Background:Use of the combination of an angiotensinconverting enzyme inhibitor (ACEI) and a calcium channel blocker (CCB) is considered a rational approach in patients whose hypertension is not controlled by monotherapy, providing better blood pressure (BP) control than the individual components...

Background: The fixed combination of the angiotensin-converting enzyme (ACE) inhibitor delapril and the dihydropyridine calcium channel blocker manidipine is a new oral, QD antihypertensive regimen that may have a role in the management of hypertension in patients with diabetes mellitus (DM).Obj...

This 12-month, multicenter, randomized, parallel-group study compared the effects of delapril with enalapril in 179 patients with congestive heart failure, New York Heart Association (NYHA) classes II and III. The initial doses of delapril (7.5 mg twice daily [BID]) and enalapril (2.5 mg BID) co...

The present study describes the development and validation of a dissolution method for delapril (DEL) and manidipine (MAN) combination tablets, using a simulated absorption profile based on in vivo data for MAN. The suitable in vitro dissolution profile for this formulation was obtained using 90...

Diethyl (2R,3R)-(−)-oxirane-2,3-dicarboxylate was converted into diethyl (2S,3S)-(+)-aziridine-2,3-dicarboxylate in two steps, viz. ring opening with trimethylsilyl azide in N,N-dimethylformamide containing one equivalent of ethanol, followed by treatment with triphenylphosphine in N,N-dimethylf...

The reduction of ethyl 2-methyl-3-oxobutanoate catalyzed by an oxidoreductase from Geotrichum candidum affords corresponding ethyl (2S,3S)-anti-2-methyl-3-hydroxybutanoate with exclusive diastereo- and enantioselectivity.

Applications of phase transfer catalysts in etherification reaction of benzyl chloride with furfuryl alcohol in the L-L-L tri-phasic system was investigated. Comparison between the L-L bi-phase system and L-L-L tri-phase system was studied to achieve significant conversion, better selectivity, a...

There is an urgent need for new antimalarial drugs with novel mechanisms of action on novel targets. Indolone-N-oxides (INODs) display antimalarial properties in vitro and in vivo, but identified leads such as 6-(4-chloro-phenyl)-5-oxy-[1,3]dioxolo[4,5-f]indol-7-one 1, suffer from very poor aque...

Fourteen prodrugs of the antitumor agent 3-[(3-amino-4-methoxy)phenyl]-2-(3,4,5-trimethoxyphenyl)cyclopent-2-ene-1-one (1) were prepared to improve its water solubility and potency. These prodrugs include α-amino acid (1a–1h), aliphatic amino acid (1i–1l), phosphoramidate (1m), and phosphate ...

The purpose of this research is to investigate the viability and efficiency of 2-[(E)-[5-methoxy-1-[4-(trifluoromethyl)phenyl]pentylidene]amino]oxyethanamine (MPPOE) as a non-toxic organic inhibitor of mild steel corrosion in oilfield acidizing environment at simulated surface to down-hole tempe...

The interaction between the veterinary drug sodium sulphadimidine and nitrite has been studied under acid conditions and the formation of 1,3-di-(4-[N-(4,6-dimethyl-2-pyrimidinyl)sulphamoylphenyl)triazene (DDPSPT) was demonstrated. This compound was not mutagenic when tested on Salmonella typhim...

A new f-nitroso compound identified in a nitrosated tea extract made from the plant Ephedra altissima and shown to be formed under in vivo conditions was identified as 2-(N-nitroso-N-methylamino)propiophenone (NMAP). N-Nitrosoephedrine (NEP), another N-nitroso compound detected in nitrosated Eph...

ABSTRACTWe evaluated the anti-asthmatic effects and mechanism of action of TMK-688, a potent 5-lipoxygenase inhibitor, on the dual-phase asthmatic response and on airway inflammation in conscious guinea pigs sensitized with ovalbumin (OA). TMK-688 inhibited both the immediate and the late asthma...

The effects of an oral anti-allergic agent, TMK-688, which inhibits 5-lipoxygenase, at doses of 3.2 and 10 mg/kg were studied in guinea pigs with dual-phase asthmatic response. We previously observed that pretreatment with TMK-688 inhibited the late asthmatic response (LAR) induced by ovalbumin ...

As part of the Department of Health and Human Services's (DHHS's) responsibility for the oversight of safety and health during the destruction of obsolete chemical warfare munitions and agent stockpiles by the Department of Defense (DOD), investigators from the National Institute for O...

A solid-phase microextraction (SPME) and gas chromatography–mass spectrometry (GC–MS) sampling and analysis method was developed for bis(diisopropylaminoethyl)disulfide (a degradation product of the nerve agent VX) in soil. A 30-min sampling time with a polydimethylsiloxane-coated fiber and hi...

The determination of the nerve agent O-ethyl S-2-diisopropylaminoethyl methylphosphonothioate (VX) by thermospray liquid chromatography—mass spectrometry was studied. The solvent system acetonitrile—methanol—0.25 M ammonium acetate was used on a reversed-phase C18 column. By selected ion moni...

The chemical warfare agent O-ethyl S-(2-diisopropylaminoethyl) methyl phosphonothiolate (VX) and many related degradation products produce poorly diagnostic electron ionization (EI) mass spectra by transmission quadrupole mass spectrometry. Thus, chemical ionization (CI) is often used for these ...

In the present work, Manganese (II) Titanium Oxide nanoparticles (MnTiO3-NPs) were dispersed in a room temperature nematic liquid crystal 4-(trans-4′-n-hexylcyclohexyl) isothiocyanatobenzene (6CHBT) at the concentrations of 0.5 wt% and 1 wt% and their thermodynamic, optical and dielectric prope...

Poly (linolenic acid)-g-poly (caprolactone)-g-poly (t-butyl acrylate) (PLilPCLPtBA) graft copolymer was used as an interfacial layer in Au/n-Si Schottky diode. The novel PLilPCLPtBA layer was coated on n-Si single crystal wafer through an electrospinning system. Nanofiber characteristics of the ...