202 articles for thisTarget
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Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor.
Takeda Pharmaceutical
Novel approach of fragment-based lead discovery applied to renin inhibitors.
Takeda Pharmaceutical
Structure-based design of a new series of N-(piperidin-3-yl)pyrimidine-5-carboxamides as renin inhibitors.
Takeda Pharmaceutical
Discovery of highly potent renin inhibitors potentially interacting with the S3' subsite of renin.
China Pharmaceutical University
trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.
Novartis Pharma
trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.
Novartis Pharma
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.
Merck Research Laboratories
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Novartis Institutes For Biomedical Research
Inhibitors ofß-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718).
Amgen
Novel BACE1 inhibitors with a non-acidic heterocycle at the P1' position.
Kyoto Pharmaceutical University
The thermodynamic basis for the use of lipophilic efficiency (LipE) in enthalpic optimizations.
Novartis Institutes For Biomedical Research
Synthesis and optimization of novel (3S,5R)-5-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)piperidine-3-carboxamides as orally active renin inhibitors.
Daiichi Sankyo
Lead optimization of 5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxyhexanamides to reduce a cardiac safety issue: discovery of DS-8108b, an orally active renin inhibitor.
Daiichi Sankyo
ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.
F. Hoffmann-La Roche
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.
Novartis Pharma
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
Novartis Pharma
Renin inhibitors. Free-Wilson and correlation analysis of the inhibitory potency of a series of pepstatin analogues on plasma renin.
Sanofi Recherche
An integrated computational workflow for efficient and quantitative modeling of renin inhibitors.
Sanofi Us
Design and discovery of new (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides as potent renin inhibitors.
Daiichi Sankyo
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.
Universite£
Dual inhibitors for aspartic proteases HIV-1 PR and renin: advancements in AIDS-hypertension-diabetes linkage via molecular dynamics, inhibition assays, and binding free energy calculations.
National Hellenic Research Foundation
Design and optimization of novel (2S,4S,5S)-5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxy-2-isopropylhexanamides as renin inhibitors.
Daiichi Sankyo
Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.
TBA
Design and synthesis of potent, isoxazole-containing renin inhibitors.
Merck Frosst Centre For Therapeutic Research
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University of Florida
Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors.
Actelion Pharmaceuticals
Non-peptide renin inhibitors containing 2-(((3-phenylpropyl)phosphoryl)oxy)alkanoic acid moieties as P2-P3 replacements.
E. Merck Darmstadt
Potent and selective inhibitors of an aspartyl protease-like endothelin converting enzyme identified in rat lung.
Abbott Laboratories
Highly potent, orally active diester macrocyclic human renin inhibitors.
Merck Research Laboratories
Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.
Parke-Davis Pharmaceutical Research Division of Warner-Lambert
Design and synthesis of potent, selective, and orally active fluorine-containing renin inhibitors.
Warner-Lambert
Determination of dissociation constants of high affinity (pM) human renin inhibitors: application to analogues of ditekiren (U-71,038).
Upjohn Laboratories
Renin inhibitors containing esters at the P2-position. Oral activity in a derivative of methyl aminomalonate.
Warner-Lambert
Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics.
Merck Sharp and Dohme Research Laboratories
Substrate analogue renin inhibitors containing replacements of histidine in P2 or isosteres of the amide bond between P3 and P2 sites.
E. Merck Darmstadt
Novel inhibitors of human renin. Cyclic peptides based on the tetrapeptide sequence Glu-D-Phe-Lys-D-Trp.
Ici Pharmaceuticals Group
Water-soluble renin inhibitors: design of a subnanomolar inhibitor with a prolonged duration of action.
Abbott Laboratories
Renin inhibitory peptides. A beta-aspartyl residue as a replacement for the histidyl residue at the P-2 site.
Upjohn
Orally potent human renin inhibitors derived from angiotensinogen transition state: design, synthesis, and mode of interaction.
Kissei Pharmaceutical
Inhibition of aminopeptidases by peptides containing ketomethylene and hydroxyethylene amide bond replacements.
University of Wisconsin-Madison
Azido glycols: potent, low molecular weight renin inhibitors containing an unusual post scissile site residue.
Abbott Laboratories
Synthesis and renin inhibitory activity of angiotensinogen analogues having dehydrostatine, Leu psi [CH2S]Val, or Leu psi [CH2SO]Val at the P1-P1' cleavage site.
