Keywords: Acac; acetylacetone; Ar; aryl; BDPP; 2,4-bis(diphenylphosphino)pentane; BINAP; 2,2â²-bis(diphenylphosphino)-1,1â²-binaphthyl; BINOL; 1,1â²-bi-2-naphthol; Bn; benzyl; Boc; tert-butoxycarbonyl; Bz; benzoyl; Cbz; benzyloxycarbonyl; Cy; cyclohexyl; DCE; 1,
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Synthesis, characterization, and application of a novel multifunctional stationary phase for hydrophilic interaction/reversed phase mixed-mode chromatography
Keywords: HPLC; High-Performance Liquid Chromatography; RPLC; Reversed-Phase Liquid Chromatography; HILIC; Hydrophilic Interaction Liquid Chromatography; DCC; Dicyclohexylcarbodiimide; HOBT; 1-Hydroxybenzotriazole hydrate; DCM; Dichloromethane; H; Hexane; EtOAc; Et
Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide
Keywords: OX1R; orexin 1 receptor; OX2R; orexin 2 receptor; DORA; dual orexin receptor antagonist; SORA; selective orexin receptor antagonist; SI; selectivity index; BBB; blood-brain barrier; CNS; central nervous system; SAR; structure-activity relationship; Boc; t
Keywords: Ac; acetyl; An; anisyl; Ar; aryl; ATP; adenosine triphosphate; Bn; benzyl; Boc; tert-butoxycarbonyl; Bu; butyl; Bz; benzoyl; cat; catalyst; conv; conversion; Cy; cyclohexyl; DABCO; 1,4-diazabicyclo[2.2.2]octane; DBU; 1,8-diazabicyclo[5.4.0]undec-7-ene; de
Recent developments in enantioselective lanthanide-catalyzed transformations
Keywords: Ar; aryl; BINOL; 1,1â²-bi-2-naphthol; Bpy; 2,2â²-bipyridyl; Bn; benzyl; BNP; Binaphthophosphole; Boc; tert-butoxycarbonyl; BSA; bis-(trimethylsilyl)acetamide; CB; carbon black; cod; 1,5-cyclooctadiene; Cy; cyclohexyl; DBDMH; 1,3-dibromo-5,5-dimethylhyda
Keywords: RNCGDQLZIATDOU-ZDRBWGSPSA-N; ICYPJNZJUFGALC-PDTBJYIYSA-N; PDRMAVOIWIVXKH-SFUSBHMVSA-N; ISADXJRTBSLWPX-ZDRBWGSPSA-N; NLBLLPROASDPSC-QWWZWVQMSA-N; XKMIKZDBUOHHDK-ZDRBWGSPSA-N; BTURADNXKHTWGA-IJOLSIAMSA-N; UEKHRDLXBMZMPD-ZYIYBEKCSA-N; UQCLCXDOXVZEOA-JARUQAPT
Keywords: Nitro compounds; Natural products; Pharmaceuticals; Stereoselective synthesis; Organocatalysis; Metal catalysis; Nitronates; Nitrile oxides; AIBN; azobisisobutyronitrile; AZADO; 2-azaadamantane-N-oxyl; 9-BBN; 9-borabicyclo[3.3.1]nonane; BINAP; 2,2â²-bis(
Keywords: Ac; acetyl; acac; acetylacetonate; AHPCS; allylhydridopolycarbosilane; Bn; benzyl; Boc; tert-butoxycarbonyl; BPR; back pressure regulator; bpy; 2,2â²-bipyridine; Bu; butyl; CFL; compact fluorescent lamp; DCB; 1,4-dicyanobenzene; de; diastereomeric excess
Keywords: AcOEt; ethyl acetate; Boc; tert-butoxycarbonyl; Boc2O; Boc anhydride; DCC; dicyclohexylcarbodiimide; DIAD; diisopropylazodicarboxylate; DMAP; 4-(N,N-dimethylamino)pyridine; DMF; N,N-dimethylformamide; PPh3; triphenylphosphine; tBu; tert-butyl; TEA; trieth
Keywords: NPJDMSUNRACWDA-SATBOSKTSA-N; PUWHCNIHRICNRN-QNPMOXIUSA-N; FZPRGLOMMOKQRW-FDCKWBIYSA-N; FZTSQIMWMZFAPH-AJEPLDCBSA-N; NSRMBSSIRRRDFQ-QIKUIUABSA-N; VNFRPOPUNVVQHM-STYNFMPRSA-N; XFUWVZUXFFLRLN-SCGPDRHWSA-N; UDZBOEHPHMLLMU-NXEZZACHSA-N; FFEGSQDYGFSWOX-DGCLKSJQ
