Výsledky vyhledávání - "Martin S. Domalski"

Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors

Autor: Theresa M. Kelly, John W. Clader, Dmitri A. Pissarnitski, Johannes H. Voigt, Duane A. Burnett, David Cole, Giovanna Scapin, Wen-Lian Wu, Zuliang Yao, Aileen Soriano, Zhiqiang Zhao, Martin S. Domalski, Mary Ann Powles

Publikováno v: Bioorganic & Medicinal Chemistry. 24:5534-5545

Molecular modeling of unbound tricyclic guanine scaffolds indicated that they can serve as effective bioisosteric replacements of xanthines. This notion was further confirmed by a combination of X-ray crystallography and SAR studies, indicating that

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b96060e96c9a81fdd52198d4a12ca14
https://doi.org/10.1016/j.bmc.2016.09.007

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Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:844-849

An investigation is detailed of the structure activity relationships (SAR) of two sulfone side chains of compound (−)- 1a (SCH 900229), a potent, PS1-selective γ-secretase inhibitor and clinical candidate for the treatment of Alzheimer’s disease

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d7acb8f10ab43bcf5cd40b91f4b39ca
https://doi.org/10.1016/j.bmcl.2012.11.047

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Discovery of Orally Efficacious Tetracyclic Metabotropic Glutamate Receptor 1 (mGluR1) Antagonists for the Treatment of Chronic Pain

Autor: Silva Fredduzzi, William J. Greenlee, Rosalia Bertorelli, and Alessio Veltri, Duane A. Burnett, Gianluca Lozza, Wen-Lian Wu, Cheng Li, Martin S. Domalski, Angelo Reggiani

Publikováno v: Journal of Medicinal Chemistry. 50:5550-5553

Metabotropic glutamate receptor 1 (mGluR1) plays important roles in the neurotransmission and pathogenesis of several neurological disorders, including chronic pain. Antagonists of mGlur1 are suggested to be useful for the treatment of pain. Herein,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::512329c68c1cabd0b549c5112ce287bd
https://doi.org/10.1021/jm070590c

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Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists

Autor: Mary Ann Caplen, Andrew Stamford, Carolyn Foster, Yusheng Wu, Ho-Sam Ahn, George Boykow, Duane A. Burnett, Leyla Arik, Martin S. Domalski, Mahua Manna, Michael Czarniecki

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 9:2073-2078

A series of pyrroloquinazolines has been discovered that represent novel small molecule inhibitors of the intramolecular ligand of the thrombin receptor. Analogs were prepared to study the structure-activity relationships of substitution at the N 1,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f136f86334731fdae2e53defb686ddda
https://doi.org/10.1016/s0960-894x(99)00339-x

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Substituted (1,2-Diarylethyl)amide Acyl-CoA:Cholesterol Acyltransferase Inhibitors: Effect of Polar Groups on in Vitro and in Vivo Activity

Autor: Dugar Sundeep, Robert E. Burrier, Brian G. Salisbury, Wayne Vaccaro, Joel G. Berger, Harry R. Davis, Timothy Kogan, John W. Clader, Martin S. Domalski

Publikováno v: Journal of Medicinal Chemistry. 38:1600-1607

Substituted (1,2-diarylethyl)amides have been prepared and evaluated for their ability to inhibit microsomal acyl-CoA:cholesterol acyltransferase activity in vitro and to lower hepatic cholesteryl ester content in vivo in a cholesterol-fed hamster. S

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::25d4adcc1028d2f8364af3276d92c19b
https://doi.org/10.1021/jm00010a004

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A-ring modification of SCH 900229 and related chromene sulfone γ-secretase inhibitors

Autor: William J. Greenlee, Duane A. Burnett, Li Qiang, Wen-Lian Wu, Julie Lee, T.K. Sasikumar, Martin S. Domalski, Tze-Ming Chan, Lili Zhang, John W. Clader

Publikováno v: Bioorganicmedicinal chemistry letters. 23(3)

Attempts to block metabolism by incorporating a 9-fluoro substituent at the A-ring of compound 1 (SCH 900229) using electrophilic Selectfluor™ led to an unexpected oxidation of the A-ring to give difluoroquinone analog 1a. Oxidation of other relate

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57c008eb3f6a1f0d4ab9d90b132179d4
https://pubmed.ncbi.nlm.nih.gov/23265902

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Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain

Autor: Peter Korakas, Duane A. Burnett, Rosalia Bertorelli, Gianluca Lozza, Stephanie Brumfield, T.K. Sasikumar, Cheng Li, Angelo Reggiani, Chad Bennett, Martin S. Domalski, Lisa S. Silverman, Wen-Lian Wu, Li Qiang, Julius Matasi, Chad E. Knutson, Deen Tulshian, Mariagrazia Grilli, William J. Greenlee

Publikováno v: Bioorganicmedicinal chemistry letters. 22(23)

High throughput screening identified the pyridothienopyrimidinone 1 as a ligand for the metabotropic glutamate receptor 1 (mGluR1=10 nM). Compound 1 has an excellent in vivo profile; however, it displays unfavorable pharmacokinetic issues and metabol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b067b63e4caa75f87ad61d50f4143220
https://pubmed.ncbi.nlm.nih.gov/23084894

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