Synthesis of derivatives of methyl rosmarinate and their inhibitory activities against matrix metalloproteinase-1 (MMP-1)
Keywords: MMP-1; Inhibitors; SAR
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Design, synthesis and SAR of piperidyl-oxadiazoles as 11β-hydroxysteroid dehydrogenase 1 inhibitors
Keywords: 11β-HSD1 inhibitor; Oxadiazole; Bioisostere; SAR; Docking
A structure–activity relationship study of 1,2,4-triazolo[1,5-a][1,3,5]triazin-5,7-dione and its 5-thioxo analogues on anti-thymidine phosphorylase and associated anti-angiogenic activities
Keywords: 1,2,4-Triazolo[1,5-a][1,3,5]triazine; Thymidine phosphorylase inhibitors; SAR; Mixed-type inhibition; Breast cancer; Anti-angiogenesisKVEUPOJZRTUXSE-UHFFFAOYSA-N; NDFXXVAZVMLCPA-UHFFFAOYSA-N; HEEUTQZCYUHGBE-UHFFFAOYSA-N
Optical and SAR sensor synergies for forest and land cover mapping in a tropical site in West Africa
Keywords: Classification; West Africa; Forests; SAR; Landsat; AVNIR-2; Texture
Deriving surface motion of mountain glaciers in the Tuomuer-Khan Tengri Mountain Ranges from PALSAR images
Keywords: SAR; Glacier; Velocity; Offset-tracking; Snowline
Spatial and temporal variability of winds in the Northern European Seas
Keywords: Offshore wind energy; Satellite remote sensing; QuikSCAT; WRF; SAR; In situ measurements
Optimizing ACS NSQIP Modeling for Evaluation of Surgical Quality and Risk: Patient Risk Adjustment, Procedure Mix Adjustment, Shrinkage Adjustment, and Surgical Focus
Keywords: ACS; American College of Surgeons; CPT; Current Procedural Terminology; O/E; observed to expected ratio; OR; odds ratio; SAR; semi-annual report; VA; Veterans Affairs; VASQIP; Veterans Affairs Surgical Quality Improvement Program;
Hydrogen-bond effect, spectroscopic and molecular structure investigation of sulfamethazine Schiff-base: Experimental and quantum chemical calculations
Keywords: Sulfamethazine; TD-DFT; Hydrogen bond; NBO; MEP; SAR
Synthesis of novel cognition enhancers with pyrazolo[5,1-c][1,2,4]benzotriazine core acting at γ-aminobutyric acid type A (GABAA) receptor
Keywords: α7nACh-R; α7nicotinic acetylcoline receptor; AD; Alzheimer's disease; BMS; borane methylsulfide; Bz site/GABAA-R; benzodiazepine site on GABAA receptor; CMC; carboxymethylcellulose; CNS; central nervous system; DAZ; diazepam, 7-chloro-1-methyl-5-pheny
Cytotoxicity of lapachol, β-lapachone and related synthetic 1,4-naphthoquinones against oesophageal cancer cells
Keywords: Naphthoquinones; Cytotoxicity; SAR; Oesophageal cancer cell line WHCO1
Design, synthesis, and biological evaluation of novel 2-ethyl-5-phenylthiazole-4-carboxamide derivatives as protein tyrosine phosphatase 1B inhibitors with improved cellular efficacy
Keywords: Protein tyrosine phosphatase 1B; Type 2 diabetes; 2-Ethyl-5-phenylthiazole-4-carboxamide (PTA); SAR
Evaluation of polarimetric Radarsat-2 SAR data for development of soil moisture retrieval algorithms over a chronosequence of black spruce boreal forests
Keywords: Polarimetric radar; SAR; Polarimetric decomposition; Polarimetric discriminators; Soil moisture; Boreal; Fuel moisture; Black spruce; Picea mariana
A proof-of-concept study of the effect of a novel H3-receptor antagonist in allergen-induced nasal congestion
Keywords: Allergic rhinitis; acoustic rhinometry; environmental exposure chamber; H3-receptor antagonist; JNJ-39220675; pseudoephedrine; total nasal symptom scores; AcR; Acoustic rhinometry; AUC; Area under the curve; CNS; Central nervous system; ECP; Eosinophil ca