Keywords: Diversity-oriented synthesis; Imidazoheterocyclic; Groebke-Blackburn-Bienayme reaction; Fused imidazole; Lewis acid; Ugi type; Ac; acetyl; Aq; aqueous; Ar; aryl; Bn; benzyl; Boc; tert-butoxycarbonyl; BDMS; bromodimethylsulfonium bromide; CDK; cyclin-d
Keywords: Methylenecyclopropanes; Alkylidenecyclopropanes; Cyclopropanes; Strained molecules; Synthesis; Reactivity; acac; acetylacetonate; Ad; adamantyl; AIBN; 2,2â²-azobisisobutyronitrile; Ar; aryl; Bn; benzyl; Boc; tert-butoxycarbonyl; Bppf; 9,9-bis[4-(pyrenyl)
Keywords: ACN; acetonitrile; AFM; atomic force microscopy; AIBN; 2,2â²-azobis-isobutyronitrile; APS; ammonium persulfate; AM; acrylamide; AML; amlodipine; ATRP; atom-transfer radical polymerization; BMA; butyl methacrylate; Boc; tert-butoxycarbonyl; Boc-Trp; tert-
Keywords: Chemoselectivity; Site selectivity; Stereoselectivity; Carbon-carbon bond-forming reactions; Transition metal catalyst; Ac; acetyl; Ar; aryl; Bn; benzyl; Boc; tert-butoxycarbonyl; n-Bu; n-butyl; t-Bu; tert-butyl; Cp; cyclopentadienyl; DABCO; 1,4-diazabi
Microcystins: Synthesis and structure-activity relationship studies toward PP1 and PP2A
Keywords: Adda; (2S,3S,8S,9S)-3-amino-9-methoxy-2,6,8-trimethyl-10-phenyldeca-4,6-dienoic acid; Amba; (2S,3S)-3-amino-2-methylbutanoic acid; Boc; tert-butoxycarbonyl; BOP; benzotriazol-1-yloxy-tris-dimethylaminophosphoniumhexafluoro phosphate; Cbz; carboxybenzyl; D
Synthesis of MOFs for heterogeneous catalysis via linker design
Keywords: MOFs; metal-organic frameworks; PCNs; porous coordination networks; PCPs; porous coordination polymers; PSM; post-synthetic modifications; SBUs; secondary building units; TCPP; tetrakis(4-carboxyphenyl)porphyrin); MMPF; metal-metalloporphyrin framework;
New insights about the peculiar role of the 28-38 C-terminal segment and some selected residues in PACAP for signaling and neuroprotection
Keywords: ACN; acetonitrile; BBB; bloodbrain barrier; Bip; biphenylalanine; Boc; tert-butoxycarbonyl; BOP; (benzotriazol-1-yloxy)tris(dimethylamino) phosphonium hexafluorophosphate; BRET; bioluminescence resonance energy transfer; CHO cells; Chinese hamster ovary c
Acylguanidine derivatives of zanamivir and oseltamivir: Potential orally available prodrugs against influenza viruses
Keywords: Acylguanidine; Zanamivir; Oseltamivir; Neuraminidase inhibitor; Influenza; Arg; arginine; Boc; tert-butoxycarbonyl; (Boc)2O; di(tert-butyl) dicarbonate; CC50; half maximal cytotoxicity concentration; CPE; cytopathic effect; DIEA; diisopropyl ethylamine; D
Cefiderocol (S-649266), A new siderophore cephalosporin exhibiting potent activities against Pseudomonas aeruginosa and other gram-negative pathogens including multi-drug resistant bacteria: Structure activity relationship
Keywords: Cefiderocol; Siderophore; Siderophore cephalosporin; Multi-drug resistant Gram-negative pathogens; ESBL; extended-spectrum β-lactamase; MDR; multi-drug resistant; PG; protecting group; ACLE·HCl; (7-amino-3-chloromethyl-3-cephem-4-carboxylate p-methoxybe
