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(
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Antiobesity and emetic effects of a short-length peptide YY analog and its PEGylated and alkylated derivatives
Keywords: Ac; acetyl; Aib; 2-aminoisobutyric acid; tBu; tert-butyl; Cha; 3-cyclohexylalanine; CHAPS; 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate; DIO; diet-induced obese; DIPCDI; N,Nâ²-diisopropylcarbodiimide; DMF; N,N-dimethylformamide; DMSO; dimeth
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 and biological evaluation of cyclopeptide GG-8-6 and its analogues as anti-hepatocellular carcinoma agents
Keywords: HCC; hepatocellular carcinoma; MDP; muramyl dipeptide; SAR; structure and activity relationship; SPPS; solid phase peptide synthesis; MeOH; methanol; MTT; 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide; PI; propidium iodide; VP-16; etop
Lactam hybrid analogues of solonamide B and autoinducing peptides as potent S. aureus AgrC antagonists
Keywords: Autoinducing peptides; Anti-virulence therapy; Solonamide; Quorum-sensing system; Staphylococcus aureus; AIP; autoinducing peptide; CA-MRSA; community-associated; Dap; (S)-2,3-diaminopropamoic acid; Fmoc; fluoren-9-ylmethoxycarbonyl; hLeu; homoleucine; HO
Phenylglycine racemization in Fmoc-based solid-phase peptide synthesis: Stereochemical stability is achieved by choice of reaction conditions
Keywords: COMU; (1-cyano-2-ethoxy-2-oxoethylidenaminooxy)dimethylaminomorpholinocarbenium hexafluorophosphate; DBU; 1,8-diazabicyclo[5.4.0]undec-7-ene; DEPBT; 3-diethoxyphosphoryloxy)-1,2,3-benzotriazin-4(3H)-one; DIPEA; N,N-diisopropylethylamine; DMF; N,N-dimethyl
Highly potent antiobesity effect of a short-length peptide YY analog in mice
Keywords: Ac; acetylated; Aib; 2-aminoisobutyric acid; tBu; tert-butyl; Cha; 3-cyclohexylalanine; CHAPS; 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate; DIO; diet-induced obese; DIPCDI; N,Nâ²-diisopropylcarbodiimide; DMF; N,N-dimethylformamide; DMSO; di
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
New amphiphilic neamine conjugates bearing a metal binding motif active against MDR E. aerogenes Gram-negative bacteria
Keywords: Antibacterial activity; Gram-negative bacteria; Metal-binding groups; Membrane permeability; Multidrug resistant bacteria; Neamine derivatives; HOAt; 1-hydroxy-7azabenzotriazole; HATU; 1-[Bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium-3-o
Effect of TLR ligands co-encapsulated with multiepitopic antigen in nanoliposomes targeted to human DCs via Fc receptor for cancer vaccines
Keywords: AAA; amino acid analysis; C18; octadecylsilica; DIEA; N,N-diisopropyl-ethylamine; DIPCDI; N,N'-Diisopropylcarbodiimide; DMF; N,N-dimethylformamide; DMSO; dimethyl sulfoxide Fmoc, 9-fluorenylmethoxycarbonyl; HOAt; 1-hydroxy-7-azabenzotriazole (3-hydroxy-
Synthesis and biological evaluation of the [d-MeAla11]-epimer of coibamide A
Keywords: Hva; α-hydroxyisovaleric acid; HATU; O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate; BTC; bis(trichloromethyl) carbonate; DIC; 1,3-diisopropylcarbodiimide; HOBt; 1-hydroxybenzotriazole; HOAt; 1-hydroxy-7-azabenzotriazole; TFA;
