Tubulin is the target of many anticancer drugs, including N-phenyl-N′-(2-chloroethyl)urea (CEU). Unlike most anti-β-tubulin agents, CEUs are protein monoalkylating agents binding through their N′-(2-chloroethyl)urea moiety to an amino acid nearby the colchicine-binding site on β-tubulin isof...
In order to identify a high-affinity, selective antagonist for the A2B subtype adenosine receptor, more than 40 1,8-disubstituted-3-(3-methoxypropyl) xanthines were prepared and evaluated for their binding affinity at recombinant human adenosine receptors, mainly of the A2A and A2B subtypes. Som...
The nucleus of the carbacephem antibiotic loracarbef was synthesized in a highly efficient and enantioselective fashion from 2S,3S-2-amino-3-hydroxy-6-heptenoic acid (AHHA), which was derived from enzyme-catalyzed condensation of glycine and 4-pentenaldehyde. The bicyclic framework of this compo...
While continuing our research on Hunsdiecker reaction, we came across an interesting application of bleach, sodium hypochlorite (NaOCl) for decarboxylative chlorination reaction. The reaction is easily scaled up to 10 mmol. The reaction has good tolerance towards wide variety of functional group...
Starting from a 3,5-dihydroxyheptanoic acid derivative, a new synthesis of pyrrole statins that contain a double bond on the dihydroxyacid chain has been developed. Key steps are N-acylamino acid enamide formation through enamine trapping with aromatic acyl chlorides and subsequent münchnone cy...
A series of disubstituted thiazoles, functionalized with the essential 3,5-dihydroxy-6-heptenoic or heptanoic chain, were prepared and evaluated for their ability to inhibit the enzyme HMG-CoA reductase in vitro. All the synthesized compounds 46–61 showed a moderate inhibitory potency.
A convenient method for the synthesis of 6-heptenoic acid by means of the pyrolysis of ω-heptano lactone (II) is reported. The lactone was prepared by Baeyer-Villiger oxidation of cycloheptanone (I).
The self-association through hydrogen bonding of four isomeric N-butylacetamides has been studied by infrared spectroscopy in carbon tetrachloride, chloroform and benzene. The spectroscopic and thermodynamic parameters for the self-association have been determined. It was found that self-associa...
This paper reports the results of FTIR study of N-tert-butylacetamide in carbon tetrachloride solution and in presence of seven different molecules as H acceptors. The spectroscopic characteristics for NH⋯O hydrogen bonded complexes are given. Also, the equilibrium constants for 1:1 complex form...
The indole nucleus of Z-Trp-OBzl is modified by acylation of the indole nitrogen using Boc-N-methyl butyric acid followed by catalytic hydrogenation and introduction of the Fmoc group. The resulting derivative, Fmoc-Trp(Boc-Nmbu)-OH, is incorporated into peptide chains via solid-phase peptide sy...
A method has been developed and optimized in order to detect and quantify the non-protein amino acid β-N-methylamino-l-alanine(BMAA) in cyanobacteria. The novelty of the method is that we have used methanol instead of acetonitrile as the eluent. The method includes extraction with 0.1 M trichlo...
A new method was developed for analysis of free β-Methylamino-alanine (BMAA) in biological matrices. The method is based on direct analysis of the underivatized molecule, using an amide column for separation by Hydrophilic Interaction Liquid Chromatography (HILIC) and detection by tandem mass s...
The cyanobacterial neurotoxin β-N-methylamino-l-alanine (BMAA) has been associated with certain forms of progressive neurodegenerative disease, including sporadic Amyotrophic Lateral Sclerosis and Alzheimer’s disease. Reports of BMAA in cyanobacterial blooms from lakes, reservoirs, and other w...
Rate coefficients for the gas-phase reactions of Cl atoms with a series of unsaturated biogenic alcohols at 298 ± 3 K and 1 atm have been measured by the relative technique in an environmental chamber with in situ FTIR detection of reactants. The rate coefficients obtained using 1-butene and is...
Mono- and dinuclear nickel(II) complexes with N3O asymmetrical Schiff bases have been prepared and characterised. The ligands used here were obtained by condensation of the amine 7-amino-4-methyl-5-aza-3-hepten-2-one (HAE) and 4(5)-imidazolecarboxaldehyde or 2-acetylpyrazine, to yield the isolat...
A series of new polysiloxanes containing chiral side groups has been prepared. These polymers were prepared by hydrosilylating chiral alkene derivatives onto polyhydromethylsiloxane. The alkene derivatives were prepared from (+) or (-)-2-phenyl-3-butenoic acid, (R)-1-hepten-3-ol and (R)-1-cycloh...
We report herein a visible light-induced aerobic oxidative hydroxylation of boronic acids. The reaction employed 7H-benzo[c]thioxanthen-7-one as metal-free catalyst and dimethyl carbonate as green solvent. Scale-up experiment was achieved using 0.1 mol% catalyst in a good yield with column-free ...
Extensive studies on the penicillin G acylase-mediated kinetic resolution of N-acylated 1-aminoalkylphosphonic and 1-aminoalkylphosphinic acids as well as their esters were carried out to recognise the relationships between the substrate structure, reaction conditions, and the enzymatic hydrolyt...
This study aimed to investigate the effects of substitution position on the electrochemical, electrochromic, optical, and photoresponsive properties of azobenzenecarboxylic acid alkyl ester derivatives. Therefore, a series of azobenzenen ester derivatives, including azobenzene-4,4′-dicarboxylic...
A novel series of 2-amino-4-oxo-6-substituted pyrrolo[2,3-d]pyrimidines were designed and synthesized as potential nonclassical antifolates targeting both thymidylate and purine nucleotide biosynthesis. Condensation of 2,4-diamino-6-hydroxypyrimidine with ethyl-4-chloroacetoacetate and subsequen...
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