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Design, synthesis and evaluation of novel 2-butyl-4-chloroimidazole derived peptidomimetics as Angiotensin Converting Enzyme (ACE) inhibitors.

Csir-Indian Institute Of Chemical Technology

Top-down Targeted Metabolomics Reveals a Sulfur-Containing Metabolite with Inhibitory Activity against Angiotensin-Converting Enzyme in Asparagus officinalis.

Riken Center For Sustainable Resource Science

CoMFA and CoMSIA analysis of ACE-inhibitory, antimicrobial and bitter-tasting peptides.

Tianjin University

Design and green synthesis of 2-(diarylalkyl)aminobenzothiazole derivatives and their dual activities as angiotensin converting enzyme inhibitors and calcium channel blockers.

Csir-Indian Institute Of Chemical Technology

Interkingdom pharmacology of Angiotensin-I converting enzyme inhibitor phosphonates produced by actinomycetes.

Vanderbilt University Department Of Chemistry

Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-ß hydrolysis.

University Of Lille

Design, synthesis and evaluation of novel 2-hydroxypyrrolobenzodiazepine-5,11-dione analogues as potent angiotensin converting enzyme (ACE) inhibitors.

Csir-Indian Institute Of Chemical Technology

Organosilicon molecules with medicinal applications.

University Of California Davis

Chemical and pharmaceutical studies on medicinal plants in Paraguay. Geraniin, an angiotensin-converting enzyme inhibitor from "paraparai mi," Phyllanthus niruri.

TBA

Thiol-based angiotensin-converting enzyme 2 inhibitors: P1 modifications for the exploration of the S1 subsite.

Glaxosmithkline

Validation of EGSITE2, a mixed integer program for deducing objective site models for experimental binding data.

University Of Michigan

Amino acid side chain descriptors for quantitative structure-activity relationship studies of peptide analogues.

University Of Illinois At Chicago

Three-dimensional quantitative structure-activity relationship of angiotesin-converting enzyme and thermolysin inhibitors. II. A comparison of CoMFA models incorporating molecular orbital fields and desolvation free energies based on active-analog and complementary-receptor-field alignment rules.

Washington University

 

Dual metalloprotease inhibitors. III. utilization of bicyclic and monocyclic diazepinone based mercaptoacetyls

TBA

 

Dual metalloprotease inhibitors. II. Effect of substitution and stereochemistry on benzazepinone based mercaptoacetyls

TBA

 

Dual metalloprotease inhibitors. I. constrained peptidomimetics of mercaptoacyl dipeptides

TBA

Synopsis of some recent tactical application of bioisosteres in drug design.

Bristol-Myers Squibb Pharmaceutical Research And Development

Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.

Universite£

Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.

Aarhus University

Remarkable potential of thea-aminophosphonate/phosphinate structural motif in medicinal chemistry.

Wroclaw University Of Technology

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.

University Of Florida

Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors.

Dipartimento Di Chimica

Targeting ACE and ECE with dual acting inhibitors.

Universit£

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells.

University Institute Of Pathology

Computer-aided selection of potential antihypertensive compounds with dual mechanism of action.

Institute Of Biomedical Chemistry Of Russian Academy Of Medical Sciences

2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.

Merck Research Laboratories

Protease inhibitors: current status and future prospects.

University Of Queensland

Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.

F. Hoffmann-La Roche

Mixture-based synthetic combinatorial libraries.

Torrey Pines Institute For Molecular Studies

New alpha-thiol dipeptide dual inhibitors of angiotensin-I converting enzyme and neutral endopeptidase EC 3.4.24.11.

Ciba-Geigy

New thiol inhibitors of neutral endopeptidase EC 3.4.24.11: synthesis and enzyme active-site recognition.

University Of Paris

Dual angiotensin converting enzyme/thromboxane synthase inhibitors.

Ciba-Geigy

Excursions in drug discovery.

Merck Research Laboratories

Configuration and preferential solid-state conformations of perindoprilat (S-9780). Comparison with the crystal structures of other ACE inhibitors and conclusions related to structure-activity relationships.

