Výsledky vyhledávání - "Stephen Condon"

Synthesis and In Vitro evaluation of fused ring heterocyle-containing angiotensin II antagonists

Autor: Stephen Condon, Jang Y. Lee, Bryan K. Sorensen, Thomas M. Zydowsky, Boyd Steven A, Daniel J. Kerkman, Steven A. Buckner, Robert J. Altenbach, Terry J. Opgenorth, Arthur A. Hancock, John F. DeBernardis, Eugene I. Novosad, Martin Winn, Fatima Z. Basha, Andrew Tasker, Biswanath De, Kazumi Shiosaki, Robert A. Mantei

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 4:173-176

Fused ring heterocyclic analogs of A-81080 (pA2= 9.9) were synthesized and their activities in the rabbit aorta in vitro assay were measued. The best compounds (pA2 = 8.6) in series 1 had R1 = Et, R2 = H, W = X = Z = C-H, and Y = C-OMe or C-COOH. In

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::13e0d3b3618271efe8730de5bf44c053
https://doi.org/10.1016/s0960-894x(01)81142-2

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Dipeptide isosteres. 1. Synthesis of dihydroxyethylene dipeptide isosteres via diastereoselective additions of alkyllithium reagents to N,N-dimethylhydrazones. Preparation of renin and HIV-1 protease inhibitor transition-state mimics

Autor: Stephen Condon, William R. Baker

Publikováno v: The Journal of Organic Chemistry. 58:3277-3284

The amino and diamino dihydroxyethylene dipeptide isosteres 19a,b and 23 are important intermediates for the preparation of inhibitors of human renin and HIV-1 protease, respectively. A general synthetic strategy was developed to access both dipeptid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ee139db24848d48454d9f33677940d54
https://doi.org/10.1021/jo00064a013

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Effects of Angiotensinase Inhibitors on Plasma Protein Binding and IC50 Determinations of Renin Inhibitors

Autor: Stephen Condon, J R Luly, B G Donner, S A Boyd, Jerome Cohen, Anthony K. L. Fung, Herman H. Stein, B D Dayton, S H Rosenberg, William R. Baker

Publikováno v: Clinical Chemistry. 38:2239-2243

To establish whether the use of proteinase inhibitors in the routine determination of in vitro plasma renin activity overestimates the potency of renin inhibitors in vivo, we examined the effects of phenylmethylsulfonyl fluoride and 8-hydroxyquinolin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6a97871d9a1678bbbc6a1bae891791e7
https://doi.org/10.1093/clinchem/38.11.2239

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1,2,3-Trisubstituted cyclopropanes as conformationally restricted peptide isosteres: application to the design and synthesis of novel renin inhibitors

Autor: Ed DeLara, Stephen F. Martin, Jerome Cohen, Richard E. Austin, Kenneth P. Spina, Stephen Condon, Hollis D. Kleinert, Herman H. Stein, Christopher J. Oalmann, Saul H. Rosenberg, William R. Baker

Publikováno v: Journal of Medicinal Chemistry. 35:1710-1721

The 1,2,3-trisubstituted cyclopropanes 6 and 7 are the first members of a novel class of isosteric replacements for peptide linkages that are more generally represented by the dipeptide mimics 2 and 3. These unique peptide surrogates are specifically

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b2f1ca0fe9c55907e3ac16a8eac056a
https://doi.org/10.1021/jm00088a005

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Slow, tight binding to human renin of some nonpeptidic renin inhibitors containing a 4-methoxymethoxypiperidinylamide at the P4 position

Autor: Stephen Condon, Brian D. Dayton, Saul H. Rosenberg, Robert A. Mantei, Jerome Cohen, Hollis D. Kleinert, Yoek Lin Armiger, Boyd Steven A, Herman H. Stein, Anthony K. L. Fung, William R. Baker

Publikováno v: FEBS Letters. 300:301-304

A series of nonpeptidic human renin inhibitors with a 4-methoxymethoxypiperidinylamide at the P4 position of the molecule exhibited slow tight binding to the enzyme. Replacement of the methoxymethoxy moiety on the piperidine ring with H, OH, methoxye

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::260d860f3633b01e90ab5eb22bb304d3
https://doi.org/10.1016/0014-5793(92)80867-g

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Synthesis and Structure Determination of (3S, 5S)-2,3,5,6-Tetrahydro-3,5-dialkyl-N-(tert-butyloxycarbonyl)-4H-1,4-oxazine-2-ones

Autor: Stephen G. Spanton, Stephen Condon, William R. Baker

Publikováno v: Tetrahedron Letters. 33:1573-1576

(5S)-2,3,5,6-Tetrahydro-5-alkyl-N-(tert-butyloxycarbonyl)-4H-1,4-oxazine-2-ones, which are readily prepared from optically pure 2-amino alcohols alkylate selectively at the C-3 position to give (3S, 5S)-dialkyl-2,3,5,6-tetrahydro-5-alkyl-N-(tert-buty

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d914fd56e2dfb5feb91e439f2ea5a68a
https://doi.org/10.1016/s0040-4039(00)91677-0

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A Practical Synthesis of the Dihydroxyethylene Dipeptide Isostere, (2S, 3R, 4S) 2-[(tert-Butyloxycarbonyl)amino]-1-cyclohexyl-3,4-dihydroxy-6-methylheptane, from D-Isoascorbic Acid

Autor: Stephen Condon, William R. Baker

Publikováno v: Tetrahedron Letters. 33:1581-1584

The N-Boc dihydroxyethylene dipeptide isostere 7 and its N-Boc 3-(thiazol-4-yl)alanyl derivative 8 were synthesized, without purification of intermediates, from (4S,5R)-2,2-dimethyl-4-(2-methylpropyl)-5-hydroxymethyl-1,3-dioxolane ( 3b ), in 24 and 3

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::438abb66811a83db27fc112db117abbf
https://doi.org/10.1016/s0040-4039(00)91679-4

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Synthesis of the Nonpeptide Renin Inhibitor A-68064 and the ACE Inhibitor Methyl Enalaprilat from (5S)-2,3,5,6-Tetrahydro-5-alkyl-N-(tert-butyloxycarbonyl-4H-1,4-oxazine-2-ones

Autor: Stephen Condon, William R. Baker

Publikováno v: Tetrahedron Letters. 33:1577-1580

The nonpeptide renin inhibitor, A-68064, and the ACE inhibitor methyl enalaprilat were synthesized from (5S) 2,3,5,6-tetrahydro-5-benzyl(butyl)-N-(tert-butoxycarbonyl)-4H-1,4-oxazine-2-ones 7a and 7b, and (5S) 2,3,5,6-tetrahydro-5-methyl-N-(tert-buto

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cc64c8f45dd426cc2705d7aa95dbe592
https://doi.org/10.1016/s0040-4039(00)91678-2

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Highly efficient EO polymers for low V π modulators

Autor: Jingdong Luo, Stephen Condon, Hui Chen, Danliang Jin, Anna Barklund, Raluca Dinu, Zhengwei Shi, Eric L. Miller, Baoquan Chen, Guomin Yu, Su Huang, Diyun Huang, Tae-Dong Kim, Don Tolstedt, Alex K.-Y. Jen

Publikováno v: Linear and Nonlinear Optics of Organic Materials VIII.

Poly(methyl methacrylate- co -9-anthrylmethyl methacrylate) (PMMA-AMA) LP-136 with various AMA contents was prepared. The polymer was modified via Diels-Alder (D-A) type "click chemistry". In one approach, the side-chain was grafted stepwise with mal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b28fae747aafd155c85279bda37e6b32
https://doi.org/10.1117/12.795561

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