Abbreviations: AcOEt, ethyl acetate; Boc, t-butoxycarbonyl; DCC, N,N'-dicyclohexylcarbodiimide; DCM, dichloromethane; DhBtOH, 3-hydroxy-1,2,3-benzotriazin-4(3H)-one; DIC, N,N'-diisopropylcarbodiimide; DIPEA, diisopropylethylamine; DMF, N,N-dimethylformamide; DMSO, dimethylsulfocide; EDC, N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide; FA, formic acid; Fmoc, 9-fluorenylmethoxycarbonyl; MeOH, met...

A versatile solid-phase approach to sequence-defined polyamidoamines was developed. Four different Fmoc-polyamino acid building blocks were synthesized by selective protection of symmetrical oligoethylenimine precursors followed by introduction of a carboxylic acid handle using cyclic anhydrides and subsequent Fmoc-protection. The novel Fmoc-polyamino acids were used to construct polyamidoamine...

Silkworm powder containing 1-deoxynojirimycin (DNJ) has α-glucosidase inhibitory activity and is promising as a complementary and alternative medicine (CAM) agent in Japan. Silkworm powder produced in Korea was extracted with 75% ethanol. The extract was derivatized with 9-fluorenylmethyl chloroformate (FMOC-Cl), and DNJ-FMOC content was measured by HPLC. Then, alfa-glucosidase inhibition by si...

In an effort to probe the inhibition of glyoxalase II (GLX2-2) from Arabidopsis thaliana, a series of N- and S-blocked glutathione compounds containing 9-fluorenylmethoxycarbonyl (FMOC) and Cbz protecting groups were synthesized and tested. The di-FMOC and di-Cbz compounds were the best inhibitors of GLX2-2 with K(i) values of 0.89+/-0.05 and 2.3+/-0.5 microM, respectively. The removal of prote...

This present paper deals with the development and validation of a stability indicating high performance liquid chromatographic method for the quantitative determination of Memantine hydrochloride. Memantine hydrochloride was derivatized with 0.015 M 9-fluorenylmethyl chloroformate (FMOC) and 0.5 M borate buffer solution by keeping it at room temperature for about 20 minutes and the chromatograp...

Glucose-dependent insulinotropic polypeptide (GIP) is an important incretin hormone, which potentiates glucose-induced insulin secretion. Antihyperglycaemic actions of GIP provide significant potential in Type II diabetes therapy. However, inactivation of GIP by the enzyme dipeptidyl peptidase IV (DPP IV) and its consequent short circulating half-life limit its therapeutic use. Therefore two no...

In this communication, solid-phase reactions for the synthesis of Lys-monofunctionalized gold nanoparticles are described. A controlled and selective fabrication of linear nanoparticle arrays can be achieved through peptide linkage systems, and therefore it is essential to prepare Fmoc amino acid nanoparticle building blocks susceptible to Fmoc solid-phase peptide synthesis. Gold nanoparticles ...

An efficient method for the synthesis of (S)-7-aza-tryptophan via tridentate chiral auxiliary derived Ni(II)-complexes has been developed. This three-step includes alkylation, disassembling and Fmoc-protection. The desired Fmoc-L-7-AzaTrp-OH was obtained in over 49 % yield with excellent diastereoselectivity.

Preparation, Characterization and Visualization of CPP-Mediated MR Contrast Agents Category: Multifunctional probes Wu Su, Ritu Mishra, Jörn Engelmann, Josef Pfeuffer, Kamil Ugurbil, Max-Planck-Institute for Biological Cybernetics, Tuebingen, Germany. Contact e-mail: [email protected] Presentation Number: 542 Recent developments in MR imaging have enabled in vivo imaging at near microscopi...