Synthesis of PET probe O6-[(3-[11C]methyl)benzyl]guanine by Pd0-mediated rapid C-[11C]methylation toward imaging DNA repair protein O6-methylguanine-DNA methyltransferase in glioblastoma
Keywords: MGMT; O6-methylguanine-DNA methyltransferase; TMZ; temozolomide; O6-BG; O6-benzylguanine; PET; positron emission tomography; AGT; O6-alkylguanine-DNA alkyltransferase; TFA; trifluoroacetyl; [11C]mMeBG; 11C-labeled O6-[(3-methyl)benzyl]guanine; BOC; tert-b
Synthesis and evaluation of analogs of 5â²-(((Z)-4-amino-2-butenyl)methylamino)-5â²-deoxyadenosine (MDL 73811, or AbeAdo) - An inhibitor of S-adenosylmethionine decarboxylase with antitrypanosomal activity
Keywords: AdoMet; S-adenosyl-l-methionine; AdoMetDC; S-adenosylmethionine decarboxylase; BBB; bloodbrain barrier; Boc; tert-butoxycarbonyl; BSA; N,O-bis(trimethylsilyl)acetamide; CNS; central nervous system; DEAD; diethyl azodicarboxylate; DIAD; diisopropyl azodica
Discovery and optimization of benzimidazole derivatives as a novel chemotype of farnesoid X receptor (FXR) antagonists
Keywords: FXR; farnesoid X receptor; CDCA; chenodeoxycholic acid; CYP7A1; cholesterol 7α-hydroxylase; SHP; small heterodimer partner; RXRα; retinoid X receptor α; 9-cis-RA; 9-cis-retinoic acid; LBD; ligand binding domain; TR-FRET; time-resolved fluorescence reso
Discovery of novel somatostatin receptor subtype 5 (SSTR5) antagonists: Pharmacological studies and design to improve pharmacokinetic profiles and human Ether-a-go-go-related gene (hERG) inhibition
Keywords: Boc; tert-butoxycarbonyl; Pd(OAc)2; palladium acetate; PBu3; tributylphosphine; DIBAL-H; diisobutylaluminum hydride; S-phos; 2-dicyclohexylphosphino-2â²,6â²-dimethoxybiphenyl; Pd2(dba)3; tris(dibenzylideneacetone) dipalladium; NaH; sodium hydride; LiAlH
Synthesis and biological activity of cyclolinopeptide A analogues modified with γ4-bis(homo-phenylalanine)
Keywords: Boc; tert-Butoxycarbonyl; C8; octyl stationary phase; C18; octadecyl stationary phase; CLA; cyclolinopeptide A; COSY-DQF; double quantum filtered proton spin correlation; CsA; cyclosporine A; DIPEA; N,N-diisopropylethylamine; DMF; dimethylformamide; DMSO;
Stereoselective synthesis of modified cysteines
Keywords: Alloc; allyloxycarbonyl; Ar; aryl; Bn; benzyl; Cbz; benzyloxycarbonyl; Cbz-OSu; benzyloxycarbonylsuccinimide; NBS; N-bromosuccinimide; Boc; tert-butoxycarbonyl; m-CPBA; m-chloroperbenzoic acid; DABCO; 1,4-diazabicyclo[2.2.2]octane; DBU; 1,8-diazabicyclo[5
Cobalt-based paramagnetic probe to study RNA-protein interactions by NMR
Keywords: NCp7; Nucleocapsid protein 7; HSQC; Heteronuclear single quantum coherence; PRE; Paramagnetic resonance enhancement; TLC; Thin layer chromatography; NMR; Nuclear magnetic resonance; RNA; Ribonucleic acid; A; Adenosine; C; Cytidine; U; Uridine; G; Guanosin
Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities
