Keywords: T-type calcium channel; 3,4-Dihydroquinazoline; Bioisostere; Cytotoxic activity; Inflammatory pain; Liver microsomal stability;
مقالات ISI (ترجمه نشده)
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Keywords: Perforin; Perforin inhibitor; Benzenesulphonamide; Bioisostere; Immunosuppressant;
Keywords: AR antagonist; Molecular modeling; Bioisostere; Nicotinamide; Pyrazinamide; Pyrimidinamide
Keywords: Azaspiro; MRSA (methicillin-resistant Staphylococcus aureus); Bioisostere; Morpholine; Antibacterial; Antitubercular; VRE (vancomycin-resistant enterococci)
Keywords: Silicon; Bioisostere; Silacyclohexane; Silacyclopentane; Silacycloalkane;
Keywords: AtKAPAS; Herbicide; Toxicity; Plumbagin; Bioisostere; Virtual screening
Keywords: Protoberberine; Bioisostere; 5-Oxaprotoberberinium; 5-Oxaprotberberin-8-one;
Keywords: 1,5-Diarylpyrazoles; Bioisostere; Carbothioamide; Sulfonamide; Anti-inflammatory activity; Cyclooxygenase inhibitors; Inflammation; NSAIDs;
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition
Keywords: 3-(Sulfonyl)-1,2,4-triazole; Triazolesulfone; Bioisostere; Acylsulfonamide; pKa; Sodium channel; NaV1.7; NaV1.5; Pain;
Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors
Keywords: Diabetes; Glucose transporter; SGLT1 inhibitor; SGLT2 inhibitor; Bioisostere; C-Aryl glucoside; QUHJWCHBJBZVQP-IDYLKPADSA-N; BILUNNIHYDMSKS-MJALHYBGSA-N; BSBHQOFIMOUJAR-MDBOPMCTSA-N; CADHWTGZCAYZEA-IDYLKPADSA-N; ADOHIJAAUMSPIL-MJALHYBGSA-N; QMNFASCAEVCTBD
Assessment of the effective dose of an experimental intramuscular formulation against immature and adult Fasciola hepatica in sheep
Keywords: Fasciola hepatica; Experimental water-soluble prodrug compound alpha; bioisostere; anthelmintics;
Squarate-based carbocyclic nucleosides: Syntheses, computational analyses and anticancer/antiviral evaluation
Keywords: Squaric acid; Carbocyclic; Nucleoside; Anticancer; Antiviral; Bioisostere;
Synthesis and evaluation of sulfonamide derivatives as potent Human Uric Acid Transporter 1 (hURAT1) inhibitors
Keywords: hURAT1 inhibitor; Bioisostere; Sulfonamide; Structure-activity relationship; Pharmacokinetic studies; Gout disease;
Substituted arylsulphonamides as inhibitors of perforin-mediated lysis
Keywords: Perforin; Perforin inhibitor; Arylsulphonamide; Bioisostere; Immunosuppressant;
Discovery of benzamides as potent human β3 adrenergic receptor agonists
Keywords: β3 adrenergic receptor agonist; Reverse amide; Pyrrolidine scaffold; Bioisostere; Overactive bladder
New small molecule inhibitors of histone methyl transferase DOT1L with a nitrile as a non-traditional replacement for heavy halogen atoms
Keywords: Protein methyltransferase; DOT1L inhibitors; Toyocamycin; Bioisostere; Cyano-deaza-SAH
Pyrazolo[3,4-d]pyrimidine based scaffold derivatives targeting kinases as anticancer agents
Keywords: Protein kinase; Bioisostere; Pyrazolo[3,4-d]pyrimidine; Synthetic strategy; SAR
Medicinal attributes of pyrazolo[1,5-a]pyrimidine based scaffold derivatives targeting kinases as anticancer agents
Keywords: Protein kinase; Bioisostere; Pyrazolo[1,5-a]pyrimidine; Anticancer;
Replacement of amide with bioisosteres led to a new series of potent adenosine A2A receptor antagonists
Keywords: Bioisostere; Adenosine receptor; Antagonist; GPCR; Parkinson's disease;