Institut De Chimie Des Substances Naturelles

Molecular and crystal structures of MDL27,467A hydrochloride and quinapril hydrochloride, two ester derivatives of potent angiotensin converting enzyme inhibitors.

University Of Calgary

Angiotensin converting enzyme inhibitors. 10. Aryl sulfonamide substituted N-[1-carboxy-3-phenylpropyl]-L-alanyl-L-proline derivatives as novel antihypertensives.

Rorer Central Research

Orally potent human renin inhibitors derived from angiotensinogen transition state: design, synthesis, and mode of interaction.

Kissei Pharmaceutical

Phosphoramidate peptide inhibitors of human skin fibroblast collagenase.

University Of Kentucky

Angiotensin converting enzyme inhibitors: spirapril and related compounds.

Schering-Plough

Inhibition of aminopeptidases by peptides containing ketomethylene and hydroxyethylene amide bond replacements.

University Of Wisconsin-Madison

Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.

Tanabe Seiyaku

Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.

Squibb Institute For Medical Research

Synthesis and pharmacological activity of angiotensin converting enzyme inhibitors: N-(mercaptoacyl)-4-substituted-(S)-prolines.

Schering-Plough

Angiotensin-converting enzyme inhibitors. 2. Perhydroazepin-2-one derivatives.

Sankyo

Conformationally restricted inhibitors of angiotensin converting enzyme: synthesis and computations.

TBA

Design and synthesis of potent and specific renin inhibitors containing difluorostatine, difluorostatone, and related analogues.

TBA

Synthesis of novel angiotensin converting enzyme inhibitor quinapril and related compounds. A divergence of structure-activity relationships for non-sulfhydryl and sulfhydryl types.

TBA

Synthesis and biological activity of modified peptide inhibitors of angiotensin-converting enzyme.

TBA

Conformational analysis and active site modelling of angiotensin-converting enzyme inhibitors.

TBA

Angiotensin converting enzyme inhibitors. (Mercaptoaroyl)amino acids.

TBA

Angiotensin converting enzyme inhibitors: N-substituted D-glutamic acid gamma dipeptides.

TBA

Angiotensin converting enzyme inhibitors: structure-activity profile of 1-benzazepin-2-one derivatives.

TBA

Difluorostatine- and difluorostatone-containing peptides as potent and specific renin inhibitors.

TBA

Synthesis and biological properties of (carboxyalkyl)amino-substituted bicyclic lactam inhibitors of angiotensin converting enzyme.

TBA

Angiotensin-converting enzyme inhibitors. New orally active antihypertensive (mercaptoalkanoyl)- and [(acylthio)alkanoyl]glycine derivatives.

TBA

Bicyclic lactam inhibitors of angiotensin converting enzyme.

TBA

Angiotensin converting enzyme inhibitors: 1-glutarylindoline-2-carboxylic acids derivatives.

TBA

Angiotensin converting enzyme inhibitors: N-substituted monocyclic and bicyclic amino acid derivatives.

TBA

Probing the importance of spacial and conformational domains in captopril analogs for angiotensin converting enzyme activity.

Universit£

 

Kelatorphan and related analogs: potent and selective inhibitors of leukotriene A4 hydrolase

TBA

 

Novel angiotensin converting enzyme inhibitors containing -hydroxy ketomethylene dipeptide isosteres

TBA

 

4-Substituted proline derivatives that inhibit angiotensin converting enzyme and neutral endopeptidase 24.11.

TBA

 

Mercaptoacyl dipeptides as dual inhibitors of angiotensin-converting enzyme and neutral endopeptidase. Preliminary structure-activity studies

TBA

 

Thiol and hydroxamic acid containing inhibitors of endothelin converting enzyme

TBA

 

A new potent inhibitor for angiotensin converting enzyme: (R,S)-captopril-F3

TBA

Synthesis and evaluation of novel 2-butyl-4-chloro-1-methylimidazole embedded chalcones and pyrazoles as angiotensin converting enzyme (ACE) inhibitors.

India Institute Of Chemical Technology

Angiotensin-I-converting enzyme inhibitory peptides: Chemical feature based pharmacophore generation.

Zhejiang University

Blockade of X4-tropic HIV-1 cellular entry by GSK812397, a potent noncompetitive CXCR4 receptor antagonist.