Synthesis, pharmacological evaluation and QSAR modeling of mono-substituted 4-phenylpiperidines and 4-phenylpiperazines
Keywords: In vivo; In vitro; Dopamine; DOPAC; D2; MAO A; SAR; QSAR(Q)SAR, (quantitative) structure–activity relationship; DOPAC, 3,4-dihydroxyphenylacetic acid; DA, dopamine; MAO, monoamine oxidase; GPCR, G-protein-coupled seven transmembrane receptor; PLS, partial
Assessment of number and distribution of persistent scatterers prior to radar acquisition using open access land cover and topographical data
Keywords: Radar; SAR; Prediction; GIS; Persistent scatterer processing
Short-term glacier velocity changes at West Kunlun Shan, Northwest Tibet, detected by Synthetic Aperture Radar data
Keywords: Glacier velocity; West Kunlun Shan; Surge; SAR; PALSAR
Species-area relationships underestimate extinction rates
Keywords: Island biogeography; Conservation biogeography; Habitat loss; Power function; SAR; Species extinction
Riccardin C derivatives as anti-MRSA agents: Structure-activity relationship of a series of hydroxylated bis(bibenzyl)s
Keywords: Bis(bibenzyl); Riccardin; Anti-MRSA; SAR;
Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism
Keywords: CRTH2; DP; PGD2; GPCR; Antagonist; Asthma; Allergic diseases; Lead optimization; SAR;
Synthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists
Keywords: Histamine; H3 antagonists; SAR; 4-Azabenzoxazole;
Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists
Keywords: CRTH2; DP; PGD2; GPCR; Dual Antagonist; SAR; Asthma
Discovery of thiadiazole amides as potent, S1P3-sparing agonists of sphingosine-1-phosphate 1 (S1P1) receptor
Keywords: S1P1 receptor agonists; Thiadiazole amides; SAR; Multiple sclerosis (MS)
Discovery of a new binding mode for a series of liver X receptor agonists
Keywords: LXR; Agonist; Nuclear receptor; SAR; Pyrrole
Synthesis, biological evaluation and SAR studies of benzimidazole derivatives as H1-antihistamine agents
Keywords: Benzimidazole derivatives; Antihistamine activity; SAR; Anti-PAF activity; hERG
Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists
Keywords: Sphingosine-1-phosphate; Agonist; Lymphopenia; Experimental autoimmune encephalomyelitis (EAE); SAR
Design and synthesis of small molecular dual inhibitor of falcipain-2 and dihydrofolate reductase as antimalarial agent
Keywords: Falcipain-2; Dihydrofolate reductase; Dual inhibitor; Antimalarial drug; SAR; Molecular docking;
Design, synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N1-arylsulfonyl indole derivatives as 5-HT6 receptor ligands
Keywords: 5-HT6R ligands; Cognitive impairment; SAR; Cross selectivity; PK profile; ORT;
Small molecule inhibitors of the HPV16-E6 interaction with caspase 8
Keywords: HPV; human papillomavirus; TNF R1; tumor necrosis factor receptor 1; FADD; fas-associated protein with death domain; TRAIL; TNF-related apoptosis-inducing ligand protein; TRADD; tumor necrosis factor receptor type 1-associated death domain protein; TRAF;
Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei
Keywords: HAT; human African trypanosomiasis; VSG; variant surface glycoprotein; HDAC; histone deacetylases; DAC; deacetylases; SAR; Structure-activity relationship; Anti-parasitic activity; Trypanosoma brucei; Histone deacetylase inhibitors; Hydroxamic acids;
Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor
Keywords: GPCRs; HTS; APJ; Apelin; Cardiovascular disease; Antagonists; SAR;
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα
Keywords: Nuclear hormone receptor; Agonists; Drug discovery; Medicinal chemistry; SAR;