O-Alkylation of 3-hydroxyisoxazoles predominates under Mitsunobu conditions
Keywords: Mitsunobu reaction; 3-Hydroxyisoxazole, 3-isoxazolol, isoxazole-3-one; Ambident (pro-)nucleophile; Regioselective; Bioisostere;
2-Aminopyrimidin-4(1H)-one as the novel bioisostere of urea: Discovery of novel and potent CXCR2 antagonists
Keywords: 2-Aminopyrimidin-4(1H)-one; Bioisostere; Urea; CXCR2 antagonists;
Discovery of 3-(trifluoromethyl)-1H-pyrazole-5-carboxamide activators of the M2 isoform of pyruvate kinase (PKM2)
Keywords: Pyruvate kinase M2; PKM2 activator; 3-(Trifluoromethyl)-1H-pyrazole-5-carboxamides; Bioisostere; Cancer metabolism;
Efficient synthesis of 1,3,4-oxadiazoles promoted by NH4Cl
Keywords: 1,3,4-Oxadiazole; Ammonium chloride; Heterocycle synthesis; Bioisostere;
Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists
Keywords: TGR5; Pyrimidine; Malonamide; Agonist; Bioisostere;
Synthesis and pharmacological characterization of new neuronal nicotinic acetylcholine receptor ligands derived from Sazetidine-A
Keywords: Sazetidine A; nAChR α4β2; Nicotinic receptor; Click chemistry; Bioisostere; Biostere; Photoaffinity label;
Synthesis and pharmacological evaluation of 5-[2′-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-4,5,6,7-tetrahydro-thieno[3,2-c]pyridine derivatives as platelet aggregation inhibitors
Keywords: Antithrombotic activity; Bioisostere; In vitro; In vivo; Tetrazole; Platelet aggregation
Synthesis of 2-{2-[(α/β-naphthalen-1-ylsulfonyl)amino]-1,3-thiazol-4-yl} acetamides with 11β-hydroxysteroid dehydrogenase inhibition and in combo antidiabetic activities
Keywords: Diabetes; In silico; Thiazole; Sub-acute; Bioisostere;
Combination of 2-methoxy-3-phenylsulfonylaminobenzamide and 2-aminobenzothiazole to discover novel anticancer agents
Keywords: Benzamide; Benzothiazole; Synthesis; Anticancer effect; Bioisostere
Discovery of 2-methoxy-3-phenylsulfonamino-5-(quinazolin-6-yl or quinolin-6-yl)benzamides as novel PI3K inhibitors and anticancer agents by bioisostere
Keywords: Benzamide; Quinazoline; PI3K inhibitor; Antiproliferative activity; Anticancer effect; Bioisostere
4-Quinolone-3-carboxylic acids as cell-permeable inhibitors of protein tyrosine phosphatase 1B
Keywords: Protein tyrosine phosphatase 1B inhibitor; 4-Quinolone-3-carboxylic acid; Bidentate ligand; Bioisostere; Insulin receptor signaling
Discovery and optimization of novel small-molecule HIV-1 entry inhibitors using field-based virtual screening and bioisosteric replacement
Keywords: ADME; absorption, distribution, metabolism, and excretion; AMLV; amphotropic murine leukemia virus; BBB; blood-brain barrier; BIF; bioisostere factor; CNS; central nervous system; DCM; dichloromethane; DiEA; diisopropylethylamine; DIPEA; N,N-diisopropyl
Synthesis and structure-activity relationship of 2-arylamino-4-aryl-pyrimidines as potent PAK1 inhibitors
Keywords: PAK1 kinase; 2-Arylamino-4-aryl-pyrimidines; Colon cancer; Pak1 inhibitor; Bioisostere;
Retention of stereochemistry in the microwave assisted synthesis of 1H-tetrazole bioisosteric moiety from chiral phenyl-acetic acid derivatives
Keywords: Tetrazole synthesis; Retention of stereochemistry; Trimethylstannyl azide; Bioisostere; C5aR antagonists;
Potent MCH-1 receptor antagonists from cis-1,4-diaminocyclohexane-derived indane analogs
Keywords: GPCR; MCHR1 antagonist; Fragment; Bioisostere; Conformation;
