[Reactions of benzylcarbonyl compounds with formamide. X. On alpha-acyl-alpha-naphthylacetonitriles (author's transl)].
Explore the source record for details and available documents.
SEARCH · Search PubMed
Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.
Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.
Explore the source record for details and available documents.
In order to prepare an immunogen for enzyme immunoassay of 3 beta-(monoglucuron-1'-beta-yl)-18 beta-glycyrrhetic acid (3MGA), which was isolated from a patient with glycyrrhizin-induced pseudoaldosteronisms, benzyl glycyrrhetate (3) was allowed to react with an acetobromosugar (2) in the presence of silver carbonate to give benzyl 3 beta-(methyl 2',3',4'-triacetyl-glucuron-1' beta-yl)-glycyrrhetate (5) and methyl 3',4'-diacetyl-alpha-1',2'-O-[1-(benzyl glycyrrhet-3 beta-yl)- ethylidene]-D-glucuronate (4). On the other hand, this reaction was carried out in the presence of mercuric cyanide in nitromethane to give compound 5, benzyl 3 beta-acetyl glycyrrhetate (6) and benzyl 11-oxo-A-neooleana-3(5),12-dien-3-oate (7). 4-Aminomethylcyclohexanecarboxylic acid and glycine were introduced as chemical bridges at C-30 of 3 beta-(tert-butylglucuron-1' beta-yl)-glycyrrhetic acid (11) derived from compound 5. The former bridge was used to prepare an immunogenic conjugate with bovine serum albumin, and the latter bridge was used for antigen labelled with beta-galactosidase.
4CMB was tested in 7 mouse micronucleus assays (3 i.p., 2 oral, 1 s.c., 1 foetal), 2 mouse sperm-head morphology assays (1 i.p., 1 s.c.), 1 dominant lethal test in mouse (oral), 3 SLRL tests in Drosophila (2 feeding, 1 injection) and one somatic cell segregation assay in Drosophila (feeding). 4HMB was tested in 4 mouse micronucleus assays (2 i.p., 1 oral, 1 s.c.), 2 mouse sperm morphology assays (1 i.p. and 1 s.c.). 1 SLRL test and 1 somatic cell segregation assay in Drosophila (both feeding). BC was tested in 4 mouse micronucleus assays (2 i.p., 2 oral, 1 s.c.), 2 sperm-morphology assays (1 i.p., 1 s.c.), 2 SLRL tests and 1 somatic cell segregation assay in Drosophila (all feeding). All the mouse assays gave negative results with all 3 compounds. The response of 4CMB and BC was not reproducible when tested under similar conditions in the SLRL test in Drosophila. All 3 compounds gave a positive response in the somatic cell segregation assay in Drosophila.
A comparative study on biodegradation of di-cumyl peroxide (DCP) crosslinked and uncrosslinked natural rubber by Pseudomonas sp. was carried out. Decrease in organic carbon content along with the changes in tensile strength of the treated rubber, both DCP crosslinked and uncrosslinked natural rubber, indicated rubber hydrocarbon utilization by the Pseudomonas sp. A decrease in 60.88% MPa and 41.66% MPa was observed after five month's old treated uncrosslinked natural rubber and DCP crosslinked rubber, respectively. Biodegradation was more pronounced in natural uncrosslinked rubber, which was further confirmed by the formation of aldehydic compounds with decrease in CH2 stretching frequencies.
Nutmeg (Myristica fragrans) is used in food preparations for its aromatic flavor. The present investigation was undertaken to evaluate the antibacterial activity of constituents of M. fragrans seeds. Seeds of M. fragrans were powdered and extracted with chloroform to obtain trimyristin, which on saponification yielded myristic acid. The mother liquor remaining after separation of trimyristin was concentrated and column-chromatographed with petroleum ether to separate myristicin. Antibacterial activity of these isolated constituents was evaluated by determination of minimum inhibitory concentration against selected Gram-positive and Gram-negative organisms. All the constituents isolated from nutmeg exhibited good antibacterial activity. This study shows the potential of natural compounds in replacement of synthetic preservatives.
OBJECTIVE: To analyze the constituents of the essential oils extracted from nine samples of commercial seeds of Myristica fragrans Houtt respectively and to provide qualities control foundations. METHOD: Water steam distillation and GC-MS were used. RESULT: 95-118 compounds were separated respectively. 79 Compounds being identified which were 95.18%-98.70% of the total essential oil. CONCLUSION: Myristicin (39.63%) and terpene series were the main compounds.