In search for new chemical entities as adenosine receptor ligands: Development of agents based on benzo-γ-pyrone skeleton
Keywords: Chromone carboxamides; Adenosine receptor ligands; SAR; ADME;
Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement
Keywords: Cathepsin S; Reversible covalent inhibitors; Triazole; SAR; Metabolic stability;
Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT2C agonists
Keywords: 5-HT2C agonists; Synthesis; SAR; Anti-obesity
Optimisation of imidazole compounds as selective TAAR1 agonists: Discovery of RO5073012
Keywords: AOHLEOYTKMSKPD-UHFFFAOYSA-N; NIRASHDWADNQJU-UHFFFAOYSA-NTAAR1 agonist; Trace amines; Imidazole; SAR
Epiminocyclohepta[b]indole analogs as 5-HT6 antagonists
Keywords: Serotonin; 5-HT6; SAR; Cognition; Weight loss
Identification of novel SAR properties of the Jak2 small molecule inhibitor G6: Significance of the para-hydroxyl orientation
Keywords: Jak2 tyrosine kinase; G6; Small molecule inhibitor; Stilbenoid; SAR
Synthesis and biological evaluation of deoxy-hematoxylin derivatives as a novel class of anti-HIV-1 agents
Keywords: Hematoxylin; SAR; HIV-1; Vpr
Design, synthesis and structure–activity relationships of 5-alkylaminolquinolines as a novel series of CRF1 receptor antagonists
Keywords: CRF; SAR; Pharmacophore; Stress; Depression
Alstiphyllanines I-O, ajmaline type alkaloids from Alstonia macrophylla showing vasorelaxant activity
Keywords: Indole alkaloids; Alstonia macrophylla; Alstiphyllanines I-O; Ajmaline type alkaloids; Vasorelaxant activity; Nitric oxide; VDCs; ROCs; SAR;
A three-step protocol for lead optimization: Quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors
Keywords: Three-step protocol; SAR; Conformation; MK2; TNFα; Non-ATP competitive; Inhibitor;
Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD)
Keywords: MMP-12; COPD; SAR; Dibenzofuran;
Adrenergic deficiency leads to impaired electrical conduction and increased arrhythmic potential in the embryonic mouse heart
Keywords: APX; Apex of ventricle; A-V; Atrioventricular; AVJ; Atrioventricular junction; Cx43; Connexin 43; Dbh; Dopamine β-hydroxylase; EPI; Epinephrine (adrenaline); Hcn4; Hyperpolarization-activated cyclic nucleotide-modulated channel isoform 4; ICA; Intrinsic
Synthesis and biological evaluation of 4,4-dimethyl lithocholic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B
Keywords: 4,4-Dimethyl lithocholic acids; Protein tyrosine phosphatase 1B; Inhibitor; SAR; Diabetes;
Recent advances in MRI technology: Implications for image quality and patient safety
Keywords: MRI; Magnets; Coils; Specific absorption rate; SAR; Peripheral nerve stimulation; PNS; Patient safety
Genome-wide comparative analysis of simple sequence coding repeats among 25 insect species
Keywords: SCR; single codon repeats; CPR; codon pair repeats; SAR; single amino acid repeats; APR; amino acid pair repeats; RSCU; relative synonymous codon usage; Syn; synonymous; Non-syn; non-synonymous; Dmel; Drosophila melanogaster; Dsim; Drosophila simulans; Ds
Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors
Keywords: HIV-1; NNRTIs; Piperidine; Triazine; AIDS; SAR
Structure–activity relationship and antitumor activity of thio-benzodiazepines as p53–MDM2 protein–protein interaction inhibitors
Keywords: p53–MDM2; Thio-benzodiazepine; SAR; Antitumor activity
Mapping evergreen forests in the Brazilian Amazon using MODIS and PALSAR 500-m mosaic imagery
Keywords: PALSAR/ALOS; MODIS; Radar; SAR; Amazonia; Brazil
A 5 MSps 13.25μW 8-bit SAR ADC with single-ended or differential input
Keywords: ADC; Ultra-low power; SAR; Single-ended to differential conversion