Upjohn
Conformationally constrained renin inhibitory peptides: gamma-lactam-bridged dipeptide isostere as conformational restriction.
Upjohn
Design, structure-activity, and molecular modeling studies of potent renin inhibitory peptides having N-terminal Nin-For-Trp (Ftr): angiotensinogen congeners modified by P1-P1' Phe-Phe, Sta, Leu psi[CH(OH)CH2]Val or leu psi[CH2NH]Val substitutions.
Upjohn
Novel renin inhibitors containing analogues of statine retro-inverted at the C-termini: specificity at the P2 histidine site.
TBA
alpha-Methylproline-containing renin inhibitory peptides: in vivo evaluation in an anesthetized, ganglion-blocked, hog renin infused rat model.
TBA
Optimization and in vivo evaluations of a series of small, potent, and specific renin inhibitors containing a novel Leu-Val replacement.
Abbott Laboratories
Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo.
TBA
Design and synthesis of potent and specific renin inhibitors containing difluorostatine, difluorostatone, and related analogues.
TBA
Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine.
TBA
Difluorostatine- and difluorostatone-containing peptides as potent and specific renin inhibitors.
TBA
Inhibition of renin by angiotensinogen peptide fragments containing the hydroxy amino acid residue 5-amino-3-hydroxy-7-methyloctanoic acid.
TBA
Renin inhibitors. Substitution of the leucyl residues of Leu-Leu-Val-Phe-OCH3 with 3-amino-2-hydroxy-5-methylhexanoic acid.
TBA
Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension.
TBA
Peptidomimetic inhibitors of human immunodeficiency virus protease (HIV-PR): Design, enzyme binding and selectivity, antiviral efficacy, and cell permeability properties
TBA
3,4-Diarylpiperidines as potent renin inhibitors.
Merck Frosst Center For Therapeutic Research
Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.
Merck Research Laboratories
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of spirocyclic piperidines.
Merck Frosst Centre For Therapeutic Research
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.
Merck Frosst Centre For Therapeutic Research
Structure-based optimization of potent 4- and 6-azaindole-3-carboxamides as renin inhibitors.
Deutschland
Structure-based design and optimization of potent renin inhibitors on 5- or 7-azaindole-scaffolds.
Sanofi-Aventis Deutschland
Biphenyl/diphenyl ether renin inhibitors: filling the S1 pocket of renin via the S3 pocket.
Vitae Pharmaceuticals
Synthesis, biological evaluation and docking studies of octane-carboxamide based renin inhibitors with extended segments toward S3' site of renin.
China Pharmaceutical University
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.
Merck Frosst Centre For Therapeutic Research
Potential virtual lead identification in the discovery of renin inhibitors: application of ligand and structure-based pharmacophore modeling approaches.
Gyeongsang National University (Gnu)
The discovery and synthesis of potent zwitterionic inhibitors of renin.
Merck Frosst Centre For Therapeutic Research
Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.
Pfizer
Discovery and optimization of a new class of potent and non-chiral indole-3-carboxamide-based renin inhibitors.
Sanofi-Aventis Deutschland
Design and optimization of new piperidines as renin inhibitors.
Actelion Pharmaceuticals
Identification of a new biaryl scaffold generating potent renin inhibitors.
Merck Frosst Center For Therapeutic Research
Addressing time-dependent CYP 3A4 inhibition observed in a novel series of substituted amino propanamide renin inhibitors, a case study.
Merck Frosst Centre For Therapeutic Research
Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension.
Merck Frosst Centre For Therapeutic Research
Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.
Wyeth Research
Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.
Wyeth Research
Synthesis and evaluation of A-seco type triterpenoids for anti-HIV-1protease activity.
University of Toyama
The P1N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin.
Nagasaki International University
Design and synthesis of novel 2,7-dialkyl substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides as in vitro potent peptidomimetic inhibitors of human renin
TBA
Novel low molecular renin inhibitors which show good oral blood pressure lowering effects in marmosets
TBA
Bioactive hydroxyethylene dipeptide isosteres with hydrophobic (P3-P1)-moieties. A novel strategy towards small non-peptide renin inhibitors
TBA
Synthesis of α-hydroxy statine through a facially selective osmylation of a chiral α-amido crotonate
TBA
Rational design, synthesis, and X-ray structure of renin inhibitors with extended P1 sidechains
TBA
The identification of a novel renin inhibitor of equivalent efficacy following oral or intravenous administration.
