Valuable chiral N-Boc-β-benzyl-β-amino acid was concisely synthesized via construction of chiral N-Boc-3-benzyl-5-oxoisoxazolidine through cross-metathesis/conjugate addition/oxidation. All of the starting materials for the synthesis of chiral N-Boc-β-benzyl-β-amino acid are cheap, and two-s...

This study selected common processing methods for orthodox black tea and investigated changes in the levels of Nε-(carboxymethyl)lysine (CML), Nε-(carboxyethyl)lysine (CEL), lysine, and polyphenols during each processing stage and using different parameters of each processing step. The effects...

Chitosan is a biopolymer that has antifungal activity against C. albicans. Chemical modification of chitosan can provide it with new functional properties for a wide range of biological and biomedical applications. Carboxymethyl chitosan is a derivative of chitosan obtained by etherification of ...

A range of small molecule scaffolds have been shown to act as structural and functional mimics of α-helices by mimicking the i, i+4, and i+7 positions, often found at the interface of PPIs. These molecules, though potent, possess complicating features—either low water solubility, or maintenanc...

Homologation of glutamic acid chain together with conformational constraint is a commonly used strategy to achieve selectivity towards different types of glutamate receptors. In the present work, starting from two potent and selective unnatural amino acids previously developed by us, we investig...

Radiolabeled amino acids have been used extensively in oncology both as diagnostic and therapeutic agents. In our pursuit to develop radiopharmaceuticals to target breast cancer, we were interested in determining the uptake of radioiodinated 4-iodophenylalanine, among other labeled amino acids, ...

Sequential Ugi reaction between p-substituted arylglyoxals, alkylamines, cyclohexyl isocyanide and 3-azido-(S)-2-(tert-butoxycarbonylamino)propanoic acid, followed by a Staudinger/aza-Wittig cyclization in the presence of triphenylphosphine, gave rise to enantiomerically pure N-cyclohexyl 4-alky...

Introductionmeta-[123/131I]Iodobenzylguanidine (mIBG) is a clinical agent used for imaging neuroendocrine tumors, where uptake in tumor is via active transport mechanism through norepinephrine transporters (NET). Our group in past have evaluated a 99mTc-analogue of the above tracer, based on 99m...

Several aza-C-pseudonucleosides bearing 1,3-benzothiazin-4-one (6 and 7) were prepared by the one-pot three-component condensation from the iminosugar aldehyde 3, amino acid ethyl/methyl ester hydrochlorides 4(a–c), and 2-mercaptobenzoic acid 5. After removal of Boc and the isopropylidene group...

A Lewis-acid promoted one-carbon homologation of an aspartic acid semialdehyde with trimethylsilyldiazomethane has led to the efficient synthesis of two silicon-containing α-amino acids. The use of trimethylaluminium or catalytic tin(II) chloride gave novel 4-oxo-5-trimethylsilanyl derived amin...

Amino acid based triple responsive (pH, thermo and salt) copolymer hydrogel system has been designed and synthesized from organogels obtained from copolymerization of tert-butoxycarbonyl (Boc)-valine methacryloyloxyethyl ester (Boc-Val-HEMA) and 2-(2-methoxyethoxy)ethyl methacrylate (MEO2MA) in ...

Amides of betulinic acid with cystamine were synthesized to investigate their antimicrobial and antitumor activity, and their influence on the cell cycle and cell apoptosis. The former target amide (6) displayed cytotoxicity in CEM cell line after 72 h of treatment (IC50 = 3.0 ± 0.7 μM; TI = 2...

Novel capric acid-tryptophan based block copolymers with unique self-assembled feature and fluorescence property have been synthesized via reversible addition fragmentation chain transfer polymerization (RAFT) polymerization. For employing the copolymerization, at first the fatty acid based meth...

Methyl 2-[1-[(tert-butoxycarbonyl)amino]ethyl]-4-methyloxazole-5-carboxylate (1) was synthesized with high optical purity via a Pd–catalyzed amide coupling with vinyl triflate with subsequent oxazole formation. The latter reaction proceeds via bromination of an enamide with NBS and DBU-promoted...

Reversible addition–fragmentation chain-transfer (RAFT) polymerization has been used for the controlled synthesis of block copolymers containing side-chain fatty acid and amino acid block segments, namely, poly(2-(methacryloyloxy)ethyl stearate)-block-poly(tert-butyloxycarbonyl phenylalanine me...

Efficient stereodivergent syntheses of (+)-lycoperdic acid (LPA) and 4-epi-LPA have been achieved based on asymmetric hydrogenation (H2, Rh/(R,S)-MeBoPhoz) of racemic enamide as a key step.

Legionaminic acid and 4-epi-legionaminic acid are 5,7-diacetamido nonulosonic acids and are assumed to play a crucial role in the virulence of Legionella pneumophila, the causative agent of Legionnaires’ disease. Moreover, they are ideal target motifs for the development of vaccines and pathoge...

Identification and SAR study of novel series of β3-AR agonists with benzoic acid are described. Conversion of ether linkage position of phenoxybenzoic acid derivative 2b led to compound 7b with moderate β3-AR activity. Further modification in right, center and left parts of compound 7b was inv...

The physicochemical properties of metallic substrates are affected by the environment in different ways. It is generally difficult to determine these effects because the molecules in the environment interact weakly with metallic substrates. In this work, we demonstrate that even the effect of vo...

The complexes [Bu2(DMPA)SnOSn(DMPA)Bu2]2 (2) and [Bu2Sn(DMPA)2] (3), where HDMPA is 2-[bis(2,6-dimethylphenyl)amino]benzoic acid, have been prepared and structurally characterized by means of, vibrational, ultra-violet, 1H and 13C NMR spectroscopies. The crystal structure of complexes 2 and 3 ha...