Keywords: Nek2 inhibitors; Imidazo[1,2-a]pyridine; Antitumor activity; Selectivity; Nek2; NIMA-related kinase 2; Nlp; ninein-like protein; SAC; spindle assembly checkpoint; Mad1/2; mitotic arrest deficient 1/2; Hec1; highly expressed in cancer 1; CIN; chromosome in
Synthesis of novel 15-membered 8a-azahomoerythromycin A acylides: Consequences of structural modification at the C-3 and C-6 position on antibacterial activity
Keywords: Macrolide antibiotics; Macrolide resistance; Acylides; Structure-activity relationships; Antibacterial activity; Heck reaction; MLSB; macrolide-lincosamide-streptogramin B; Mef; macrolide efflux; SAR; structure-activity relationships; DABCO; 1,4-diazabicy
Nanowires of indigo and isoindigo-based molecules with thermally removable groups
Keywords: Conjugated molecules; tert-butoxycarbonyl; Thermal cleavage; Hydrogen bonding; Nanowires; Organic field effect transistors;
An update on the stereoselective synthesis of γ-amino acids
Keywords: ABO; 2,7,8-trioxabicyclo[3.2.1]octane; Ac; acetyl; ACPECA; 4-aminocyclopent-2-ene-1-carboxylic acid; AHPPA; 4-amino-3-hydroxy-5-phenylpentanoic acid; AMCP; 2-(aminomethyl)-cyclopentanecarboxylic acid; APCH; 2-(1-aminopropyl)cyclohexanecarboxylic acid; APT
Achievement of regioselectivity in transition metal-catalyzed direct C-H (hetero)arylation reactions of heteroarenes with one heteroatom through the use of removable protecting/blocking substituents or traceless directing groups
Keywords: Chemoselectivity; Regioselectivity; Direct C-H (hetero)arylation; Transition metal catalysts; Removable groups; Traceless directing groups; Deprotection; Ac; acetyl; acac; acetylacetonate; 1-Ad; 1-adamantyl; AIBN; azobisisobutyronitrile; Ar; aryl; Boc;
Cyclen-based double-tailed lipids for DNA delivery: Synthesis and the effect of linking group structures
Keywords: Boc; tert-butoxycarbonyl; cyclen; 1, 4, 7, 10-tetraazacyclododecane; lipoplexes; liposome/DNA complexes; TE; gene transfection efficiency; EDC HCl; 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride; HOBt; 1-hydroxybenzotriazole; TFA; trifluoroac
Synthesis of a mixed-model stationary phase derived from glutamine for HPLC separation of structurally different biologically active compounds: HILIC and reversed-phase applications
Keywords: HPLC; high-performance liquid chromatography; RPLC; reversed-phase liquid chromatography; NPLC; normal-phase liquid chromatography; HILIC; hydrophilic interaction chromatography; DCC; dicyclohexylcarbodiimide; DCM; dichloromethane; H; hexane; EtOAc; ethyl
Novel benzidine and diaminofluorene prolinamide derivatives as potent hepatitis C virus NS5A inhibitors
Keywords: HCV; NS5A inhibitor; Benzidine; Diaminofluorene; Structure-activity relationship; HCV; hepatitis C virus; Peg-IFNα; pegylated interferon α; SVR; sustained virological response; GT1a; hepatitis C virus genotype 1a, a subtype of hepatitis C virus genoty
