muscarinic receptor subtypes, a series of acylhydrazones A was synthesized. The SAR indicates that the binding affinity in the pirenzepine assay (M1) correlates well with lipophilicity. Intrinsic activity (30% of carbachol response) of agonists at M1 remains unchanged. Compounds with n = 0 and 6, where X = NHCO(CH 2 ) n Me, did not inhibit cAMP formation in rat heart membrane (M2). Most of the compounds are more efficacious at the M3 receptor than at M1. The results suggest that the M1 and M3 receptors can better tolerate bulky and long chained substituents than the M2 receptor.
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7
Всего цитирований:
7
Цитирований c 2025:
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ГОСТ
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Wu E. S. C. et al. Acylhydrazones as M1/M3 selective muscarinic agonists // Bioorganic and Medicinal Chemistry Letters. 1996. Vol. 6. No. 21. pp. 2525-2530.
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Kover A., Loch J. T., Rosenberg L. P., Semus S. F., Verhoest P. R., Gordon J., Machulskis A. C., Mccreedy S. A., Zongrone J., Blosser J. C. Acylhydrazones as M1/M3 selective muscarinic agonists // Bioorganic and Medicinal Chemistry Letters. 1996. Vol. 6. No. 21. pp. 2525-2530.
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TY - JOUR
DO - 10.1016/0960-894x(96)00471-4
UR - https://doi.org/10.1016/0960-894x(96)00471-4
TI - Acylhydrazones as M1/M3 selective muscarinic agonists
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Kover, Alexander
AU - Loch, James T
AU - Rosenberg, L Paul
AU - Semus, Simon F.
AU - Verhoest, Patrick R.
AU - Gordon, John
AU - Machulskis, Anthony C
AU - Mccreedy, Sally A
AU - Zongrone, John
AU - Blosser, James C.
PY - 1996
DA - 1996/11/01
PB - Elsevier
SP - 2525-2530
IS - 21
VL - 6
SN - 0960-894X
SN - 1464-3405
ER -
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BibTex (до 50 авторов)
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@article{1996_Wu,
author = {Alexander Kover and James T Loch and L Paul Rosenberg and Simon F. Semus and Patrick R. Verhoest and John Gordon and Anthony C Machulskis and Sally A Mccreedy and John Zongrone and James C. Blosser},
title = {Acylhydrazones as M1/M3 selective muscarinic agonists},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {1996},
volume = {6},
publisher = {Elsevier},
month = {nov},
url = {https://doi.org/10.1016/0960-894x(96)00471-4},
number = {21},
pages = {2525--2530},
doi = {10.1016/0960-894x(96)00471-4}
}
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MLA
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Wu, Edwin S. C., et al. “Acylhydrazones as M1/M3 selective muscarinic agonists.” Bioorganic and Medicinal Chemistry Letters, vol. 6, no. 21, Nov. 1996, pp. 2525-2530. https://doi.org/10.1016/0960-894x(96)00471-4.
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