Antifungal studies were made of mixtures of minimal inhibitory concentrations (MICs) of 8-quinolinol and its bischelates with copper(II), zinc(II), and manganese(II) and with mixed ligand chelates composed of 8-quinolinol, copper(II) and a second ligand including salicylic acid, 3-hydroxy-2-naph...

7-Methoxy-3,4-dihydro-2H-1-benzopyran-2-one 2 was converted into 3-(2′-tert-butyldimethylsilyloxy-4′-methoxyphenyl)-N-methyl-N-phenylpropanamide 25 and reaction of this with methyl trifluoromethanesulfonate, followed by reaction with sodium methoxide, gave 2,2,7-trimethoxy-2H-1-benzopyran1a in...

By applying a diversity oriented synthesis strategy for the search of new antagonists of the thrombin receptor PAR1, a series of peptide-based ureas and thioureas, including analogues of the PAR1 reference antagonist RWJ-58259, has been designed and synthesized. The general synthetic scheme invo...

The triazol compound 4-(4-methoxyphenethyl)-5-benzyl-2H-1,2,4-triazol-3(4H)-one monohydrate (I) has been synthesized and characterized by 1H NMR, 13C NMR, IR, and X-ray single-crystal determination. The molecular geometry, vibrational frequencies and gauge including atomic orbital (GIAO) 1H and ...

4-(4-Methoxyphenethyl)-3,5-dimethyl-4H-1,2,4-triazole (3) was synthesized from the reaction of ethyl N′-acetylacetohydrazonate (1) with 2-(4-methoxyphenyl)ethanamine (2). The structure of the title compound 3 has been inferred through IR, 1H/13C NMR, mass spectrometry, elemental analyses and co...

A novel series of N-arylbenzo[d]oxazol-2-amines (4a–4m) were synthesized and evaluated for their α-glucosidase inhibitory activity. Compounds 4f–4i, 4k and 4m displayed potent inhibitory activity against α-glucosidase with IC50 values in the range of 32.49 ± 0.17–120.24 ± 0.51 μM as comp...

The new synthesis of chiral and sterically hindered 1,2-amino alcohols derivatives of 2-methyl-indane and 1,2,3,4-tethrahydrophenanthrene based on cyclic enol phosphates were investigated. The desired products were obtained using three step procedure: oxidation of accessible enol phosphates, tra...

A diastereomeric mixture of racemic α-amino nitriles [1SR,2RS,(SR)]- (1) and [1SR,2RS,(RS)]-N-cyano(phenyl)methyl-1-aminoindan-2-ol (2) was thermally epimerized in the solid state to give diastereopure [1SR,2RS,(SR)]-1. The reaction was about 26 times slower than the same reaction of a mixture ...

Pseudomonas cepacia lipase (PSL) efficiently catalyses the kinetic resolution of (±)-cis- and (±)-trans-1-aminoindan-2-ol through the O-acylation reaction of the corresponding N-benzyloxycarbonyl derivative using vinyl acetate as the acyl donor. In a similar way, cis-N-Cbz-2-aminoindan-1-ol is...

SummaryThe transcription factor Max is a basic-helix-loop-helix leucine zipper (bHLHLZ) protein that forms homodimers or interacts with other bHLHLZ proteins, including Myc and Mxd proteins. Among this dynamic network of interactions, the Myc/Max heterodimer has crucial roles in regulating norma...

In filamentous ascomycetes, HOG-like signal transduction cascades are involved in the resistance to hyper-osmotic conditions and to dicarboximides and phenylpyrroles. The histidine kinase (HK) Bos1 and the mitogen-activated protein kinase (MAPK) Sak1 are important for the adaptation to hyper-osm...

Ethylene polymerization with linked amido-cyclopentadienyl or “constrained-geometry” titanium catalysts, Ti(η5:η1-C5Me4SiMe2NtBu)X2 (X=Me, Bz, Cl), activated by tritylpyridinium tetrakis(entafluorophenyl)borate, [Ph3C(NC5H5)] [B(C6F5)4], and silica-supported tritylpyridinium tetrakis(entaflu...

Fluorescent adenine mimetics are useful tools for studying DNA, RNA and enzyme functions. Herein we describe the synthesis of eight 1-(purinyl)triazoles and two 4-(purinyl)triazoles utilizing the 1,4-regioselective copper-catalyzed azide–alkyne cycloaddition (CuAAC) reaction as the key step. Th...

Publisher SummaryThis chapter addresses recent findings concerning the identity of the cysteine S-conjugate β-lyases in mammals, the reactions catalyzed by these enzymes, and the pharmacological aspects of the cysteine S-conjugate β-lyases are addressed. It also discusses β-elimination reacti...

The toxicity of most drugs and chemicals is associated with their enzymatic conversion to toxic metabolites. Bioactivation reactions occur in a range of organs and organelles, including mitochondria. The toxicity of haloalkene-derived cysteine S-conjugates and related 4-thiaalkanoates is associa...

Glutathione (γ-glutamyl-l-cysteinylglycine; GSH) is present in high concentrations in most living cells and participates in a variety of vital cellular reactions. In particular, GSH protects cells from potentially toxic electrophiles formed via the metabolism of xenobiotics, and such reactions ...

Brain efflux systems export such conjugated metabolites as glutathione (GSH) and glucuronate conjugates, generated by the detoxification process, from the brain and serve to protect the brain from harmful metabolites. The intracerebral injection of a radiolabeled conjugate is a useful technique ...

The aim of this work is to design, prepare and characterize l-lysine based prodrugs capable of targeting 6-mercaptopurine to the colon, an anti-tumor and immunosuppressant drug, and 5-aminosalicylic acid (5-ASA), drug of choice for inflammatory bowel disease (IBD). More specifically, Nɛ-feruloyl...

A series of trans-4-(6-substituted-9-purinyl) cyclohexylcarbinols were prepared by the following procedure. Ethyl p-aminobenzoate gave, on catalytic hydrogenation, trans-4-ethoxycarbonylcy clohexylamine which, on reduction with sodium and ethanol, generated trans-4-hydroxymethylcyclohexylamine. ...

The syntheses of cis-4-(6-chloro-9-purinyl)cyclohexylcarbinol (VI) and cis-3-(6-chloro-9-purinyl)cyclopentylcarbinol (XVII) have been accomplished by the condensation of 5-amino-4,6-dichloropyrimidine with the appropriate amino alcohol, followed by ring closure of the resultant substituted pyrim...