Keywords: ثبات متابولیک; Endomorphin-1 analogues; Metabolic stability; Analgesic activity;
مقالات ISI ثبات متابولیک (ترجمه نشده)
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Keywords: ثبات متابولیک; Mitochondrial function; Respiratory chain substrates; Lipid peroxidation; Reactive oxygen species; Metabolic stability;
Keywords: ثبات متابولیک; BBB; blood brain barrier; BK; bradykinin; Boc; t-butyloxycarbonyl; BR; bradykinin receptor; CNS; central nervous system; DALKD; [des-Arg10, Leu9]-kallidin; DIPEA; diisopropylethylamine; DMF; N,N-dimethylformamide; Dyn A; dynorphin A; Fmoc; fluorenylmethyl
Keywords: ثبات متابولیک; Griseofulvin analogues; Anticancer; Synthesis; Antifungal; Metabolic stability;
Keywords: ثبات متابولیک; Metabolic stability; Metabolic steady state; Cofactor balance; Cofactor turnover; Enzyme feedback control; Emergent property of metabolic network
Keywords: ثبات متابولیک; Reactive carbonyl; Ferroptosis; Covalent; Erastin; Metabolic stability;
Keywords: ثبات متابولیک; meso-Dihydroguaiaretic acid; Metabolic stability; Pharmacokinetics; CYP inhibition; CYP2E1;
Keywords: ثبات متابولیک; Aminothiazoles; Visceral leishmaniasis; Leishmania donovani; Metabolic stability; Pharmacokinetics
Keywords: ثبات متابولیک; G-protein coupled receptors; Orexin antagonists; CNS drug discovery; Metabolic stability; Structure-activity relationship studies;
First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain
Keywords: ثبات متابولیک; HIV-1 NNRTI; RDEA427; Carbonate prodrug; Anti-HIV activity; Metabolic stability;
Novel aromatic sulfonyl naphthalene-based boronates as 20S proteasome inhibitors
Keywords: ثبات متابولیک; TEA; triethylamine; THF; tetrahydrofuran; Py; pyridine; DIPEA; N,N-diisopropylethylamine; TBTU; 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate; DCM; dichloromethane; TPLM; (1R)-(S)-pinanediol-1-ammonium trifluoroacetate-3-methylbut
Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands
Keywords: ثبات متابولیک; Histamine H3 receptor; Histamine H3 receptor ligands; Non-imidazole histamine H3R ligands; Piperazine derivatives; Anticonvulsants; Pro-cognitives; Molecular docking; Metabolic stability; QOXOVGLCVCFFFR-UHFFFAOYSA-N; DWCLOFJVHUBMBQ-UHFFFAOYSA-N; AXSBUUREH
Synthesis, molecular structure, and metabolic stability of new series of N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1H-pyrazol-1-yl)amidine as potential anti-cancer agents
Keywords: ثبات متابولیک; Benzenesulfonamides; Anticancer activity; Molecular structures; Metabolic stability; Cell cycle flow cytometry analysis;
Toxicological safety evaluation of 3,3â²-diselenodipropionic acid (DSePA), a pharmacologically important derivative of selenocystine
Keywords: ثبات متابولیک; Acute toxicity; Mutagenicity; Ames test; Metabolic stability; S9 liver fraction; Cytotoxicity;
In-vitro metabolism, CYP profiling and metabolite identification of E- and Z- guggulsterone, a potent hypolipidmic agent
Keywords: ثبات متابولیک; 1-ABZT; 1-aminobenzotriazole; CYP450; cytochrome P450; HLM; human liver microsomes; IS; internal standard; LC-MS/MS; liquid chromatography-tandem mass spectrometry; NADPH; reduced form of nicotinamide adenine dinucleotide phosphate; HPLC; high-performan
Development of novel 2,4-bispyridyl thiophene-based compounds as highly potent and selective Dyrk1A inhibitors. Part I: Benzamide and benzylamide derivatives
Keywords: ثبات متابولیک; Dyrk1A; Alzheimer's disease; Bispyridyl thiophene amides; Selectivity; Metabolic stability;
Structural development of 1,2,3,4-tetrahydroisoquinoline-type positive allosteric modulators of prostacyclin receptor (IPPAMs) to improve metabolic stability, and investigation of metabolic fate
Keywords: ثبات متابولیک; Positive allosteric modulator; Metabolic stability; Metabolic fate; CYP P450;
Discovery of BMS-961955, an allosteric inhibitor of the hepatitis C virus NS5B polymerase
Keywords: ثبات متابولیک; HCV NS5B; Polymerase; Cyclopropyl-fused indolobenzazepine; Metabolic stability; Direct-acting antiviral agent; Antiviral agent;
Approaches to improve metabolic stability of a statine-based GRP receptor antagonist
Keywords: ثبات متابولیک; Gastrin-releasing peptide receptor antagonists; Metabolic stability; 68Ga; PET-imaging;