TBA
Peptidomimetic inhibitors of renin incorporating topographically modified isosteres spanning the P1(→ P3)-P1' sites
TBA
MDL 74147, a novel selective and soluble inhibitor of human renin. Synthesis, structure-activity relationship, species and protease selectivities.
TBA
Conformationally restricted peptide isosteres. 2.1 Synthesis and in vitro potency of dipeptide renin inhibitors employing a 2-alkylsulfonyl-3-phenylcyclopropane carboxamide as a P3 amino acid replacement
TBA
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
Abbott Laboratories
An overview of anti-SARS-CoV-2 and anti-inflammatory potential of baicalein and its metabolite baicalin: Insights into molecular mechanisms.
Tripura University
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Merck Research Laboratories
Side Chain Cyclized Aromatic Amino Acids: Great Tools as Local Constraints in Peptide and Peptidomimetic Design.
Vrije Universiteit Brussel
A concise review of recent advances in anti-heart failure targets and its small molecules inhibitors in recent years.
University of Electronic Science and Technology of China
Discovery of Novel 2-Carbamoyl Morpholine Derivatives as Highly Potent and Orally Active Direct Renin Inhibitors.
Mitsubishi Tanabe Pharma
Discovery of SPH3127: A Novel, Highly Potent, and Orally Active Direct Renin Inhibitor.
Mitsubishi Tanabe Pharma
Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors.
Pfizer
Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors.
Pfizer
Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema.
Kalvista Pharmaceuticals
Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of
Ucb
Re-emerging Aspartic Protease Targets: Examining
Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences
The discovery of structurally novel CCR1 antagonists derived from a hydroxyethylene peptide isostere template.
Pfizer
Rational design and synthesis of selective BACE-1 inhibitors.
Merck Research Laboratories
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Novartis Institutes For Biomedical Research
Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules.
Annamalai University
Piperidine-renin inhibitors compounds with improved physicochemical properties.
F. Hoffmann-La Roche
Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.
F. Hoffmann-La Roche
Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
TBA
Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3- [[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-L-alanine amide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (A-725
Abbott Laboratories
Studies directed toward the design of orally active renin inhibitors. 1. Some factors influencing the absorption of small peptides.
Abbott Laboratories
Specificity in the binding of inhibitors to the active site of human/primate aspartic proteinases: analysis of P2-P1-P1'-P2' variation.
University of Florida
Analyses of ligand binding in five endothiapepsin crystal complexes and their use in the design and evaluation of novel renin inhibitors.
Warner-Lambert
Nonpeptide renin inhibitors with good intraduodenal bioavailability and efficacy in dog.
Abbott Laboratories
Time-resolved ligand exchange reactions: kinetic models for competitive inhibitors with recombinant human renin.
Boehringer Ingelheim Pharmaceuticals
alpha-Hydroxy phosphinyl-based inhibitors of human renin.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis of analogues of the carboxyl protease inhibitor pepstatin. Effects of structure on inhibition of pepsin and renin.
TBA
Inhibition of renin by substrate analogue inhibitors containing the olefinic amino acid 5(S)-amino-7-methyl-3(E)-octenoic acid.
TBA
Pepstatin-derived inhibitors of aspartic proteinases. A close look at an apparent transition-state analogue inhibitor.
TBA
Renin inhibitors based on novel dipeptide analogues. Incorporation of the dehydrohydroxyethylene isostere at the scissile bond.
Abbott Laboratories
Renin inhibitors. Statine-containing tetrapeptides with varied hydrophobic carboxy termini.
Merck Sharp & Dohme Research Laboratories
Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond.
Abbott Laboratories
Analysis of structure-activity relationships in renin substrate analogue inhibitory peptides.
TBA
Renin inhibitors. Design of angiotensinogen transition-state analogues containing novel. (2R,3R,4R,5S)-5-amino-3,4-dihydroxy-2-isopropyl-7-methyloctanoic acid.
TBA
New inhibitors of human renin that contain novel Leu-Val replacements. Examination of the P1 site.
Abbott Laboratories
Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogues of angiotensinogen.
Abbott Laboratories
Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability.
Abbott Laboratories
Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a dihydroxyethylene transition-state mimic at the scissile bond to impart greater inhibitory potency.
Abbott Laboratories
Synthesis and biological activity of some transition-state inhibitors of human renin.
Ciba-Geigy
New human renin inhibitors containing an unnatural amino acid, norstatine.
Kissei Pharmaceutical
Inhibition of porcine pepsin by two substrate analogues containing statine. The effect of histidine at the P2 subsite on the inhibition of aspartic proteinases.
