The mammary carcinogenicity of two diol epoxide metabolites of the commonly occurring environmental carcinogen benzo[j]fluoranthene (BjF) was investigated by direct application to the tissue beneath the mammary glands of female CD rats. The compounds tested were trans-4,5-dihydroxy-anti-6,6a-epo...

Benzo[b]fluoranthene and 4-, 5-, 6-, and 7-fluorobenzo[b]fluoranthene were evaluated for tumor-initiating activity in mouse skin. These fluorinated benzo[b]fluoranthene derivatives were assayed at doses of 400, 120, 40, and 10 nmol per mouse. Similar tumorigenic activity was observed for benzo[b...

[4S-(4I,7I,10aJ)]1-Octahydro-5-oxo-4-[phenylmethoxy)carbonyl]amino]-7H-pyrido-[2,1-b] [1,3]thiazepine-7-carboxylic acid methyl ester (BMS-199541-01) is a key chiral intermediate for the synthesis of Omapatrilat (BMS-186716), a new vasopeptidease inhibitor under development. By using a selective ...

For the purpose of developing novel EGFR/HER2 tyrosine kinases inhibitors with high inhibition activity and low toxicity, two novel series of oxazolo[4,5-g]quinazolin-2(1H)-one derivatives as EGFR/HER2 dual inhibitors introducing two electrophiles 2-(2-bromoacetyl)ethyl and 2-(2-chloroacetoxy)et...

A gas chromatographic method for the determination of oxpentifylline and a metabolite, 1-(5′-hydroxyhexyl)-3,7-dimethylxanthine is described. Oxpentifylline, metabolite and internal standard are extracted from basified plasma into dichloromethane, then the metabolite and internal standard are c...

Previously untreated patients with smear-positive pulmonary tuberculosis were randomly allocated to treatment with 600, 300, 150 or 75 mg doses of rifabutin (LM427, ansamycin), 600, 300 or 150 mg of rifampicin, 300 mg isoniazid or to no drug daily for 2 days. The fall in viable counts of Mycobac...

A specific, precise and accurate assay for determination of rifabutin in human plasma using Extrelut column extraction was developed and validated. Rifabutin concentrations were calculated with a standard curve ranging from 5 to 800 ng ml−1, using a split-curve approach. Chromatographic peaks we...

A simple, specific and sensitive high-performance liquid chromatographic (HPLC) method was developed for the determination of rifabutin in human plasma. Rifabutin and sulindac (internal standard) are extracted from human plasma using a C8 Bond Elut extraction column. Methanol (1 ml) is used to e...

BackgroundThis series of studies examines the pharmacokinetic/pharmacodynamic interactions between buprenorphine, an opioid partial agonist increasingly used in treatment of opioid dependence, and rifampin, a medication used as a first line treatment for tuberculosis; or rifabutin, an alternativ...

A novel assay using high pressure liquid chromatography (HPLC) coupled to mass spectrometer (MS) detection was developed and validated for the rifamycin anti-tuberculosis antibiotics rifampicin (RIF), rifabutin (RBT), rifapentine (RPT) and their active desacetyl metabolites (dRIF, dRBT and dRPT,...

Rifabutin, an anti-mycobacterial agent, is reported to be extensively metabolized in vivo into more than 20 biotransformation products, with similar profile both in humans and rats. Among the metabolites formed, only seven have been characterized, the remaining are unknown. Hence, the purpose of...

A series of novel substituted 1-[bis(4-fluorophenyl)-methyl]piperazine derivatives (4a–g) and (5h–m) have been synthesized. The synthesized compounds were characterized by IR and 1H NMR. All the synthesized compounds were evaluated in vitro for their efficacy as antimicrobial agents against re...

Five novel antimony(III) complexes with the mono- and bis(thiosemicarbazone) ligands of 2N1S or 4N2S donor atoms, N′-[1-(2-pyridyl)ethylidene]morpholine-4-carbothiohydrazide (Hmtsc, L1) and bis[N′-[1-(2-pyridyl)ethylidene]]-1,4-piperazinedicarbothiohydrazide (H2ptsc, L7), and the tridentate se...

The Schiff base methyl 2-pyridyl ketone semicarbazone (HL) was prepared from the condensation of methyl 2-pyridyl ketone and semicarbazide, and used in the synthesis of a series of novel binuclear Cu(II) complexes with three distinct bridging ligands: [Cu(L)(μ1,1-N3)]2 (1), [Cu(L)(μS,N-SCN)]2 ...

The aim of this study was to identify a candidate drug for the development of anti-tuberculosis therapy from previously synthesized compounds based on the thiosemicarbazones, semicarbazones, dithiocarbazates and hydrazide/hydrazones compounds. The minimal inhibitory concentration (MIC) of these ...

A new nano-structured Mn(II) coordination polymer [Mn(HL)(dca)(Cl)]n (1), [HL= Pyridine-2-carbaldehyde semicarbazone, dca= dicyanamide] has been synthesized by a sonochemical method and has been characterized by scanning electron microscopy, X-ray powder diffraction elemental analysis and IR spe...

An unprecedented cobalt(III) compound with methyl 2-pyridyl ketone semicarbazone (HL) and the auxiliary azide ligand, [Co(L)2] [Co(L)(N3)3] (1) was synthesized and further characterized crystallographically and spectroscopically. Compound 1 crystallizes in the triclinic system and space group of...

A new inorganic–organic nanohybrid based on a Keggin-type polyoxomolybdate and a copper(II) semicarbazone complex, namely [Cu2(HL)2(PMo12O40)(OCH3)2(Cl)(H2O)]·8CH3OH·4H2O [HL = pyridine-2-carbaldehyde semicarbazone] (1) was synthesized by a sonochemical method. Single crystals of 1 were synth...

Substituted semicarbazones/thiosemicarbazones and their copper complexes have been prepared and several single crystal structures examined. The copper complexes of these semicarbazone/thiosemicarbazones were prepared and several crystal structures examined. The single crystal X-ray structure of ...

The 4-O-methyl-D-glucuronic acid groups attached to xylose chains in wood xylan can form uronate salts with alkali and alkaline earth metal cations. These uronic acid and metal uronate moieties may act as acid and base catalysts, respectively, during xylan pyrolysis. In this study, commercial be...