Binding cooperativity between a ligand carbonyl group and a hydrophobic side chain can be enhanced by additional H-bonds in a distance dependent manner: A case study with thrombin inhibitors
Keywords: Cooperativity; Protein-ligand binding; Ligand binding affinity; Scoring functions; B-factor; Thrombin; Non-additivity; Me; methyl; Bn; benzyl; Boc; tert-butoxycarbonyl; ÎGË; standard Gibbs free energy; Ki; inhibition constant; EDCI; 1-(3-dimethylaminopr
An update on the stereoselective synthesis of α-aminophosphonic acids and derivatives
Keywords: α-Aminophosphonic acids; α-Aminophosphonates; Stereoselective synthesis; Three-component reaction; ABSA; 4-acetamidobenzenesulfonyl azide; Abu; aminobutyric acid; Ac; acetyl; ACE; angiotensin-converting enzyme; Ala; alanine; Ar; aryl; BINAP; 2,2â²-bis(
Boronic species as promising inhibitors of the Staphylococcus aureus NorA efflux pump: Study of 6-substituted pyridine-3-boronic acid derivatives
Keywords: Boronic acids; Pyridine derivatives; Antimicrobial agents; Efflux pump inhibitors; Staphylococcus aureus; a.u.; arbitrary unit; Boc; tert-butoxycarbonyl; n-BuLi; n-butyllithium; EPI; efflux pump inhibitor; EtBr; ethidium bromide; MFS; major facilitator su
Synthetically modified l-histidine-rich peptidomimetics exhibit potent activity against Cryptococcus neoformans
Keywords: AA; amino acid; Boc; tert-butoxycarbonyl; DIC; 1,3-diisopropylcarbodiimide; DIEA; N,N-diisopropylethylamine; EYPC; egg yolk l-a-phosphatidylcholine; DMF; N,N-dimethylformamide; EYPG; egg yolk l-a-phosphatidyl-dl-glycerol; TBTU; O-(benzotriazol-1-yl)-N,N,N
The CuI-catalyzed alkyne-azide cycloaddition as direct conjugation/cyclization method of peptides to steroids
Keywords: Steroids; Peptide conjugates; Click chemistry; Peptidosteroids; Conjugation; Boc; tert-butoxycarbonyl; CuAAC; CuI-catalyzed alkyne-azide 1,3-dipolar cycloaddition; EDC; 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide; DIPEA; N,N-di-iso-propyl-N-ethylamine
Functional polypeptide and hybrid materials: Precision synthesis via α-amino acid N-carboxyanhydride polymerization and emerging biomedical applications
Keywords: AMM; “activated monomer” mechanism; AOB-l-Glu NCA; γ-(4-allyoxylbenzyl)-l-glutamate N-carboxyanhydride; APP; 5-(4-aminophenyl)-10,15,20-triphenyl-porphyrin; ATRP; atom transfer radical polymerization; BLA-NCA; β-benzyl-l-aspartate N-carboxyanhydride
Development of a novel amide-silica stationary phase for the reversed-phase HPLC separation of different classes of phytohormones
Keywords: HPLC; high-performance liquid chromatography; RPLC; reversed-phase liquid chromatography; NPLC; normal-phase liquid chromatography; HILIC; hydrophilic interaction chromatography; DCC; dicyclohexylcarbodiimide; DCM; dichloromethane; H; hexane; EtOAc; ethyl
Synthesis and evaluation of N8-acetylspermidine analogues as inhibitors of bacterial acetylpolyamine amidohydrolase
