Výsledky vyhledávání - "Koehl Jack Roger"

Inhibition of Human Neutrophil Elastase. 4. Design, Synthesis, X-ray Crystallographic Analysis, and Structure−Activity Relationships for a Series of P2-Modified, Orally Active Peptidyl Pentafluoroethyl Ketones

Autor: Herman Schreuder, William A. Metz, R.V. Hoffman, Robert J. Cregge, Farr Robert A, Koehl Jack Roger, Hwa-Ok Kim, Norton P. Peet, Shyam Sunder, S L Durham, M J Janusz, C M Hare, Chantal Tardif, J.T. Pelton, Shujaath Mehdi, S.L. Gallion

Publikováno v: Journal of Medicinal Chemistry. 41:2461-2480

A series of P2-modified, orally active peptidic inhibitors of human neutrophil elastase (HNE) are reported. These pentafluoroethyl ketone-based inhibitors were designed using pentafluoroethyl ketone 1 as a model. Rational structural modifications wer

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4e62bd64a5e7c526d716bc7351e4672
https://doi.org/10.1021/jm970812e

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Synthesis of constrained thiorphan analogs as inhibitors of neutral endopeptidase

Autor: Beight Douglas W, Gary A. Flynn, Shujaath Mehdi, Koehl Jack Roger

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 6:2053-2058

Constrained derivatives of thiorphan were prepared and found to be potent inhibitors of neutral endopeptidase 24.11.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c7fb5a3b810ac66990bacecb3677833b
https://doi.org/10.1016/0960-894x(96)00367-8

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The synthesis of aminobenzazepinones as anti-phenylalanine dipeptide mimics and their use in nep inhibition

Autor: Warshawsky Alan M, Gary A. Flynn, Roy J. Vaz, Koehl Jack Roger, Shujaath Mehdi

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 6:957-962

A general and stereoselective synthesis of 4-aminobenzazepinones is presented. This peptidomimetic structure was used in the preparation of MDL 100,407, a potent inhibitor of NEP.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d9475836f9793fb4b4bed7b019166a37
https://doi.org/10.1016/0960-894x(96)00149-7

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(E) and (Z)5′-fluoro olefin carbocyclic nucleosides: effect of olefin geometry on inhibition of s-adenosyl-l-homocysteine hydrolase

Autor: Donald P. Matthews, Shujaath Mehdi, Jeffrey A. Wolos, James R. McCarthy, Koehl Jack Roger, Edwards Michael L

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 3:165-168

(E) and (Z) 4′,5′-Didehydro-5′-deoxy-5′-fluoroaristeromycin ( 9a and 9b ) were synthesized utilizing the fluoro-Pummerer reaction . Fluoro olefin 9a was a time-dependent inhibitor of S-adenosyl-L- homocysteine hydrolase whereas 9b was a compe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e5db2813b6129b4f2c4fa403062bb6bf
https://doi.org/10.1016/s0960-894x(01)80869-6

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ChemInform Abstract: The Synthesis of Ketomethylene Pseudopeptide Analogues of Dipeptide Aldehyde Inhibitors of Calpain

Autor: Shujaath Mehdi, Angela L. Marquart, Norton P. Peet, Philippe Bey, Michael R. Angelastro, Koehl Jack Roger, Roy J. Vaz

Publikováno v: ChemInform. 30

The ketomethylene phenylalanal and alanal analogues of Cbz-Val-Phe-H and Cbz-Val-Ala-H have been prepared and the K i values versus chicken gizzard smooth muscle calpain were determined. The ketomethylene isosteres were significantly less potent than

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9b51b3fef29849012b50d7ce70b67dda
https://doi.org/10.1002/chin.199919227

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The Mechanism of Inhibition of S-Adenosyl-L-Homocysteine Hydrolase by Fluorine-Containing Adenosine Analogs

Autor: Esa T. Jarvi, Philippe Bey, Koehl Jack Roger, James R. McCarthy, Shujaath Mehdi

Publikováno v: Journal of Enzyme Inhibition. 4:1-13

(Z)-4',5'-Didehydro-5'-deoxy-5'-fluoroadenosine (I), 5'-deoxy-5'-difluoroadenosine (II), and 4',5'-didehydro-5'-deoxy-5'-fluoroarabinosyl-adenosine (III) are inhibitors of rat liver S-adenosyl-L-homocysteine hydrolase. Compounds I and II are time-dep

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3e81ac4810044145455a1c5926f86f3
https://doi.org/10.3109/14756369009030383

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Hydroxyoxazolidines as alpha-aminoacetaldehye equivalents: novel inhibitors of calpain

Autor: Gary A. Flynn, Michael R. Angelastro, Julie N. White, Mark E. Webster, Kin-Kai Hwang, Bart Emary, Angela L. Marquart, Koehl Jack Roger, Dirk Friedrich, Shujaath Mehdi, Nieduzak Thaddeus R, Norton P. Peet, Philippe Bey, Hwa-Ok Kim, Roy J. Vaz, Matthew D Linnik

Publikováno v: Bioorganicmedicinal chemistry letters. 9(16)

The synthesis of [1-[(5-hydroxy-4-(phenylmethyl)-3-oxazolidinyl)carbonyl]-2-ethylpropyl]carbamic acid phenylmethyl ester (2; MDL 104,903), a potent inhibitor of calpain, is described. Synthesis of related compounds, which offer insights into the mech

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b99fd2dc1413c4e220bbc60c4c7f83c9
https://pubmed.ncbi.nlm.nih.gov/10476870

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