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
A total synthesis of a highly N-methylated cyclodepsipeptide [2S,3S-Hmp]-aureobasidin L using solid-phase methods
Keywords: Aureobasidin; N-Methylated cyclodepsipeptide; Depsidipeptide; Fmoc-based solid-phase peptide synthesis; Boc; tert-butyloxycarbonyl; BTC; bis-(trichloromethyl)-carbonate; 13C NMR; carbon-13 nuclear magnetic resonance; COSY; correlation spectroscopy; DBU; 1
Backbone cyclic helix mimetic of chemokine (C-C motif) receptor 2: A rational approach for inhibiting dimerization of G protein-coupled receptors
Keywords: ACN; acetonitrile allocallyloxycarbonyl; BBB; blood brain barrier; Boc; t-butyloxycarbonyl; BTC; bis(trichloromethyl)carbonate; CCR2; chemokine (C-C motif) receptor 2; CCR5; chemokine (C-C motif) receptor 5; CNS; central nervous system; DIPEA; diisopr
Membrane thickness and the mechanism of action of the short peptaibol trichogin GA IV
Keywords: HFIP; 1,1,1,3,3,3-hexafluoroisopropanol; Aib; α-aminoisobutyric acid; Alm; alamethicin; AMP; antimicrobial peptide; CF; carboxyfluorescein; DIEA; N,N-diisopropylethylamine; DMF; N,N-dimethylformamide; EDC; N-ethyl, Nâ²-[3-(dimethylamino)propyl]carbodiim
Anthelmintic PF1022A: stepwise solid-phase synthesis of a cyclodepsipeptide containing N-methyl amino acids
Keywords: ACN; acetonitrile; Boc; tert-butyloxycarbonyl; BOPCl; N,Nâ²-bis(2-oxo-3-oxazolidinyl)phosphinic chloride; DCM; dichloromethane; DEAD; diethylazodicarboxylate; DHP; 3,4-dihydro-2H-pyrane; DIC; N,Nâ²-diisopropylcarbodiimide; DIEA; diisopropylethylamine; D
Proteasome inhibitors for cancer therapy
Keywords: BOP; (benzotriazol-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate; DMSO; dimethyl sulfoxide; HMPA; hexamethyl phosphoramide; HOBt; 1-hydroxybenzotriazole; NMM; N-methylmorpholine; DMF; N,N-dimethyformamide; LDA; lithium diisopropylamide; THF;
Interaction and transport of kynurenic acid via human organic anion transporters hOAT1 and hOAT3
Keywords: hOAT; human organic anion transporter; NMDA; N-methyl d-aspartate; NSAID; nonsteroidal anti-inflammatory drug; hOAT1; hOAT3; Tryptophan metabolites; Kynurenic acid; Transport;
Paromomycin and neomycin B derived cationic lipids: Synthesis and transfection studies
Keywords: Boc; tertbutyloxycarbonyle; CholNeo; cholesterol-neomycin; CholParomo; cholesterol-paromomycin; DOPE; dioleoyl-l-α-phosphatidylethanolamine; DOSCP; dioleyl-succinyl-caproic-paromomycin; DOSLP; dioleyl-succinyl-lysine-paromomycin; DOSN; dioleyl-succinyl-n
Fast and efficient characterization of an anti-gliadin monoclonal antibody epitope related to celiac disease using resin-bound peptides
Keywords: AcOH; acetic acid; Anti-gliadin mAb; anti-gliadin monoclonal antibody; AP; alkaline phosphatase; BSA; bovine serum albumin; CD; celiac disease; DCM; dichloromethane; DIC; N,N'-diisopropylcarbodiimide; DMAP; 4-dimethylaminopyridine; ELISA; enzyme-linked im
Novel analogues of the therapeutic complement inhibitor compstatin with significantly improved affinity and potency
Keywords: Ac; acetyl group; DCM; dichloromethane; DIC; 1,3-diisopropylcarbodiimide; DIPEA; N,N-diisopropylethylamine; DMF; N,N-dimethylformamide; ESI; electrospray ionization; Fmoc; 9-fluorenylmethoxycarbonyl; HOAt; 1-hydroxy-7-aza-benzotriazole; ITC; isothermal ti
