PMID
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Article Title
Organization
The design and synthesis of orally active short duration spiroindane growth hormone secretagogues

TBA
Selection, synthesis, and anti-inflammatory evaluation of the arylidene malonate derivatives as TLR4 signaling inhibitors.

University of Colorado At Boulder
Practical synthesis of bredemolic acid, a natural inhibitor of glycogen phosphorylase.

China Pharmaceutical University
Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.

Merck Research Laboratories
GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a.

Merck Research Laboratories
Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists.

Merck Research Laboratories
Development ofß-amino alcohol derivatives that inhibit Toll-like receptor 4 mediated inflammatory response as potential antiseptics.

University of Colorado At Boulder
Probes for narcotic receptor mediated phenomena. Part 42: synthesis and in vitro pharmacological characterization of the N-methyl and N-phenethyl analogues of the racemic ortho-c and para-c oxide-bridged phenylmorphans.

National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
Probes for narcotic receptor mediated phenomena. 43. Synthesis of the ortho-a and para-a, and improved synthesis and optical resolution of the ortho-b and para-b oxide-bridged phenylmorphans: compounds with moderate to low opioid-receptor affinity.

National Institute On Drug Abuse and The National Institute On Alcohol Abuse and Alcoholism
Identification of pentacyclic triterpenes derivatives as potent inhibitors against glycogen phosphorylase based on 3D-QSAR studies.

Chinese Academy of Sciences
Probes for narcotic receptor mediated phenomena. 41. Unusual inverseµ-agonists and potentµ-opioid antagonists by modification of the N-substituent in enantiomeric 5-(3-hydroxyphenyl)morphans.

National Institute On Drug Abuse
Synthesis, biological evaluation, and molecular docking studies of 2-chloropyridine derivatives possessing 1,3,4-oxadiazole moiety as potential antitumor agents.

Nanjing University
GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.

Merck Research Laboratories
Anthranilic acid replacements in a niacin receptor agonist.

Merck
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.

Merck Research Laboratories
Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumor agents.

Nanjing University
Discovery of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (nelotanserin) and related 5-hydroxytryptamine2A inverse agonists for the treatment of insomnia.

Arena Pharmaceuticals
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.

Merck Research Laboratories
Molecular modeling aided design of nicotinic acid receptor GPR109A agonists.

Merck Research Laboratories
3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.

Arena Pharmaceuticals
Research progress on GPX4 targeted compounds.

Peking University
Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.

Merck Research Laboratories
Heterocyclic-Modified Imidazoquinoline Derivatives: Selective TLR7 Agonist Regulates Tumor Microenvironment against Melanoma.

Southern Medical University
Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.

National Institute On Drug Abuse
Pyrazolone derivatives as potent and selective small-molecule SIRT5 inhibitors.

University of Michigan
Discovery of an ellipticine derivative as TLR3 inhibitor against influenza A virus and SARS-CoV-2.

Southern Medical University
Design, synthesis and bioactivity evaluation of a series of quinazolinone derivatives as potent PI3Kγ antagonist.

Southern Medical University
Potential treatment methods targeting 2019-nCoV infection.

Southern Medical University
Discovery of Cyclic Peptide Inhibitors Targeting PD-L1 for Cancer Immunotherapy.

University of Missouri-Kansas City
Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists.

Merck Research Laboratories
Design, Synthesis, and Structure-Activity Relationship of

Southern Medical University
Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists.

Merck
Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists.

Merck Research Laboratories
N-benzylpiperidinol derivatives as novel USP7 inhibitors: Structure-activity relationships and X-ray crystallographic studies.

China Pharmaceutical University
2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.

Merck Research Laboratories
Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.

Merck Research Laboratories
Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus.

Merck Research Laboratories
Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists.

Merck Research Laboratories
Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists.

Merck Research Laboratories
2-(3,5-Dimethylphenyl)tryptamine derivatives that bind to the GnRH receptor.

Merck Research Laboratories
A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor.

Merck Research Laboratories
SAR studies of novel 5-substituted 2-arylindoles as nonpeptidyl GnRH receptor antagonists.

Merck Research Laboratories
Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles.

Merck Research Laboratories
Nipecotic and iso-nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists.

Merck Research Laboratories
Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents.

Merck Research Laboratories
Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides.

Merck Research Laboratories
Design, synthesis and biological evaluation of novel human monoamine oxidase B inhibitors based on a fragment in an X-ray crystal structure.

Hefei University of Technology
Investigation of the 4-O-alkylamine substituent of non-peptide quinolone GnRH receptor antagonists.

Merck Research Laboratories
Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist.

Merck Research Laboratories
Structure-activity relationship study and biological evaluation of SAC-Garlic acid conjugates as novel anti-inflammatory agents.

Southern Medical University
A new lateral root growth inhibitor from the sponge-derived fungus Aspergillus sp. LS45.

Ningbo University
Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.

Merck Research Laboratories
Potent 3-spiropiperidine growth hormone secretagogues.

Merck Research Laboratories
Synthesis of urea analogues bearing N-alkyl-N'-(thiophen-2-yl) scaffold and evaluation of their innate immune response to toll-like receptors.

Southern Medical University
Discovery of novel 2,3-dihydro-1H-inden-1-amine derivatives as selective monoamine oxidase B inhibitors.

Hefei University of Technology
Synthesis, molecular modeling and biological evaluation of PSB as targeted antibiotics.

Nanjing University
Synthesis, antibacterial activities and molecular docking studies of peptide and Schiff bases as targeted antibiotics.

Nanjing University
The selectivity and bioavailability improvement of novel oral anticoagulants: An overview.

Hefei University of Technology
Discovery of novel small molecule TLR4 inhibitors as potent anti-inflammatory agents.

School of Pharmaceutical Sciences
Design, synthesis and bioevalucation of novel 2,3-dihydro-1H-inden-1-amine derivatives as potent and selective human monoamine oxidase B inhibitors based on rasagiline.

Hefei University of Technology
Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold.

Hefei University of Technology
Pyrazolyl-substituted heteroaryls and their use as medicaments

Boehringer Ingelheim International
Scaffold hopping, synthesis and structure-activity relationships of 5,6-diaryl-pyrazine-2-amide derivatives: a novel series of CB1 receptor antagonists.

Astrazeneca
Terphenyl-Based Bak BH3 alpha-helical proteomimetics as low-molecular-weight antagonists of Bcl-xL.

Yale University
HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.

Merck Research Laboratories