University of Wisconsin
Renin inhibitors containing hydrophilic groups. Tetrapeptides with enhanced aqueous solubility and nanomolar potency.
Merck Sharp & Dohme Research Laboratories
Discovery of renin inhibitors containing a simple aspartate binding moiety that imparts reduced P450 inhibition.
Glaxosmithkline
Renin inhibitors. Synthesis of transition-state analogue inhibitors containing phosphorus acid derivatives at the scissile bond.
Ciba-Geigy Pharmaceuticals Division
Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites.
Warner-Lambert
Renin inhibitors based on dipeptide analogues. Incorporation of the hydroxyethylene isostere at the P2/P3 sites.
Abbott Laboratories
Inhibitors of human renin. Cyclic peptide analogues containing a D-Phe-Lys-D-Trp sequence.
Ici Pharmaceuticals Group
Thermodynamics of the interaction of inhibitors with the binding site of recombinant human renin.
Upjohn
Potent, low molecular weight renin inhibitors containing a C-terminal heterocycle: hydrogen bonding at the active site.
Abbott Laboratories
Discovery of benzimidazole derivatives as orally active renin inhibitors: Optimization of 3,5-disubstituted piperidine to improve pharmacokinetic profile.
Takeda Pharmaceutical
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 2. Synthesis, biological properties and molecular modeling of hydroxyethylene isostere derivatives.
Ici Pharmaceuticals Group
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 1. Synthesis and biological properties of alkyl alcohol and statine derivatives.
Ici Pharmaceuticals Group
New inhibitors of renin that contain novel phosphostatine Leu-Val replacements.
Abbott Laboratories
Design, synthesis and biological evaluation of renin inhibitors guided by simulated annealing of chemical potential simulations.
Bioleap
Renin inhibitory peptides. Incorporation of polar, hydrophilic end groups into an active renin inhibitory peptide template and their evaluation in a human renin infused rat model and in conscious sodium-depleted monkeys.
Upjohn
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 3.1 Synthesis and biological properties of aminodeoxystatine and difluorostatone derivatives.
Ici Pharmaceuticals Group
New inhibitors of human renin that contain novel replacements at the P2 site.
Warner-Lambert
Design and synthesis of P2-P1'-linked macrocyclic human renin inhibitors.
Merck Sharp and Dohme Research Laboratories
Renin inhibitors containing C-termini derived from mercaptoheterocycles.
Merck Sharp & Dohme Research Laboratories
C-terminal modifications of nonpeptide renin inhibitors: improved oral bioavailability via modification of physicochemical properties.
Abbott Laboratories
Nonpeptide renin inhibitors employing a novel 3-aza(or oxa)-2,4-dialkyl glutaric acid moiety as a P2/P3 amide bond replacement.
Abbott Laboratories
1,2,3-trisubstituted cyclopropanes as conformationally restricted peptide isosteres: application to the design and synthesis of novel renin inhibitors.
University of Texas
Synthesis and use of 3-amino-4-phenyl-2-piperidones and 4-amino-2-benzazepin-3-ones as conformationally restricted phenylalanine isosteres in renin inhibitors.
Merck Sharp and Dohme Research Laboratories
New modified heterocyclic phenylalanine derivatives. Incorporation into potent inhibitors of human renin.
Wyeth-Ayerst Research
Inhibitors of human renin with C-termini derived from amides and esters of alpha-mercaptoalkanoic acids.
Merck Research Laboratories
Renin inhibitors containing new P1-P1' dipeptide mimetics with heterocycles in P1'.
E. Merck Darmstadt
PYRAZOLO[3,4-D]PYRIMIDIN-6-YL-SULFONAMIDE DERIVATIVES FOR THE INHIBITION OF SGK-1
Thryv Therapeutics
Substituted N-bicyclo-2-aryl-quinolin-4-carboxamides and use thereof
Bayer Pharma Aktiengesellschaft
Synthesis and preliminary biological assay of uridine glycoconjugate derivatives containing amide and/or 1,2,3-triazole linkers.
Silesian University of Technology
Modulation of [35S]TBPS binding by ligands with preferential affinity for benzodiazepine BZ1 sites in the cerebral cortex of newborn and adult rats.
University of Cagliari
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
National Health Research Institutes
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.
Hoffmann-La Roche
Identification of selective inhibitors of cyclin dependent kinase 4.
Dupont Pharmaceuticals