Glaxosmithkline

The synthesis and angiotensin converting enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives.

University Of Calabria

Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors.

Cea

The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.

Gsk Medicines Research Centre

Inhibition of Angiotensin-I-Converting Enzyme by Tetrahydroxyxanthones Isolated from Tripterospermum lanceolatum

TBA

Isolation and structure of leukotriene-A4 hydrolase inhibitor: 8(S)-amino-2(R)-methyl-7-oxononanoic acid produced by Streptomyces diastaticus.

Searle Research And Development

 

Novel low molecular renin inhibitors which show good oral blood pressure lowering effects in marmosets

TBA

 

The design of a dipeptide library for screening at peptide receptor sites

TBA

 

K-13 and of4949: Evaluation of key partial structures and pharmacophore delineation

TBA

 

Synthesis of 6-amino-5-oxo-7-phenyl-1,4-oxazepines as conformationally constrained gauche (−) dipeptide mimetics

TBA

 

Acid-catalyzed O-allylation of β-hydroxy-α-amino acids: an entry into conformationally constrained dipeptide surrogates

TBA

 

An acyliminium ion route to Cis and Trans "Anti" phe-gly dipeptide mimetics

TBA

Synthesis and biological evaluation of N-mercaptoacylcysteine derivatives as leukotriene A4 hydrolase inhibitors.

Santen Pharmaceutical

Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.

University Of Athens

Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.

University Of Leipzig

Synthesis and biological evaluation of N-mercaptoacylproline and N-mercaptoacylthiazolidine-4-carboxylic acid derivatives as leukotriene A4 hydrolase inhibitors.

Santen Pharmaceutical

Synthesis of novel keto-ACE analogues as domain-selective angiotensin I-converting enzyme inhibitors.

University Of Cape Town

Enzyme inhibition as a potential therapeutic strategy to treat COVID-19 infection.

Kingston University

Synthesis and molecular modeling of a lisinopril-tryptophan analogue inhibitor of angiotensin I-converting enzyme.

University Of Cape Town

Structure-activity relationship study between Ornithyl-Proline and Lysyl-Proline based tripeptidomimics as angiotensin-converting enzyme inhibitors.

Institute Of Genomics And Integrative Biology

Zinc enzymes in medicinal chemistry.

Hefei University Of Technology

Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.

F. Hoffmann-La Roche

Natural products from mangrove sediments-derived microbes: Structural diversity, bioactivities, biosynthesis, and total synthesis.

Chinese Academy Of Sciences

Bradykinin-Potentiating Peptide-Paclitaxel Conjugate Directed at Ectopically Expressed Angiotensin-Converting Enzyme in Triple-Negative Breast Cancer.

Hong Kong Baptist University

Probing the Requirements for Dual Angiotensin-Converting Enzyme C-Domain Selective/Neprilysin Inhibition.

University Of Cape Town

Silanediol peptidomimetics. Evaluation of four diastereomeric ACE inhibitors.

State University Of New York

Virtual Screening Approach to Identifying a Novel and Tractable Series of

Antabio

Asymmetric synthesis of BB-3497--a potent peptide deformylase inhibitor.

British Biotech Pharmaceuticals

2-(2-Oxo-1,4-dihydro-2H-quinazolin-3-yl)- and 2-(2,2-dioxo-1,4-dihydro-2H-2lambda6-benzo[1,2,6]thiadiazin-3-yl)-N-hydroxy-acetamides as potent and selective peptide deformylase inhibitors.

F. Hoffmann-La Roche

Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.

Roche Pharma Research And Early Development

N-formyl hydroxylamine containing dipeptides: generation of a new class of vasopeptidase inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Molecular Basis for Omapatrilat and Sampatrilat Binding to Neprilysin-Implications for Dual Inhibitor Design with Angiotensin-Converting Enzyme.

University Of Bath

1-(2-Hydroxybenzoyl)-thiosemicarbazides are promising antimicrobial agents targeting d-alanine-d-alanine ligase in bacterio.

Universit£

Vasopeptidase inhibitors: incorporation of geminal and spirocyclic substituted azepinones in mercaptoacyl dipeptides.