Structure-activity relationship studies on 1-(2-oxopropyl)indole-5-carboxylic acids acting as inhibitors of cytosolic phospholipase A2α: Effect of substituents at the indole 3-position on activity, solubility, and metabolic stability
Keywords: ثبات متابولیک; Cytosolic phospholipase A2α; Inhibitors; Indole derivatives; Metabolic stability; Ketone reduction; Glucuronidation; Aqueous solubility;
Partially fluorinated alkoxy groups â Conformational adaptors to changing environments
Keywords: ثبات متابولیک; 5-Alkoxyindoles; Fluorinated alkoxy groups; Lipophilicity; Metabolic stability; Bond vector model; X-ray structures; Conformations;
Novel 2-benzylthio-5-(1,3,4-oxadiazol-2-yl)benzenesulfonamides with anticancer activity: Synthesis, QSAR study, and metabolic stability
Keywords: ثبات متابولیک; 2-Mercaptobenzenesulfonamide; Synthesis; 1,3,4-Oxadiazole; Anticancer activity; QSAR; Metabolic stability; RXWMIDCHADMLTA-UHFFFAOYSA-N; NYKXLLRMQVSYSI-UHFFFAOYSA-N; KIOPAJUWSSWZNF-UHFFFAOYSA-N; NSSMUONXQDEUTA-UHFFFAOYSA-N; VULJIZVBMIZUKD-UHFFFAOYSA-N; JHA
Novel 2-(2-alkylthiobenzenesulfonyl)-3-(phenylprop-2-ynylideneamino)guanidine derivatives as potent anticancer agents - Synthesis, molecular structure, QSAR studies and metabolic stability
Keywords: ثبات متابولیک; Benzenesulfonamides; Synthesis; Anticancer activity; QSAR studies; Metabolic stability;
Identification of a novel 5-amino-3-(5-cyclopropylisoxazol-3-yl)-1-isopropyl-1H-pyrazole-4-carboxamide as a specific RET kinase inhibitor
Keywords: ثبات متابولیک; RET kinase; Metabolic stability; Specific inhibitor; 5-Aminopyrazole-4-carboxamide;
Discovery of 4-chloro-2-(2,4-dichloro-6-methylphenoxy)-1-methyl-7-(pentan-3-yl)-1H-benzimidazole, a novel CRF1 receptor antagonist
Keywords: ثبات متابولیک; CRF; corticotropin-releasing factor; HPA; hypothalamus-pituitary-adrenocortical; ACTH; adrenocorticotropic hormone; SAR; structureactivity-relationship; CDI; N,Nâ²-carbodiimidazole; WSC; 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride; HOBt;
1-Heteroarylpropan-2-ones as inhibitors of fatty acid amide hydrolase: Studies on structure-activity relationships and metabolic stability
Keywords: ثبات متابولیک; Propan-2-one; Fatty acid amide hydrolase; Enzyme inhibition; Metabolic stability; Aqueous solubility;
Sulfoximines from a Medicinal Chemist's Perspective: Physicochemical and in vitro Parameters Relevant for Drug Discovery
Keywords: ثبات متابولیک; Synthesis; Sulfoximines; Sulfondiimides; Sulfonimidamides; Metabolic stability; Permeability; Solubility;
Design, synthesis, and pharmacological evaluation of 4-azolyl-benzamide derivatives as novel GPR52 agonists
Keywords: ثبات متابولیک; SAR; structure-activity relationship; cAMP; 3â²,5â²-cyclic adenosine monophosphate; EC50; half maximal effective concentration; MAP; methamphetamine; NMDA; N-methyl-d-aspartate; PK; pharmacokinetic; CHO; Chinese hamster ovary; SEM; standard error of t
α-Aryl pyrrolidine sulfonamides as TRPA1 antagonists
Keywords: ثبات متابولیک; TRPA1; Metabolic stability; Ion channel;
1,4-Diazepane compounds as potent and selective CB2 agonists: Optimization of metabolic stability
Keywords: ثبات متابولیک; Cannabinoid receptor; CB2; 1,4-Diazepane; Metabolic stability
Explorative study on the anticancer activity, selectivity and metabolic stability of related analogs of aminosteroid RM-133
Keywords: ثبات متابولیک; Steroid; Anticancer agent; Selective cytotoxicity; Metabolic stability; Drug;
Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold
Keywords: ثبات متابولیک; GPR40; Free fatty acid receptor 1; FFA1 agonists; Bioisosteric replacement; Total polar surface area; c Log P; Metabolic stability; Aqueous solubility
Structural modifications at the 6-position of thieno[2,3-d]pyrimidines and their effects on potency at FLT3 for treatment of acute myeloid leukemia
Keywords: ثبات متابولیک; Fms-like tyrosine kinase 3 (FLT3); Acute myeloid leukemia (AML); Thieno[2,3-d]pyrimidine; Metabolic stability;
Synthesis of novel amide and urea derivatives of thiazol-2-ethylamines and their activity against Trypanosoma brucei rhodesiense
Keywords: ثبات متابولیک; Thiazole; Amide; Urea; Antitrypanosomal; Metabolic stability;
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents
Keywords: ثبات متابولیک; VGGMLGZQRUZPAC-HQKYYOGZSA-N; SORDYQMTTXQNIQ-CQSZACIVSA-NAminoalkanols; Anticonvulsant activity; Seizures; Sigma receptors; 5-HT; MES; Metabolic stability; Mutagenicity; Vibrio harveyi; Pharmacokinetics
