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Start Over Author "Angelastro A" Journal bioorganic & medicinal chemistry letters
15 results on '"Angelastro A"'

2. Time-dependent inactivation of steroid C17(20) lyase by 17β-cyclopropyl ether-substituted steroids

Author

Angela L. Marquart, Marie E. Laughlin, Norton P. Peet, Cynthia A. Gates, Thomas R. Blohm, Philip M. Weintraub, and Michael R. Angelastro

Subjects
chemistry.chemical_classification, C17 20 lyase, Stereochemistry, medicine.medical_treatment, Organic Chemistry, Clinical Biochemistry, Heteroatom, Pharmaceutical Science, Ether, Lyase, Biochemistry, Steroid, chemistry.chemical_compound, Enzyme, chemistry, Drug Discovery, medicine, Molecular Medicine, Androstenes, Molecular Biology, Linker
Abstract

Androstenes bearing a cyclopropyl group attached to the C-17β position with a heteroatom linker, designed as mechanism-based inhibitors of steroid C 17(20) lyase, were found to be potent, time-dependent inhibitors of this enzyme.

Published
1996

3. Janus compounds: dual inhibitors of proteinases

Author

Michael R. Angelastro, Shujaath Mehdi, Philippe Bey, Michael J. Janusz, and Norton P. Peet

Subjects
Chemistry, Organic Chemistry, Clinical Biochemistry, Drug Discovery, Pharmaceutical Science, Molecular Medicine, Janus, DUAL (cognitive architecture), Molecular Biology, Biochemistry, Combinatorial chemistry
Abstract

The concept of dual proteinase inhibition has been demonstrated with the preparation of unsymmetrical bis-terephthalamides.

Published
1993

4. Synthesis of a peptidyl 2,2-difluoro-3-aminopropionate

Author

Shujaath Mehdi, Norton P. Peet, Michael R. Angelastro, and Philippe Bey

Subjects
Proteinase inhibitor, Organic Chemistry, Clinical Biochemistry, Imine, Pharmaceutical Science, Biochemistry, Isovaleraldehyde, chemistry.chemical_compound, Benzylamine, chemistry, Drug Discovery, Molecular Medicine, Organic chemistry, Reformatsky reaction, Molecular Biology
Abstract

Ethyl 3-(benzylamino)-2,2-difluoro-4-methylpentanoate (4) was prepared via a Reformatsky reaction of ethyl bromodifluoroacetate with the imine from isovaleraldehyde and benzylamine. N-Debenzylation of 4 gave amino ester 6, which was coupled to Boc·Ala·Ala·Pro·OH to provide a potential proteinase inhibitor.

Published
1992

7. Preparation of α-keto ester enol acetates as potential prodrugs of human neutrophil elastase inhibitors

Author

Joseph P. Burkhart, Koehl Jack Roger, Norton P. Peet, Shujaath Mehdi, Michael R. Angelastro, and Philippe Bey

Subjects
Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Peptide, Acetates, Biochemistry, Chemical synthesis, chemistry.chemical_compound, Drug Discovery, Humans, Prodrugs, Protease Inhibitors, Molecular Biology, chemistry.chemical_classification, biology, Organic Chemistry, Elastase, Esters, Prodrug, Enol, In vitro, Enzyme, chemistry, Enzyme inhibitor, biology.protein, Molecular Medicine, Leukocyte Elastase
Abstract

Enol acetates of a-keto esters with E configuration were prepared as potential prodrugs for human neutrophil elastase (HNE) inhibitors.

Published
1998

8. Inhibition of oxidosqualene cyclase by substituted quinolizidines

Author

Angela L. Marquart, Steven L. Gallion, Edward W. Huber, Michael R. Angelastro, Gerald L. Schatzman, William R. Moore, and Norton P. Peet

Subjects
chemistry.chemical_classification, Bicyclic molecule, biology, Squalene monooxygenase, Stereochemistry, Lanosterol, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Biological activity, Alkylation, Biochemistry, Quinolizidines, chemistry.chemical_compound, Enzyme, chemistry, Enzyme inhibitor, Drug Discovery, biology.protein, Molecular Medicine, Molecular Biology
Abstract

Substituted hydroxyquinolizidines have been synthesized as conformationally restricted analogs of the type II high energy intermediate formed during the cyclization of 2,3-oxidosqualene to lanosterol. Compounds 4a and 4b were found to be potent inhibitors of rat liver oxidosqualene cyclase (OSC) with Kn values of 0.51 μM and 0.11 μM, respectively.

Published
1994

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