Acid-catalyzed dehydration of methyl and ethyl 2-methyl-5-(d-arabino-tetrahydroxybutyl)-3-furoate (4a, b) takes place preferentially with inversion of configuration at C-1′, yielding the corresponding 5-(1,4-anhydro-d-ribo-tetrahydroxybutyl)-2-methyl-3-furoate (6a, b), and, to a much smaller ex...

PurposeFirst-line treatment for patients with extensive-stage small cell lung cancer (SCLC) includes treatment with platinum-based combination chemotherapy. Amrubicin is a synthetic anthracycline with single-agent activity in relapsed/refractory SCLC. In an attempt to improve treatment efficacy,...

ObjectivesAmrubicin monotherapy is a treatment option for patients with relapsed small cell lung cancers (SCLCs). Topoisomerase-II (Topo-II) – a target of amrubicin – has been reported as a predictive or prognostic marker for chemosensitivity or outcomes in patients with various malignancies. ...

A series of multi-heterocyclic anti-bacterial drugs 3-(4-(tetrazol-1-yl)phenyl)-5-phenyl-1H-pyrazoles are synthesized using the reaction with (E)-1-(4-(1H-tetrazol-1-yl)phenyl)-3-arylprop-2-en-1-one and hydrazine hydrate in the presence of weak acidic catalyst like acetic acid. The structures of...

In this study, a 50-membered library of substituted 4-hydroxyquinolin-2(1H)-ones and two closely related analogues was designed, scored in-silico for drug likeness and subsequently synthesized. Thirteen derivatives, all sharing a common 3-phenyl substituent showed minimal inhibitory concentratio...

Two new series of diethyl 2-[2-(substituted-2-oxo-1,2-dihydroquinolin-4-yl)hydrazono]-succinates 6a-g and 1-(2-oxo-1,2-dihydroquinolin-4-yl)-1H-pyrazoles 7a-f have been designed and synthesized. The structures of the synthesized compounds were proved by IR, mass, NMR (2D) spectra and elemental a...

Metal-complexing agents (1,10-phenanthroline (OP), 8-hydroxyquinoline (OHQ), EDTA, and histidine) produce essential activation of yeast aldehyde dehydrogenase (E.C.1.2.1.5), like cysteine and BAL. The extent of enzyme activation varies according to the coenzyme structure. Diethyldithiocarbamate ...

Benzodiazepinones are privileged scaffolds with activity against multiple therapeutically relevant biological targets. In support of our ongoing studies around allosteric modulators of metabotropic glutamate receptors (mGlus) we required the multigram synthesis of a β-ketoester key intermediate...

3-Cyanopyridine-2(1H)-thiones have been shown to react with Biginelli-type ethyl 4-aryl-6-(bromomethyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates upon heating in DMF giving rise to ethyl 4-aryl-6-{[(3-cyanopyridin-2-yl)thio]methyl}-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates. The l...

Two high-performance liquid chromatography (HPLC) methods were developed for the determination of trecetilide in plasma samples. Differing only in the addition of a derivatization step and different detection wavelengths, the two methods encompassed a wide concentration range. In both methods, p...

ABSTRACTColistin is an antimicrobial peptide (AMP) used as a drug of last resort, although plasmid-mediated colistin resistance (MCR) has been reported. AA139 and SET-M33 are novel AMPs currently in development for the treatment of multidrug-resistant (MDR) Gram-negative bacterial infections. As...

Tracheal antimicrobial peptide (TAP) is a β-defensin produced by mucosal epithelial cells of cattle. Although effective against several human pathogens, the activity of this bovine peptide against the bacterial pathogens that cause bovine respiratory disease have not been reported. This study c...

The production of antimicrobial peptides is an important key of innate immunity. Tracheal antimicrobial peptide (TAP) expression has been reported in bovine tracheal epithelial cells and it can be modulated by bacterial infection or bacterial components. In mammary gland TAP expression has been ...

Respiratory disease is an important cause of morbidity and mortality in cetaceans, which are also threatened by environmental degradation caused by crude oil spills. Following oil spills, cetaceans at the water surface may inhale droplets of oil containing toxic polycyclic aromatic hydrocarbons ...

The σ54 promoter (P3) upstream of the pilE gene in Neisseria gonorrhoeae was shown to be non-functional by transcriptional analysis of a PpilE::lacZ fusion containing only P3. A region on the chromosome of N. gonorrhoeae strain MS11-A was identified that potentially encodes a protein with a sig...

The intracellular pathogen Brucella abortus has an alternative sigma factor σ54 (RpoN) highly similar to Sinorhizobium meliloti NtrA. RpoN was described to be required for the transcription of a wide range of genes involved in diverse physiological functions including the regulation of virulenc...

OprE is a channel-forming outer membrane protein of Pseudomonas aeruginosa, the expression of which is induced under anaerobic conditions. We constructed various mutants and observed the effects on oprE expression. Deficiency in RpoN, an alternative sigma factor for RNA polymerase, abolished opr...

SummaryIn response to environmental and other stresses, the σ54 subunit of bacterial RNA polymerase (RNAP) controls expression of several genes that play a significant role in the virulence of both plant and animal pathogens. Recruitment of σ54 to RNAP initiates promoter-specific transcription...

Sorghum procyanidins (SPC) tetramers were reported to have inhibitory effects on the adhesion of Streptococcus mutans (S. mutans), which is one of the primary pathogenic bacteria that cause caries. To make clear the mechanism underlying the inhibitory effects of SPC tetramers on the adhesion of ...

Publisher SummaryThis chapter discusses the application of the signal hypothesis to the incorporation of integral membrane proteins. Signal hypothesis is a proposed explanation of the biosynthesis of secreted polypeptides. It has become increasingly clear that much of the knowledge may be extend...