Lead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation
Keywords: WZVLQVVHYKFKAZ-UHFFFAOYSA-NPI3K; Cancer; SBDD; Bioisostere; Glucuronic acid conjugation
Search for α3β2/3γ2 subtype selective ligands that are stable on human liver microsomes
Keywords: GABA; Benzodiazepines; Bioisostere; Anxiolytic
Design, synthesis and SAR of piperidyl-oxadiazoles as 11β-hydroxysteroid dehydrogenase 1 inhibitors
Keywords: 11β-HSD1 inhibitor; Oxadiazole; Bioisostere; SAR; Docking
The development of a new class of inhibitors for betaine-homocysteine S-methyltransferase
Keywords: BHMT; Inhibitor; Homocysteine; Phosphonate; Phosphinate; Amino acid derivative; Bioisostere; S-Alkylated homocysteineBHMT, betaine-homocysteine S-methyltransferase; Boc, tert-butoxycarbonyl; Boc2O, di-tert butyl dicarbonate; CDI, 1,1′-carbonyldiimidazole;
A novel 3,4-dihydropyrimidin-2(1H)-one: HIV-1 replication inhibitors with improved metabolic stability
Keywords: HIV; Inhibitor; 3,4-Dihydropyrimidin-2(1H)-one; Biginelli reaction; Bioisostere
Discovery of ITX 4520: A highly potent orally bioavailable hepatitis C virus entry inhibitor
Keywords: Hepatitis C virus; Entry inhibitors; Bioisostere; Oral bioavailability; Scavenger receptor B-1
Concise and divergent approach to 3-O-acyl-l-noviose derivatives and their 3-amino bioisosteres: 3-O-benzoyl-l-noviose and N-benzoyl-3-amino-l-noviose
Keywords: Aminocoumarin; 3-O-acyl-l-Noviose; Bioisostere;
2-Arylmethylaminomethyl-5,6-dihydroxychromone derivatives with selective anti-HCV activity
Keywords: 2-Arylmethylaminomethyl-5,6-dihydroxychromone; ADK (aryl diketoacid); Bioisostere; Hepatitis C virus (HCV)
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors
Keywords: Factor Xa inhibitor; Bioisostere; Valerolactam; Arylsulfonamide; Antithrombotic agent; X-ray crystal structure
Bioisostere of valtrate, anti-HIV principle by inhibition for nuclear export of Rev
Keywords: Valtrate; Rev-export inhibitor; Anti-HIV; Iridoid; Bioisostere
Discovery of novel (S)-α-phenyl-γ-amino butanamide containing CCR5 antagonists via functionality inversion approach
Keywords: CCR5 antagonist; HIV-1 entry inhibitor; Functionality inversion; Bioisostere; Butanamide; Tropane; 2-Methyl-3H-imidazo[4,5-b]pyridine; 3H-[1,2,3]Triazolo[4,5-b]pyridine
Design, synthesis and prostate cancer cell-based studies of analogs of the Rho/MKL1 transcriptional pathway inhibitor, CCG-1423
Keywords: Metastasis; RhoA; Prostate cancer; Serum response factor; Serum response element; Conformational restriction; Bioisostere
Synthesis of 3,5-disubstituted 1,2,4-oxadiazoles using ionic liquid-phase organic synthesis (IoLiPOS) methodology
Keywords: Ionic liquid; Liquid phase; 1,2,4-Oxadiazole; Bioisostere; O-acylamidoxime; Amidoxime;
Structure–activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists
Keywords: Androgen receptor; Pure antagonist; Prostate cancer; Bioisostere; Sulfonamide
The preparation of optically active α-amino 4H-[1,2,4]oxadiazol-5-ones from optically active α-amino acids
Keywords: Oxadiazolone; Bioisostere; Optically active; α-Amino acid;
17β-Nitro-5α-androstan-3α-ol and its 3β-methyl derivative: Neurosteroid analogs with potent anticonvulsant and anxiolytic activities
Keywords: Neurosteroid; Allopregnanolone; GABAA receptor; Anticonvulsant; Anxiolytic; Bioisostere