Search Results - "Romoff, Todd"
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Scale-up Synthesis of (R)- and (S)‑N‑(2-Benzoyl-4-chlorophenyl)-1-(3,4-dichlorobenzyl)pyrrolidine-2-carboxamide Hydrochloride, A Versatile Reagent for the Preparation of Tailor-Made α- and β‑Amino Acids in an Enantiomerically Pure Form
Published in Organic process research & development (19-05-2017)“…Unusual amino acids are of crucial importance to the synthesis of bioactive peptides and new chemical entities. Innovative methodology is always needed for the…”
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Development of Hamari Ligands for Practical Asymmetric Synthesis of Tailor-Made Amino Acids
Published in ACS omega (19-11-2019)“…Enantiomerically pure tailor-made amino acids are in extremely high demand in nearly every sector of the health-related industries. In particular, the rapidly…”
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Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors
Published in Bioorganic & medicinal chemistry (15-03-2008)“…The synthesis, SAR, and in vivo activity of highly potent thiamine mimetics utilized as transketolase (TK) antagonists is presented. Tumor cells extensively…”
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4
Non-charged thiamine analogs as inhibitors of enzyme transketolase
Published in Bioorganic & medicinal chemistry (15-01-2008)“…The synthesis and SAR including structure-based rationale drug design for highly potent non-thiazolium TK antagonists is presented. Inhibition of the…”
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Prodrug thiamine analogs as inhibitors of the enzyme transketolase
Published in Bioorganic & medicinal chemistry (15-01-2008)“…Synthesis of prodrugs of the transketolase inhibitor 5a and their evaluation in murine pharmacokinetic and pharmacodynamic models. Transketolase, a key enzyme…”
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6
Mechanistic Studies of an Unusual Amide Bond Scission
Published in Journal of the American Chemical Society (28-07-1999)“…Unusual acid cleavage reactions are reported for derivatives containing acylated N-methyl-α-aminoisobutyryl (NMeAib) residues. The bond linking the NMeAib…”
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7
Rapid and efficient syntheses of tryptophans using a continuous-flow quaternization-substitution reaction of gramines with a chiral nucleophilic glycine equivalent
Published in Organic & biomolecular chemistry (02-11-2022)“…A continuous-flow quaternization reaction of gramines with MeI (<1 min) followed by a substitution reaction with a chiral nucleophilic glycine-derived…”
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Conformationally Constrained Peptides and Semipeptides Derived from RGD as Potent Inhibitors of the Platelet Fibrinogen Receptor and Platelet Aggregation
Published in Journal of medicinal chemistry (01-03-1994)“…Structure-activity studies have been pursued on cyclo-S,S-[Ac-Cys-(N alpha-Me)Arg-Gly-Asp-Pen]-NH2, 2 (SK&F 106760), a potent inhibitor of platelet…”
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3-(Diethoxyphosphoryloxy)-1,2,3- benzotriazin-4(3H)-one (DEPBT): A New Coupling Reagent with Remarkable Resistance to Racemization
Published in Organic letters (15-07-1999)“…The new crystalline phosphate reagent 3-(diethoxyphosphoryloxy)-1,2,3-benzotriazin-4(3H)-one (DEPBT) mediates amide bond formation with a remarkable resistance…”
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11
The in vitro pharmacological profile of SK&F 106760, a novel GPIIB/IIIA antagonist
Published in Thrombosis research (15-07-1994)“…The properties of SK&F 106760 [N alpha-acetyl-cyclo(S,S)-cysteinyl-N alpha-methyl-arginyl-glycyl-aspartyl-penicillamine-amide] as a GPIIb/IIIa antagonist have…”
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Regioselectivity and kinetics of hydride transfer in substituted 1-benzyl-3-quinolinecarboxamide redox reactions
Published in Journal of organic chemistry (01-10-1987)Get full text
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Large-Scale Synthesis of the Glycine Schiff Base Ni(II) Complex Derived from (S)- and (R)‑N‑(2-Benzoyl-4-chlorophenyl)-1-[(3,4-dichlorophenyl)methyl]-2-pyrrolidinecarboxamide
Published in Organic process research & development (21-02-2020)“…Non-natural, tailor-made amino acids are of crucial importance to the synthesis of bioactive peptides and new chemical entities. Innovative methodology is…”
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14
Identification and characterization of a potent and selective antagonist of the prostaglandin D2 receptor (94.23)
Published in The Journal of immunology (1950) (01-04-2009)“…Abstract Prostaglandin D2 (PGD2) is a potent lipid mediator released from activated mast cells during allergic responses which exerts its pro-inflammatory…”
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Investigation of conformational specificity at GPIIb/IIIa: evaluation of conformationally constrained RGD peptides
Published in Journal of medicinal chemistry (01-10-1992)“…RGD-containing proteins and peptides are known to bind to the platelet GPIIb/IIIa receptor and inhibit platelet aggregation. That a conformational component to…”
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16
Stereochemical considerations for the synthesis of peptides and peptidomimetics
Published 1996“…This dissertation focuses largely on methodology for the preparation of peptidic and peptidomimetic lead compounds for drug discovery projects. As such, the…”
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Dissertation -
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Urethane-protected N-carboxyanhydrides (UNCAs) as unique reactants for the study of intrinsic racemization tendencies in peptide synthesis
Published in The journal of peptide research (01-04-1997)“…We have established that urethane‐protected N‐carboxyanhydrides (UNCAs) are uniquely suited for the study of intrinsic racemization tendencies in peptide…”
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