Pd(OAc)2/KOAc was found to be an efficient catalytic system for the direct arylation of thiophene and furan derivatives bearing an acrylate at C3. The selectivity of the reaction strongly depends on the nature of the coordinating base. Na2CO3 and Li2CO3 favours the Heck type reaction; whereas th...

This contribution investigates mechanistic and kinetic parameters pertinent to formation of mixed dibenzo-p-dioxins and dibenzofurans (PXDD/Fs) from the condensation reactions involving 2-chlorophenoxy (2-CPxy) and 2-bromophenoxy (2-BPxy) radicals. Keto-ether structures act as direct intermediat...

A novel and practical synthetic route for the preparation of candesartan cilexetil from methyl 2-amino-3-nitrobenzoate is described. The key steps are the reaction of methyl 2-bromo-3-(diethoxymethyleneamino)benzoate with (2′-(1-trityl-1H-tetrazol-5-yl) biphenyl-4-yl) methanamine and the final ...

2,3,3,3-Tetrafluoroprop-1-ene, known as the environmentally benign fluorinated olefin recently employed for the car air-conditioning system, was proved to follow the addition–elimination sequence at its C2 position by the reaction of a variety of alkoxides, forming CF3-containing vinyl ethers i...

Two new biphenyls characterized as 4-(3-methyl-but-2-enyl)-5-methoxy-[1,1′-biphenyl]-3-ol 1 and 2-carboxy-4-(3-methyl-but-2-enyl)-5-methoxy- [1,1′-biphenyl]-3-ol 5 have been isolated from Rhynchosia suaveolens. Both compounds displayed antibacterial activity.

Electrospray ionization-mass spectrometry (ESI-MS) was used to investigate stereoselective interactions between seven zwitterionic alkylsulfonate-modified cinchona alkaloid chiral selectors and biologically relevant lysine–alanine–alanine tripeptide and alanine–alanine dipeptide selectands in...

PurposeThe aim of this research work was to explore the possibility of providing multifunctional oral insulin delivery system by conjugating several types of dipeptides on chitosan and trimethyl chitosan to be used as drug carriers.

Bifidobacterium bifidum is a useful probiotic agent exhibiting health-promoting properties, and its peptidoglycans have the potential for applications in the fields of food science and medicine. We investigated the bifidobacterial alanine racemase, which is essential in the synthesis of d-alanin...

Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring. Of the four oxadiazoles known, 1,3,4-oxadiazole has become an important structural motif for the development of new drugs and the compounds containing 1,3,4-oxadiazole cores have a bro...

We synthesized methyl ester of N-(1-methylbut-2-en-1-yl)-N-phenylglycine which underwent acid catalyzed aromatic amino Claisen rearrangement to provide methyl-N-[2-(1-methylbut-2-en-1-yl)phenyl]glycinate. A mixture of syn- and anti-atropisomeric methyl-N-acetyl-N-[4-methyl-2-(1-methylbut-2-en-1-...

D-23129 [N-(2-amino-4-(4-fluorobenzylamino)phenyl)carbamic acid ethyl ester] and D-20443 (dihydrochloride of D-23129) are promising anticonvulsant compounds with a broad spectrum activity in animal models of epilepsy. Their effects on de novo synthesis of excitatory (glutamate and aspartate) and...

Cefcapene pivoxil hydrochloride (CFPN-PI), an ester cephem antibiotic, was orally given at a dose of 100mg three times daily in patients with infection and soft stool or diarrhea, and its absorption was determined using the recovery ratio of 12-h urine pooled after the initial administration as ...

Simple, rapid and specific liquid chromatography–mass spectrometry (LC–MS) methods have been developed and validated for the quantification of cefcapene acid in human plasma and urine. Plasma samples were simply pretreated with methanol for deproteinization. Urine samples were briefly diluted ...

In order to compare the bacteriological and clinical efficacy and safety of cefcapene-pivoxil (CFPN-PI) for 5 days, CFPN-PI for 10 days, and amoxicillin (AMPC) for 10 days for the treatment of pharyngitis due to group A β-hemolytic streptococcus (GAS) in children, a prospective multicenter rand...

To investigate the effects of gastrectomy on the absorption of drugs, the blood concentrations of the active moieties, cefcapene (CCAP) and ceftizoxime (CTIZ), were determined in 36 gastrectomized patients after oral administration of cefcapene pivoxil (CCAP-PI) and AS-924, prodrug type cephem a...

Isolated pituitary neurointermediate lobes from adult male Sprague-Dawley rats were incubated for up to 90 minutes in media containing stimulatory or inhibitory agents, to study the potential effects on secretion of alpha-melanocyte stimulating hormone (α-MSH) from the pars intermedia. Dopamine...

A new piperazine-based dicationic Brönsted acidic ionic salt named as piperazine-1,4-diium dihydrogen phosphate was prepared. After characterization by FT-IR, Mass and NMR spectroscopy, it was used as an efficient and reusable catalyst for the synthesis of 5-arylidenepyrimidine-2,4,6(1H,3H,5H)-t...

Different series of novel pyrazole and pyrazolo[1,5-a] pyrimidine derivatives (2a-g), (3a-c), (7a-d) and (10a-e) were designed, synthesized and evaluated for their ability to inhibit CDK2/cyclin A2 enzyme in vitro. In addition, the cytotoxicity of the newly synthesized compounds was screened aga...

Two cyclometalated alkynylgold(III) complexes [AuCl(tpy)(C≡C–C6H4CH3)] (1) and [AuCl(ppy)(C≡C–C6H4CH3)] (2), where ppy = 2-phenylpyridine and tpy = 2-(p-tolyl)-pyridine, were successfully synthetized. Their photophysical properties were investigated by absorption and photoluminescence spectr...

The quenching of fluorescence of 2-(4′-t-butylphenyl)-5-(4′′-biphenylyl)-1,3,4-oxadiazole (BPBD) has been studied by aniline in different solvent mixtures of benzene and acetonitrile at room temperature. The quenching is found to be appreciable and a positive deviation from linearity was obse...