Rational conversion of noncontinuous active region in proteins into a small orally bioavailable macrocyclic drug-like molecule: The HIV-1 CD4:gp120 paradigm
Keywords: AcOH; acetic acid; Alloc; allyloxycarbonyl; Boc; t-butoxycarbonyl; BTC; bis(trichloromethyl)carbonate; DBU; 1,8-diazabicyclo[5.4.0]undec-7-ene; DCM; methylene chloride; DIC; N,Nâ²-diisopropylcarbodiimide; DIPEA; diisopropylethylamine; DMAP; dimethylamino
Synthesis of the chlorofusin cyclic peptide
Keywords: Ada; 2-aminodecanoic acid; EDCI; 1-ethyl-3-(3-dimethylamino-propyl)carbodiimide; HOAt; 1-hydroxy-7-azabenzotriazole; MDM2; murine double minute 2 protein; p53; protein 53; SES; 2-(trimethylsilyl)ethylsulfonyl; Trt; trityl (triphenylmethyl);
Preparation of peptide thioesters using Fmoc strategy through hydroxyl side chain anchoring
Keywords: Bpoc; 2-(4-biphenylyl)isopropoxycarbonyl; HATU; 2-(1H-7-azabenzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate; HOAt; hydroxy-7-azabenzotriazole; DCC; N,Nâ²-dicyclohexylcarbodiimide; DIEA; N,N-diisopropylethylamine; Fmoc; 9-fluorenylmethox
PS-IIDQ: a supported coupling reagent for efficient and general amide bond formation
Keywords: Coupling reagent; Polymer-supported reagent; Immobilized reagent; IIDQ; Parallel synthesis; Amide bond formation; Amidation; Amide; BOP; benzotriazolyl-N-oxytrisdimethylaminophosphonium hexafluorophosphate; BOP-Cl; N,Nâ²-bis(2-oxo-3-oxazolidinyl)-phosphi
Controlling the outcome of overacylation of N-protected aminooxyacetic acid during the synthesis of an aminooxy-peptide for chemical ligation
Keywords: Aloc; allyloxycarbonyl; Aoa; aminooxyacetic acid; DCC; N,Nâ²-dicyclohexylcarbodiimide; DIEA; N,N-diisopropylethylamine; DMAP; 4-dimethylaminopyridine; Fmoc; 9-fluorenylmethoxycarbonyl; HATU; 2-(1H-7-azabenzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexaf
Synthetic applications of fluorous solid-phase extraction (F-SPE)
Keywords: Fluorous; Light fluorous; Fluorous silica gel; Fluorous solid-phase extraction (F-SPE); Reverse F-SPE; Plate-to-plate SPE; Parallel synthesis; High-throughput synthesis; Solution-phase synthesis; Separation; Reagents; Reactants; Catalysts; Chiral auxiliar
A concise synthesis of (3S,4S,5R)-1-(α-d-galactopyranosyl)-3-tetracosanoylamino-4,5-decanediol, a C-glycoside analogue of immunomodulating α-galactosylceramide OCH
Keywords: TMSOTf; trimethylsilyl trifluoromethanesulfonate; PTSA; p-toluenesufonic acid; MTPA; 2-methoxy-2-phenyl-2-(trifluoromethyl)acetic acid; DME; 1,2-dimethoxyethane; EDCI·HCl; 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride; HOAt; 1-hydroxy-7-a
Explosive properties of 1-hydroxybenzotriazoles
Keywords: 1-Hydroxybenzotriazoles; HOBt; 6-Cl-HOBt; TBTU; HOAt; Explosive properties;
Potentiation of bradykinin actions by analogues of the bradykinin potentiating nonapeptide BPP9α
Keywords: AA; arachidonic acid; ABA; 4-azidobenzoic acid; ACE; angiotensin I-converting enzyme; Aloc; allyl oxycarbonyl; ASA; 4-azidosalicylic acid; BK; bradykinin; BKR; bradykinin receptor; BKR-B1; bradykinin B1 receptor; BKR-B2; bradykinin B2 receptor; Boc; tert-