The synthesis and in vitro antibacterial activity of 7β-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]cephalosporins bearing N-mono or dialkyl and carbamoyl aminopyrazolium, and five- or six-membered rings fused to the 3-aminopyrazolium methyl groups at the 3-position, are described. Ami...

Quinones, precursors of aromatic structures, were firstly employed as the electrophiles for the organocatalytic Michael addition/cyclization cascade reaction with versatile 3-isothiocyanato oxindoles. Chiral bifunctional organocatalyst was appropriate for this enantioselective transformation to ...

The parkinsonian inducing agent 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and its corresponding five-membered ring analogue 1-methyl-3-phenyl-3-pyrroline are cyclic tertiary allylamines and good substrates of monoamine oxidase B (MAO-B). The MAO-B catalyzed 2-electron α-carbon oxidati...

A general method for formulating complex thermodynamic systems in terms of hierarchical interactions has been developed, and has been applied in a previous analyses to the theoretical analysis of cooperativity in a dimeric protein, to the statistical analysis of hemoglobin oxygen binding data, a...

This study was designed to examine the potential structure–activity relationship between carboxylic acids, histone acetylation and T cell cycle blockade. Toward this goal a series of structural homologues of the short-chain carboxylic acid n-butyrate were studied for their ability to block the ...

A new method for quantification of short chain C1–C6 carboxylic acids in vegetable oils and fats by employing Liquid Chromatography Mass Spectrometry (LC–MS) has been developed. The method requires minor sample preparation and applies non-conventional Electrospray Ionization (ESI) liquid phase...

Recently, concerns have been raised that residues of glyphosate-based herbicides may interfere with the homeostasis of the intestinal bacterial community and thereby affect the health of humans or animals. The biochemical pathway for aromatic amino acid synthesis (Shikimate pathway), which is sp...

The emergence of various drug-resistant Mycobacterium tuberculosis (Mtb) strains has necessitated the exploration of new drugs that lack cross-resistance with existing therapeutics. By screening the MedChemExpress bioactive compound library, ceritinib was identified as a compound with activity a...

Checkpoint kinase 1 (CHK1) inhibitors can potentiate the effectiveness of deoxyribonucleic acid (DNA) damaging agents in the treatment of cancer. A novel series of 2,6-disubstituted-9H-purine (3a-p, 5a and 5b), 2,4-disubstituted-thieno[3,2-d]pyrimidine (8a-c) and 2,4-disbustituted-7H-pyrrolo[2,3...

Using 2-(2,4-difluorophenyl)-4-(trifluoromethyl)pyrimidine as main ligand and tetraphenylimidodiphosphinate as ancillary ligand, one iridium complex was synthesized. This complex shows a green emission peaking at 543 nm with a quantum efficiency yield as 48% in deareated CH2Cl2 solution. It also...

The increasing incidences of multidrug resistant bacterial infections urge the development of novel antibacterial having a new mechanism of action. The small molecule-based inhibitors targeting at the cell division protein FtsZ has been recognized as a promising approach to search for new antiba...

SIB-1553A ((±)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thiophenol HCl) is a neuronal nicotinic acetylcholine receptor (nAChR) ligand which is active in rodent and primate models of cognition. In functional assays, SIB-1553A exhibits marked subtype selectivity for nAChRs as compared to nicotine. In ...

A simple quantitative structure–activity relationship (QSAR) method of analysis used to predict biological activity for congeneric series of compounds is reported. This method is based on the application of bilinear or multilinear partial least squares regression to a data set, which is a binar...

Publisher SummaryThis chapter discusses the preparation and properties of β–glucuronidase. All mammalian tissues contain a group-specific enzyme that catalyzes the hydrolysis of the biosynthetic β-D-glucopyranosiduronic acids of all types to the aglycons and D-glucuronic acid. This enzyme is ...

1-deoxynojirimycin was used for the treatment of type II diabetes. However, due to its poor water solubility and low oral bioavailability, clinical application was limited. This study aimed to prepare controlled release matrix pellets of 1-deoxynojirimycin to enhance its oral bioavailability. Th...

Seven methyl and/or ethyl esters of carboxylic acids (CH2CH2C(O)OEt, CH2CH2CH2C(O)OMe, CH2CH2CH2C(O)OEt, CH(C2H5)C(O)OMe, CH(n-C3H7)C(O)OMe, CH2CH2CH2CH2C(O)OEt and CH2CH2CH2CH2CH2C(O)OEt) having a morpholino group were subjected to electrochemical fluorination (ECF). On ECF, the c...

A set of isomeric para- and meta-trimethylsilylphenyl ortho-substituted N,N-phenyl α-diimine ligands [(Ar–NC(Me)–(Me)CN–Ar) Ar=2,6-di(4-trimethylsilylphenyl)phenyl (16); Ar=2,6-di(3-trimethylsilylphenyl)phenyl (17)] have been synthesized through a two-step procedure. The palladium-cataly...

SnCl4 acts primarily as an oxidant and oxidizes monolithium bis(trimethylsilyl) hydrazide 1 to mainly bis(trimethylsilyl)amine, BSA and tris(trimethylsilyl)hydrazine, TrSH and itself get reduced to SnCl2. Similarly, reaction of SnCl4 with dilithiumbis(trimethylsilyl) hydrazide 2, oxidizes it to ...

The reaction of diphenylketene with tris(trimethylsilyl)silyllithium, followed by hydrolysis of the mixture afforded 2,2-diphenyl-1-trimethylsiloxy-1-[bis(trimethylsilyl)silyl]ethene (1) in 78% yield. Treatment of the silyllithium adduct with chlorotrimethylsilane produced 2,2-diphenyl-1-trimeth...

In exploring the suitability of tetraborylmethane precursors as C4− synthons, we have studied the limits of stepwise trimethylsilyl and trimethylgermyl substitutions on tetrakis (1,3-propanediolatoboryl)methane. In contrast to previous reports indicating minimal silylation of tetraborylmethanes,...