Keywords: APAH; acetylpolyamine amidohydrolase; dppm; bis(diphenylphosphino)methane; 9-BBN; 9-borabicyclo[3.3.1]nonane; DMP; Dess-Martin periodinane; DFMO; α-difluoromethylornithine; Boc2O; di-tert-butyl pyrocarbonate; ESI; electrospray ionization; HRMS; high-re
Cyanoacetamide-based oxime carbonates: an efficient, simple alternative for the introduction of Fmoc with minimal dipeptide formation
Keywords: Amino acids; 9-Fluorenylmethyloxycarbonyl; Oxime; N-Protecting group; Peptide synthesis; Boc; tert-butoxycarbonyl; DCM; dichloromethane; ESI-MS; electrospray ionization mass spectrometry; Fmoc; fluorenylmethyloxycarbonyl; NMR; nuclear magnetic resonance;
Total synthesis and structure-activity relationships of caspofungin-like macrocyclic antifungal lipopeptides
Keywords: Echinocandin; Caspofungin; Macrocyclic lipopeptide; Synthesis; Antifungal; SAR; Boc; tert-Butoxycarbonyl; Cbz; benyloxycarbonyl; Fmoc; 9-fluorenylmethoxycarbonyl; Ms; methanesulfonyl;
Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors
Keywords: ATP; adenosine triphosphate; Boc; tert-butoxycarbonyl; CDI; 1,1â²-carbonyldiimidazole; DMF; N,N-dimethylformamide; DMSO; dimethyl sulfoxide; DNPH; O-(2,4-dinitrophenyl)hydroxylamine; EDTA; ethylenediaminetetraacetic acid; ip; intraperitoneal; MEM; minimu
Tetrahedron report number 967Asymmetric organocatalytic cycloadditions
Keywords: Ac; acetyl; Ad; adamantyl; Ar; aryl; BINAM; 1,1â²-binaphthalenyl-2,2â²-diamine; BINOL; 1,1â²-bi-2-naphthol; Bn; benzyl; Boc; tert-butoxycarbonyl; Bu; butyl; Bz; benzoyl; Cbz; benzyloxycarbonyl; Cy; cyclohexyl; DABCO; 1,4-diazabicyclo[2.2.2]octane; DDQ;
A sucrose-derived scaffold for multimerization of bioactive peptides
Keywords: Boc; tert-butoxycarbonyl; BSA; bovine serum albumin; CCK2R; cholecystokinin 2 receptor; CCK4; Trp-Met-Asp-Phe-NH2; Cl-HOBt; 6-chloro-1-hydroxybenzotriazole; CuAAC; copper(I)-catalyzed azide-alkyne cycloaddition; DCM; dichloromethane; DIC; diisopropyl carb
Conformationally restricted analogs of the direct thrombin inhibitor FM 19
Keywords: DTI; direct thrombin inhibitor; HOBt; hydroxybenzotriazole; HBTU; O-benzotriazole-N,N,Nâ²,Nâ²-tetramethyl-uroniumhexafluorophosphate; DIEA; N,N-diisopropylethylamine; Oic; (2S,3aS,7aS)-octahydroindole-2-carboxylic acid; Phe(p-Me); p-methyl phenylalanine
Synthesis and characterization of degradable multivalent cationic lipids with disulfide-bond spacers for gene delivery
Keywords: Boc; tert-butoxycarbonyl; CL; cationic liposome; DEAD; diethylazodicarboxylate; DIEA; N,N-diisopropylethylamine; DLS; dynamic light scattering; DOB; 3,4-di(oleyloxy)benzoic acid; DOPC; 1,2-dioleoyl-sn-glycero-3-phosphatidylcholine; DOTAP; 2,3-dioleoyloxyp
Tetrahedron report number 952Aspartimide formation in peptide chemistry: occurrence, prevention strategies and the role of N-hydroxylamines
Keywords: Acm; acetamidomethyl; API; active pharmaceutical ingredient; Boc; tert-butoxycarbonyl; CRH; corticotropin-releasing hormone; DBU; 1,8-diazabicyclo[5.4.0]undec-7-ene; DCM; dichloromethane; DEPBT; 3-(diethoxy-phosphoryloxy)-3H-benzo[d][1,2,3] triazin-4-one;