Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead
Тип публикации: Journal Article
Дата публикации: 2006-05-01
SCImago Q2
WOS Q2
БС2
SJR: 0.426
CiteScore: 4.5
Impact factor: 2.3
ISSN: 0960894X, 14643405
PubMed ID:
16527483
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
High-throughput screening of the Merck sample collection identified benzodiazepinone tetralin-spirohydantoin 1 as a CGRP receptor antagonist with micromolar activity. Comparing the structure of 1 with those of earlier peptide-based antagonists such as BIBN 4096 BS, a key hydrogen bond donor-acceptor pharmacophore was hypothesized. Subsequent structure activity studies supported this hypothesis and led to benzodiazepinone piperidinyldihydroquinazolinone 7, CGRP receptor K(i)=44nM and IC(50)=38nM. Compound 7 was orally bioavailabile in rats and is a lead in the development of orally bioavailable CGRP antagonists for the treatment of migraine.
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MLA
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ГОСТ
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Williams T. M. et al. Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead // Bioorganic and Medicinal Chemistry Letters. 2006. Vol. 16. No. 10. pp. 2595-2598.
ГОСТ со всеми авторами (до 50)
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Williams T. M., Stump C. A., Nguyen D. B., Quigley A. G., Bell I., Gallicchio S. N., Zartman C., Wan B., Penna K. D., Kunapuli P., Kane S. A., Koblan K. S., Mosser S. D., Rutledge R. Z., Salvatore C., Fay J. F., Vacca J. P., Graham S. Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead // Bioorganic and Medicinal Chemistry Letters. 2006. Vol. 16. No. 10. pp. 2595-2598.
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TY - JOUR
DO - 10.1016/j.bmcl.2006.02.051
UR - https://doi.org/10.1016/j.bmcl.2006.02.051
TI - Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Williams, Theresa M.
AU - Stump, Craig A.
AU - Nguyen, Diem B.
AU - Quigley, Amy G.
AU - Bell, Ian
AU - Gallicchio, Steven N
AU - Zartman, C.Blair
AU - Wan, Bang-Lin
AU - Penna, Kimberly Della
AU - Kunapuli, Priya
AU - Kane, Stefanie A
AU - Koblan, Ken S.
AU - Mosser, Scott D
AU - Rutledge, Ruth Z.
AU - Salvatore, Christopher
AU - Fay, John F.
AU - Vacca, Joseph P.
AU - Graham, Samuel
PY - 2006
DA - 2006/05/01
PB - Elsevier
SP - 2595-2598
IS - 10
VL - 16
PMID - 16527483
SN - 0960-894X
SN - 1464-3405
ER -
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BibTex (до 50 авторов)
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@article{2006_Williams,
author = {Theresa M. Williams and Craig A. Stump and Diem B. Nguyen and Amy G. Quigley and Ian Bell and Steven N Gallicchio and C.Blair Zartman and Bang-Lin Wan and Kimberly Della Penna and Priya Kunapuli and Stefanie A Kane and Ken S. Koblan and Scott D Mosser and Ruth Z. Rutledge and Christopher Salvatore and John F. Fay and Joseph P. Vacca and Samuel Graham},
title = {Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2006},
volume = {16},
publisher = {Elsevier},
month = {may},
url = {https://doi.org/10.1016/j.bmcl.2006.02.051},
number = {10},
pages = {2595--2598},
doi = {10.1016/j.bmcl.2006.02.051}
}
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MLA
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Williams, Theresa M., et al. “Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead.” Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 10, May. 2006, pp. 2595-2598. https://doi.org/10.1016/j.bmcl.2006.02.051.
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