In a separate study on the orally active acyloxymethyl esters(1)of 7{2一(2-aminothiazol4-yl)acetamido}3一[[[1一(2-dimethylaminoethy1)一1H-tetrazol-5-y1】thio]methyl]ceph-3-em-4-carboxylic acid(cefotiam, CTM), we have shown, by quantitative structure-oral bioavailability (BA)relation analysis, that the R2 group in the acyl group R2CO must have both an adequate lipophilicity(HANscH's lipophilic parame...

1. Gray CH, Urn CK, Nicholson DC. The differentiation of the porphyrins by means of high pressure liquid chromatography. Clin Chim Acta 77, 167-178 (1977). 2. Doss M. Analytical and preparative thinlayer chromatography of porphyrin methyl esters. Z Kiln Chem Kiln Biochem 8, 197207 (1970). 3. Straka JG, Kushner, JP, Burnham BF. High-performance liquid chromatography of porphyrin esters. Identifi...

WITH THE growing interest in the metabolism of cholesterol esters, procedures have been developed which frequently make desirable the use of chemically pure compounds. Some of the radioactive cholesterol esters are either commercially unavailable or expensive when made to order. The high cost of the starting materials (cholesterol-4-CI4, pure fatty acids) makes it desirable to have a good yield...

The hydrolysis of cholesteryl esters contained in plasma low density lipoprotein was reduced in cultured fibroblasts derived from a patient with cholesteryl ester storage disease, an inborn error of metabolism in which lysosomal acid lipase activity is deficient. While these mutant cells showed a normal ability to bind low density lipoprotein at its high affinity cell surface receptor site, to ...

1. The flavonoid constituents o f Flaveria bidentis have been identified as the 3-O-glucosides of kaempferol, 6 -m ethoxykaem pferol and 6 -methoxyquercetin (patuletin), as well as six flavonol sulfate esters belonging to quercetin and isorhamnetin. The two latter glucosides are reported here for the first time in this species; whereas quercetin-3,7-disulfate, is a novel compound from nature. 2...

The etiologic agent(s) that was responsible for the 1981 toxic oil syndrome [TOS] epidemic in Spain has not been identified. Liquid chromatography combined with atmospheric pressure ionization tandem mass spectrometry was used for the analysis of oils associated with TOS. Analyses focused on measuring 3-(N-phenylamino)-1,2-propanediol [PAP], the 3-oleyl ester of PAP [MEPAP], and the 1,2-di-oley...

Phthalic acid esters are presently being used in amounts and products that can easily, although inadvertently, contribute to environmental pollution. As plasticizers, phthalic acid esters are added to synthetic plastic resins to impart flexibility to the finished product, improve workability during fabrication, and extend or modify properties not present in the original resins (1). Plastic form...

Reaction of the sulfuric acid ester of /V-hydroxy-4acetylaminobiphenyl and of the acetic acid esters of /V-hydroxy-4-acetylaminobiphenyl, /V-hydroxy-4-acetylaminostilbene, and /V-hydroxy-2-acetylaminophenanthrene with transforming DNA of Bacillus subtilis in vitro caused both inactivation of transforming activity and the induction of mutations. The parent amides, amines, /V-hydroxy amides, and ...

9-(S)-[3-Hydroxy-2-(phosphonomethoxy)propyl]adenine [(S)-HPMPA] has been reported to have antischistosomal activity. Ether lipid esters of (S)-HPMPA and cidofovir (CDV) have greatly increased activities in antiviral assays and in lethal animal models of poxvirus diseases. To see if ether lipid esters of CDV and (S)-HPMPA enhance antischistosomal activity, we tested their alkoxyalkyl esters usin...

The bacterial phosphotriesterase has been shown to catalyze the stereoselective hydrolysis of phosphinate esters. The wild-type enzyme preferentially hydrolyzes the SP-enantiomers of methyl phenyl p-X-phenylphosphinate esters by 3 orders of magnitude. The mutant enzyme, I106T/F132A/H254G/H257W, exhibits the opposite stereoselectivity and hydrolyzes the RP-enantiomer up to 30 times faster than t...