Discovery of small-molecule nonpeptide antagonists of nociceptin/orphanin FQ receptor: The studies of design, synthesis, and structure–activity relationships for (4-arylpiperidine substituted-methyl)-[bicyclic (hetero)cycloalkanobenzene] derivatives
Keywords: ثبات متابولیک; Nociceptin/Orphanin FQ (N/OFQ); Human NOP (ORL1) receptor selective antagonist; Multisite interactions with NOP receptor; Metabolic stability; HERG potassium ion channel binding; Prolong QT interval issuesGPCR, G-protein-coupled receptor; N/OFQ, nocicepti
Free fatty acid receptor 1 (GPR40) agonists containing spirocyclic periphery inspired by LY2881835
Keywords: ثبات متابولیک; GPCR; GPR40; Free fatty acid receptor 1; FFA1 agonists; Type 2 diabetes mellitus; Prins reaction; Spirocyclic motifs; Metabolic stability;
Design, synthesis and biological evaluation of LpxC inhibitors with novel hydrophilic terminus
Keywords: ثبات متابولیک; LpxC; CHIR-090; Kojic acid derivatives; Methylsulfone derivatives; Metabolic stability
Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability
Keywords: ثبات متابولیک; Metabotropic glutamate receptor subtype 4 (mGlu4); Positive allosteric modulator (PAM); Positron emission tomography (PET); Affinity; Metabolic stability; Structure–affinity relationship (SAR)
Selective CB2 receptor agonists. Part 2: Structure–activity relationship studies and optimization of proline-based compounds
Keywords: ثبات متابولیک; KRHYYFGTRYWZRS-UHFFFAOYSA-N; SNQTVUXJKJMYRL-ZDUSSCGKSA-NCannabinoid receptor 2 (CB2); Proline; Metabolic stability; Solubility; Pharmacokinetic properties
Selective CB2 receptor agonists. Part 3: The optimization of a piperidine-based series that demonstrated efficacy in an in vivo neuropathic pain model
Keywords: ثبات متابولیک; Cannabinoid receptor; CB2; CB1; Piperidine; Metabolic stability; Solubility
Discovery of novel S1P2 antagonists. Part 2: Improving the profile of a series of 1,3-bis(aryloxy)benzene derivatives
Keywords: ثبات متابولیک; PZFBUIYFAFMDBM-UHFFFAOYSA-N; Sphingosine-1-phosphate receptor 2; Antagonist; G protein-coupled receptors; Metabolic stability;
Synthesis and biological evaluation of picolinamides as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)
Keywords: ثبات متابولیک; 11β-HSD1 inhibitor; Diabetes; Metabolic syndrome; Picolinamide; Metabolic stability
Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2
Keywords: ثبات متابولیک; Orexin receptors; Dual orexin receptor antagonists; Selective orexin-2 receptor antagonists; Sleep; CNS drug discovery; Metabolic stability
In Vitro Evaluation of the Effect of 7-Methyl Substitution on Glucuronidation of Daphnetin: Metabolic Stability, Isoform Selectivity, and Bioactivity Analysis
Keywords: ثبات متابولیک; daphnetin; glucuronidation; methyl substitution; structural modification; metabolic stability; phase II enzymes; glucuronosyl-transferases; human liver microsomes; enzyme kinetics; metabolic clearance;
Discovery of novel purine-based heterocyclic P2X7 receptor antagonists
Keywords: ثبات متابولیک; Human P2X7R; Antagonists; Ethidium bromide uptake; IL-1β; Metabolic stability;
Identification of 2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide (29) as an orally available MGAT2 inhibitor
Keywords: ثبات متابولیک; MGAT2; monoacylglycerol acyltransferase 2; TG; triglyceride; FeSSIF; Fed State Simulated intestinal Fluid; MS; metabolic stability; TFAA; trifluoroacetic anhydride; EDC·HCl; 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride; HOBt·H2O; 1-hydrox
Determination of species-difference in microsomal metabolism of amitriptyline using a predictive MRM-IDA-EPI method
Keywords: ثبات متابولیک; Amitriptyline; CYP; UGT; Metabolic stability; Metabolite identification;
Novel endomorphin-1 analogs with C-terminal oligoarginine-conjugation display systemic antinociceptive activity with less gastrointestinal side effects
Keywords: ثبات متابولیک; Endomorphin-1 analogs; Metabolic stability; Peripheral administration; Antinociception; Gastrointestinal effect
Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2
Keywords: ثبات متابولیک; Formyl peptide receptor; Ureidopropanamide; Chiral agonist; Ca2+ mobilization; Neutrophil; Metabolic stability