Lipophilic analogues of trimethoprim (1) bearing 3,5-dialkyl-4-hydroxy substituents in the benzene ring are much more active in vitro against Neisseria gonorrhoeae than is 1. The 3,5-diisopropyl-4-hydroxy derivative (2) was selected as a candidate for clinical evaluation as an antigonococcal agent, and as part of the preliminary evaluation it was submitted to extended pharmacokinetic and metabolism studies in dogs. Although the compound was not extensively conjugated by metabolic enzymes, one of the methyl groups was metabolized to produce a 3-isopropyl-4-hydroxy-5-(alpha-carboxyethyl)benzyl derivative (43), which was rapidly excreted. Related analogues were likewise extensively metabolized.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
A diffusion cell type which is suitable for investigation of water-insoluble compounds is shown. The chamber consists of two compartments, the so-called bottom-chamber, which contains the solid substance under investigation, and the main chamber, which is above it. In this chamber only the dissolved part of the substance is present. The solubility of dibenzylsulfide was determined and it was demonstrated that the dissolved part of this compound is accumulated by a receptor substance from the liquid phase.
Explore the source record for details and available documents.
Members of a group of substituted 9-benzyladenines have been identified as effective inhibitors of inflammatory aspects of the delayed hypersensitivity skin reaction in the guinea-pig. Inhibitory activity was demonstrable in the efferent arc of the cell-mediated tuberculin and contact dermatitis (2,4-dinitrochlorobenzene) reactions. One of the compounds, 2-amino-9-benzyladenine, inhibited both turpentine-induced and histamine-induced inflammation in the skin. The toxicity and inhibitory activities of some of these compounds are discussed, and reference is made to the structurally related mercaptopurines.
In order to investigate the stereochemical requirements of planar structure at 4-position of 4-phenyl-1-arylsulfonylimidazolidinones (1) for their cytoxicities against human cancer cell lines, the size, the distance from imidazolidinone ring, and the conformation of this moiety were variegated. Replacement of phenyl moiety with naphthyl in compounds 2 and 3 or benzyl moiety in compound 4 sharply reduced activity of 1. Conformational restriction on phenyl ring in compound 5 also resulted in the loss of activity of 1. Therefore, phenyl moiety without any substituents directly attached to imidazolidinone ring of 1 should be considered as an essential pharmacophore for this analog.
Ortho-, meta- and para-nitrobenzyl bromides, alcohols, ethers and esters were synthesised and tested for their mutagenicity toward Salmonella typhimurium TA100, TA100NR (nitroreductase deficient) and TA98 in absence of S9 mix and in TA100 with S9 mix. Compounds of the ortho- and meta-series were non mutagenic with and without S9 mix. Except for the alcohol and ether, the compounds of the para-series were mutagenic in TA100 with activity sequence propionate > butyrate > benzoate > acetate > bromide and this specific activity was reduced considerably by S9 mix. The Ames Salmonella test system does not seem to be an appropriate model to evaluate mutagenicity of o-nitrobenzyls. However, further work is in progress to test all the compounds for mutagenicity in mammalian system.
Selectivity properties are established for membrane electrodes prepared by incorporating bis(p-methylbenzyl)tin dichloride, dibenzyltin dichloride, and bis(p-chlorobenzyl)tin dichloride in plasticized polymer membranes. These electrodes display an unusually high level of selectivity for dibasic phosphate over many common anions. Electrodes prepared with the p-chloro derivative possess the best detection limit and the highest degree of selectivity for phosphate. Selectivity coefficients are calculated for phosphate relative to the following groups of anions: salicylate, benzoate, thiocyanate, iodide, nitrate, bromide, chloride, acetate, fluoride, pyrophosphate, arsenate, adenosine 5'-cyclic monophosphate, adenosine 5'-monophosphate, adenosine 5'-diphosphate, and adenosine 5'-triphosphate. Tin-carbon hyperconjugation within the organotin compound is hypothesized to be critically important in the selective response to phosphate. Enhancement of tin-carbon hyperconjugation by increasing the electron-withdrawing power of substituents on the benzyl ring is predicted to provide even higher levels of selectivity for phosphate.
A series of omegadibenzylaminoalkylamines and related compounds have been prepared and tested as inhibitors of fibrin cross-linking. This structural type was chosen in an attempt to develop noncompetitive inhibitors of fibrinoligase. By the combination of the dibenzylamino moiety at one end and the primary amino group at the other end of a polymethylene chain, the same compound could function both as a pseudo donor substrate and as a noncompetitive alkylating inhibitor. Some of the compounds, notably 74-79, are among the most active fibrinoligase inhibitors described. However, the data indicate that the compounds probably function only as pseudo donor inhibitors.
8,3'-Anhydro-8-mercapto-9-beta-D-xylofuranosyladenine (8,3'-s-cycloadenosine) was phosphorylated with cyanoethyl phosphate and DCC to 5'-phosphate. After 6-amino group was benzoylated, the monophosphate was treated with DCC to give a cyclic phosphate (II). The structure of compound II was elucidated as 8,3'-s-cycloadenosine 2',5'-cyclic phosphate by UV, NMR and CD spectra, as well as enzymatic hydrolyses. When compound II was desulfurized with Raney nickel, cordycepin 2',5'-cyclic phosphate (III) was obtained. Although compound III could be obtained from cordycepin 5'-phosphate with DCC, the yield was extremely low.