The Bristol-Myers Squibb Pharmaceutical Research Institute

Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives.

Shionogi

Meta-substituted benzofused macrocyclic lactams as zinc metalloprotease inhibitors.

Ciba-Geigy

Discovery of TD-0212, an Orally Active Dual Pharmacology AT

Theravance Biopharma Us

Dual metalloprotease inhibitors. 6. Incorporation of bicyclic and substituted monocyclic azepinones as dipeptide surrogates in angiotensin-converting enzyme/neutral endopeptidase inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and analgesic effects of N-[3-[(hydroxyamino) carbonyl]-1-oxo-2(R)-benzylpropyl]-L-isoleucyl-L-leucine, a new potent inhibitor of multiple neurotensin/neuromedin N degrading enzymes.

Ccipe-Faculté

Exploration of neutral endopeptidase active site by a series of new thiol-containing inhibitors.

University Of Paris

Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors.

Csir-Indian Institute Of Chemical Technology

Application of a conformationally restricted Phe-Leu dipeptide mimetic to the design of a combined inhibitor of angiotensin I-converting enzyme and neutral endopeptidase 24.11.

Marion Merrell Dow Research Institute

Heterocyclic lactam derivatives as dual angiotensin converting enzyme and neutral endopeptidase 24.11 inhibitors.

Ciba-Geigy

Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.

E£Tv£S Lor£Nd University

Perindopril and ramipril phosphonate analogues as a new class of angiotensin converting enzyme inhibitors.

Universit£

Mercaptoacyl amino acid inhibitors of atriopeptidase. 1. Structure-activity relationship studies of methionine and S-alkylcysteine derivatives.

Schering-Plough Research Institute

PRO_LIGAND: an approach to de novo molecular design. 2. Design of novel molecules from molecular field analysis (MFA) models and pharmacophores.

Proteus Molecular Design

Non-peptidic inhibitors of human leukocyte elastase. 4. Design, synthesis, and in vitro and in vivo activity of a series of beta-carbolinone-containing trifluoromethyl ketones.

Zeneca Pharmaceuticals

The molecular basis for the selection of captopril cis and trans conformations by angiotensin I converting enzyme.

Mrc Laboratory Of Molecular Biology, Hills Road, Cambridge, Cb2 2Qh

Molecular Basis for Multiple Omapatrilat Binding Sites within the ACE C-Domain: Implications for Drug Design.

University Of Bath

Angiotensin-converting enzyme inhibitors: perhydro-1,4-thiazepin-5-one derivatives.

Sankyo

Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.

Csir-National Chemical Laboratory

Angiotensin-converting enzyme inhibitors: new orally active 1,4-thiazepine-2,5-diones, 1,4-thiazine-2,5-diones, and 1,4-benzothiazepine-2,5-diones possessing antihypertensive activity.

TBA

N alpha-(diphenoxyphosphoryl)-L-alanyl-L-proline, N alpha-[bis (4-nitrophenoxy)phosphoryl]-L-alanyl-L-proline, and N alpha-[ (2-phenylethyl)phenoxyphosphoryl]-L-alanyl-L-proline: releasers of potent inhibitors of angiotensin converting enzyme at physiological pH and temperature.

TBA

Metabolomics-Guided Discovery of Microginin Peptides from Cultures of the Cyanobacterium Microcystis aeruginosa.

University Of North Carolina Wilmington

Therapeutic investigations of novel indoxyl-based indolines: A drug target validation and Structure-Activity Relationship of angiotensin-converting enzyme inhibitors with cardiovascular regulation and thrombolytic potential.

Vit University

A novel class of enkephalinase inhibitors containing a C-terminal sulfo group.

Dainippon Pharmaceutical

Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.

Ranbaxy Laboratories

Insights from selective non-phosphinic inhibitors of MMP-12 tailored to fit with an S1' loop canonical conformation.

Commissariat À

Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.

Taisho Pharmaceutical

Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors.

Millennium Pharmaceuticals

Development of Potent and Selective Phosphinic Peptide Inhibitors of Angiotensin-Converting Enzyme 2.

University Of Athens