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PubMed1961

Ross' azo mustard.

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Azo Compounds↗
PubMedDate not supplied

Role of Nad(P)h: quinone oxidoreductase in the regulation of intracellular redox state.

This paper is a brief overview of current knowledge about DT-diaphorase [NAD(P)H: Quinone Oxidoreductase, NQO], flavoprotein that catalyzes the obligatory two-electron reduction of a wide variety of substrates. The most efficient substrates are quinones but the enzyme will also reduce quinone-imines, nitro and azo compounds. NQO is unique among known NAD(P)H-oxidizing flavoproteins in being a 2-electron transferring quinone reductase, and play a major role in preventing one-electron reduction of exogenous quinones by other enzymes to auto-oxidable semiquinones and concomitant superoxide-radical generation. Induction of NQO by a variety of xenobiotics (potential sources of free-radical formation which lead to DNA and cell damage) provides protection from the cytotoxic and carcinogenic effects of these compounds. NQO has an important role in the bioreductive activation of various quinones used in cancer chemotherapy.

Animals↗
PubMed2001

FP-21399 (Lexigen Pharmaceuticals).

Lexigen (formerly Fuji ImmunoPharmaceuticals) is developing FP-21399, a bis-azo compound, for the potential treatment of HIV infections. By March 1998, a phase II clinical study had been initiated to explore the immunologic and virologic activity of the compound. In the phase II study, the compound was being administered once a month for 48 weeks to 40 patients who are failing on protease inhibitor regimens either alone or with the antiretrovirals currently being taken by the patients. In a previous phase II study conducted by the company, researchers observed hints of a cellular immune response in a small subset of subjects at risk for disease progression or development of opportunistic infections [310177]. Phase I clinical trials commenced in the US in 1995 [178794]. In a small 21-patient phase I dose escalation trial of intravenous FP-21399, 13 patients with baseline CD4 cell counts between 50 and 400 received infusions of various doses (1,2 or 3 mg/kg) of the compound once a week for four weeks. The compound was well-tolerated and 9 patients showed an increase in CD4 count of at least 15% over their baseline values, 2 showed a decrease in viral load of 1 log (90%), and 2 went from low viral loads to below the limit of quantification [310771,310177]. FP-21399 has been reported to interfere with the ability of the HIV envelope glycoproteins to use CXCR4 and CCR5 as co-receptors when entering CD4 cells. It concentrates in the lymph nodes, which are important viral reservoirs. In addition, the drug has demonstrated antiviral activity against many clinical and laboratory strains of HIV, including those that are AZT-resistant [310177]. FP-21399 was selected via a screening program of Fuji's compounds developed originally for photographic use. It has been demonstrated, in preclinical studies, that FP-21399 inhibits HIV entry to the target cell by interfering with the V3 loop of the viral envelope. The compound has the advantage that it has lower toxicity than reverse transcriptase inhibitors because it does not enter the cells [178794].

Journal Article↗
PubMed1991

[New salicylic acid derivatives in the treatment of inflammatory intestinal diseases].

Drug therapy for inflammatory bowel disease was limited for many years to sulfasalazine and some corticosteroids. Since the discovery that 5-aminosalicylic acid (5-ASA) is the active moiety of sulphasalazine in the treatment of chronic inflammatory bowel disease, several new drugs have been developed. These consist either of slow- or delayed-release formulations of plaint 5-ASA (mesalazin) or sulpha-free azo-compounds of 5-ASA. The varying bioavailabilities of the different formulations and compounds make it possible to use them alternatively in different clinical situations. A review of the literature is given and suggestions as to how the new drugs can be used in different diseases.

Aminosalicylic Acids↗
PubMed1989

One-step protocol for assays of total and direct bilirubin with stable combined reagents.

We describe an improved colorimetric method for assays of total and direct bilirubin in serum. Bilirubin reacts with diazotized sulfanilic acid in an acidic medium to form a blue azopigment. Total bilirubin is assayed in the presence of reaction accelerators (caffeine, urea, and citric acid), direct bilirubin in their absence. The azo compound so formed is read at the same wavelength (570 nm) in both assays. A sample blank is run in parallel. Standard curves are linear for total and direct bilirubin concentrations up to 513.0 and 256.5 mumol/L, respectively. The method is characterized by (a) use of the same protocol for both assays, i.e., a one-step procedure with short reaction time (5 min at room temperature), and (b) use of a single working solution, which, refrigerated, is stable for one month. The method is reliable, yields results that compare closely with those of the classical Jendrassik--Gróf method, is suitable for routine use, and lends itself to automation.

Bilirubin↗
PubMedDate not supplied

Liquid chromatographic determination of 2,4-dinitroaniline and 2-naphthol in D&C Orange No. 17.

A method is described for the determination of the intermediates in D&C Orange No. 17 by reverse phase liquid chromatography. The pigment is dissolved in boiling dioxane and then precipitated. The filtrate is chromatographed by isocratic elution, which is followed by a wash and equilibration. Peak area calibrations were linear. At the provisional specification levels, 99% prediction limits were 0.200 +/- 0.0012% 2,4-dinitroaniline (2,4-DNA) and 0.200 +/- 0.006% 2-naphthol. The limits of determination were 0.0023% for 2,4-DNA and 0.013% for 2-naphthol at the 99.5% confidence level. Recoveries were 98-100% for 2,4-DNA added at the 0.005-2% level, and 93-103% for 2-naphthol added at the 0.025-2% level. A survey of certified D&C Orange No. 17 samples showed that the lots contained higher levels of the intermediates than were determined previously by a cellulose column method, in which the pigment is not dissolved.

Aniline Compounds↗