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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
A variant peptide of buffalo colostrumß-lactoglobulin inhibits angiotensin I-converting enzyme activity.

University of Mysore
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.

University of Montreal
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
Phosphinic derivatives as new dual enkephalin-degrading enzyme inhibitors: synthesis, biological properties, and antinociceptive activities.

University of Paris
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
Investigation of subsite preferences in aminopeptidase A (EC 3.4.11.7) led to the design of the first highly potent and selective inhibitors of this enzyme.

University of Paris
Mixture-based synthetic combinatorial libraries.

Torrey Pines Institute For Molecular Studies
Optimal recognition of neutral endopeptidase and angiotensin-converting enzyme active sites by mercaptoacyldipeptides as a means to design potent dual inhibitors.

University of Paris
Design of orally active dual inhibitors of neutral endopeptidase and angiotensin-converting enzyme with long duration of action.

University of Paris
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
1,2-Cyclomethylenecarboxylic monoamide hydroxamic derivatives. A novel class of non-amino acid angiotensin converting enzyme inhibitors.

Laboratori Guidotti
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
Angiotensin-converting enzyme inhibitors. 9. Novel [[N-(1-carboxy-3-phenylpropyl)amino]acyl]glycine derivatives with diuretic activity.

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
Synthesis and structure-activity relationships of potent new angiotensin converting enzyme inhibitors containing saturated bicyclic amino acids.

TBA
Angiotensin converting enzyme inhibitors as antihypertensive agents: 1-[(2-mercaptocycloalkyl)carbonyl]-L-prolines.

TBA
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
Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine.

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
Angiotensin converting enzyme inhibitors: 1,5-benzothiazepine derivatives.

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
(Mercaptopropanoyl)indoline-2-carboxylic acids and related compounds as potent angiotensin converting enzyme inhibitors and antihypertensive agents.

TBA
Antihypertensive agents: angiotensin converting enzyme inhibitors. 1-[3-(Acylthio)-3-aroylpropionyl]-L-prolines.

TBA
New carboxyalkyl inhibitors of brain enkephalinase: synthesis, biological activity, and analgesic properties.

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

University of Montreal
Design and synthesis of phosphinic acids that triply inhibit endothelin converting enzyme, angiotensin converting enzyme and neutral endopeptidase 24.11

TBA
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
Studies on the structural feature of S'1 subsite of neprilysin (EC.3.4.24.11): Stereochemical requirement for the enzyme-inhibitor docking process

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
Small-molecule inhibitors of bacterial-producing metallo-β-lactamases: insights into their resistance mechanisms and biochemical analyses of their activities.

University Sains Malaysia
Structure-Guided Chemical Optimization of Bicyclic Peptide (

Bicycletx
1,2,4-Triazole-3-thione analogues with an arylakyl group at position 4 as metallo-β-lactamase inhibitors.

Cnrs
Side Chain Cyclized Aromatic Amino Acids: Great Tools as Local Constraints in Peptide and Peptidomimetic Design.

Vrije Universiteit Brussel
Pseudoprolines as stereoelectronically tunable proline isosteres.

Bristol Myers Squibb
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
Facile incorporation of urea pseudopeptides into protease substrate analogue inhibitors.

Purdue 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
N-[2-(Indan-1-yl)-3-mercapto-propionyl] amino acids as highly potent inhibitors of the three vasopeptidases (NEP, ACE, ECE): In vitro and In vivo activities.

University of Paris
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.

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

The Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery, synthesis, and in vitro evaluation of a novel bioactive peptide for ACE and DPP-IV inhibitory activity.

University of Mysore
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
A mechanism-based inactivation study of neutral endopeptidase 24.11.

Salk Biotechnology/Industrial Associates
Heterocyclic lactam derivatives as dual angiotensin converting enzyme and neutral endopeptidase 24.11 inhibitors.

Ciba-Geigy
New dual inhibitors of neutral endopeptidase and angiotensin-converting enzyme: rational design, bioavailability, and pharmacological responses in experimental hypertension.

University of Paris
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.

Orleans University
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
Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.

Zeneca Pharmaceuticals
Inhibitory effects of various flavonoids isolated from leaves of persimmon on angiotensin-converting enzyme activity.

Ehime University
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
Carboxyalkyl dipeptides with atrial natriuretic factor potentiating and antihypertensive activity.

Schering-Plough Research Institute
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
Structure-function studies of BPP-BrachyNH

Universidade Federal Do Piau£
Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats.

Research and Development Laboratories
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
Quinoxaline compounds and uses thereof

Millennium Pharmaceuticals
Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors

Array Biopharma
Synthesis of some pyrazolyl benzenesulfonamide derivatives as dual anti-inflammatory antimicrobial agents.

University of Alexandria
Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis.

Glaxosmithkline