Two series of 1,4-bis(2-amino-ethylamino)anthraquinone–amino acid conjugates (BACs), ametantrone (AT)–amino acid conjugates (AACs) and mitoxantrone (MX)–amino acid conjugates (MACs), were designed and synthesized. The DNA binding of BACs was evaluated by DNA thermal denaturation experiment. I...

To search for new drugs for intervention of drug-resistant lung cancer, a series of hybrids 4-15 from 2-cyano-3,12-dioxooleana-9-dien-28-oic acid (CDDO) and O2-(2,4-dinitrophenyl) diazeniumdiolate were designed, synthesized and biologically evaluated. The most active compound 7 produced relative...

The electrochemical treatment of low-salinity reverse osmosis (RO) concentrates was investigated using tramadol (100 μM) as a model substance for persistent organic contaminants. Galvanostatic degradation experiments using boron-doped diamond electrodes at different applied currents were conduc...

The stoichiometric reactions of amines with tri(4-chlorophenyl)boroxine (CPB) led to the formation of adducts CPB·L {L = morpholine (1a), benzylamine (1b) cyclohexylamine (1c), 2-picoline (1d), 4-picoline (1e), piperidine (1f)} and (CPB)2·(4,4′-trimethylenedipiperidine) (1g). Compounds 1a-1g ...

The FTIR and FT-Raman vibrational spectra of N-(4-bromophenyl)-2,2-dichloroacetamide molecule has been recorded and analysed the complete vibrational fundamental modes of the most stable geometry of the compound using the experimental FTIR and FT-Raman data on the basis of peak positions, relati...

The aim of this study was to determine the effects of 4-(4-bromophenyl)-5-(3-chlorophenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione (TP4—a new S-triazole derivative possessing anticonvulsant properties in preclinical studies) on the protective action of four different classical antiepileptic drug...

BackgroundCobamide diversity arises from the nature of the nucleotide base. Nicotinate mononucleotide (NaMN):base phosphoribosyltransferases (CobT) synthesize α-linked riboside monophosphates from diverse nucleotide base substrates (e.g., benzimidazoles, purines, phenolics) that are incorporate...

SummaryCobamides are members of the vitamin B12 family of cofactors that function in a variety of metabolic processes and are synthesized only by prokaryotes. Cobamides produced by different organisms vary in the structure of the lower axial ligand. Here we explore the molecular factors that con...

Several analogues of thuriferic acid and derivatives, with the 3,4-methylenedioxyphenyl ring replaced by naphthalene, furan, thiophene and carbazole ring systems, have been prepared. The synthetic strategy is based on a conjugate addition–alkylation methodology followed by cationic cyclization ...

In this paper we report on the development of a flexible and efficient synthetic approach towards 6,7-didehydrocarnosoic acid type analogues. The elaboration of the required trans-decalin system, the installation of the carboxylic acid in the angular position as well as the generation of the C6–...

Publisher SummaryThis chapter explains the description, physical properties, total synthesis, drug stability, and methods of analysis of homatropine hydrobromide. Examination of the nuclear magnetic resonance (NMR) spectra of some tropane deuterohalides has shown that the N-substituent in tropan...

A comparison of the effects of scopolamine and physostigmine on working memory and reference memory in White Carneaux pigeons was undertaken. In Experiment 1, the pigeons received injections of scopolamine hydrobromide (0.03 mg/kg), or saline. Scopolamine hydrobromide had greater disruptive effe...

Sprague-Dawley rats were trained to discriminate a subcutaneous injection of physostigmine (0.2 mg/kg) from a similar injection of saline in a two-lever, food-reinforced behavior paradigm. The training dose of physostigmine reduced the response rate to about 50% of that in saline sessions. The d...

Pre-treatment with reversible acetylcholinesterase (AChE) inhibitors is an effective strategy for reducing lethality following organophosphate nerve agent exposure. AChE inhibition may have unwanted cardiac side effects, which could be negated by adjunctive anti-cholinergic therapy. The aims of ...

Herein, we embarked on a structural optimization campaign aiming at the discovery of second generation anti-angiogenesis agents with our previously reported BPS-7 as lead compound. A library of 27 compounds has been afforded based on the highly conserved ATP-binding pocket of VEGFR-2, Tie-2, and...

Conversion of the easily accessible racemic bis(amino acid)s cis- and trans-2a into the (S)-enantiomers via the corresponding Schiff bases with (1S,2S,5S)-2-hydroxy-3-pinanone is described. Condensation of the N-Boc-protected bis(amino acid)s with esters of the corresponding axially chiral amino...

The syntheses of the terminally protected, crowned, Cα-tetrasubstituted α-amino acids with only axial chirality, the two diastereomers Boc-(S)-Bip[(R)-Binol-22-C-6]-OMe and Boc-(R)-Bip[(R)-Binol-22-C-6]-OMe, and their respective enantiomers Boc-(R)-Bip[(S)-Binol-22-C-6]-OMe and Boc-(S)-Bip[(S)...

The title compound 4, possessing a biaryl axis as the sole source of chirality, has been prepared in the enantiomerically pure (R) as well as racemic form by two alternative procedures starting from dibromide 1.

N-t-Boc 6-amino-1,11-(20-crown-6)-6,7-dihydro-5H-dibenzo[a,c]cycloheptene-6-carboxylic acid methyl ester: Boc-[20-C-6]-Bip-OMe 1, a new crown-carrier-α,α-disubstituted glycine with axial dissymmetry and a potential building block for the synthesis of polypeptide supramolecular devices, has bee...

A series of mono-substituted 4-phenylpiperidines and -piperazines have been synthesized and their effects on the dopaminergic system tested in vivo. The structure activity relationship (SAR) revealed that the position and physicochemical character of the aromatic substituent proved to be critica...