共查询到20条相似文献,搜索用时 15 毫秒
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B N Dhawan J N Sharma C R Prasad R C Srimal 《Indian journal of experimental biology》1977,15(12):1134-1136
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Matabolic fate of a new antiandrogen, 16 beta-ethyl-17 beta-hydroxy-4-estren-3-one (TSAA-291), was studied in rats. 14C-TSAA-291 intramuscularly injected as an aqueous suspension was absorbed gradually to give an increase in the plasma level which attained a plateau at 0.5 h, persisted till 8 h and then declined with an approx. half-life of 3.6 days. The drug was widely distributed in tissues, with the concns. almost equal to or higher than that in the plasma. The 14C-drug was eliminated mostly as metabolites within 10 days after dosing with higher activities found in the feces than in urine. Biliary 14C effectively underwent enterohepatic cycling. Biliary metabolites of TSAA-291 were characterized by the combined use of deuterium labeling and GLC-MS analysis. The metabolites identified were as follows: the parent drug, monohydroxy TSAA-291 having the additional hydroxy function in the steroid skeleton, 17 beta-hydroxy-16 beta-(1 xi-hydroxyethyl)-4-estren-3-one, 16 beta-ethyl-17 beta-hydroxy-5 beta-estran-3-one, 16 beta-ethyl-17 beta-hydroxy-5 alpha-estran-3-one, 16 beta-ethyl-5 beta-estrane-3 alpha, 17 beta-diol, 16 beta-ethyl-5 alpha-estrane-3 alpha, 17 beta-diol, 16 beta-ethyl-3 alpha-hydroxy-5 beta-estran-17-one and 16 beta-ethyl-3 alpha-hydroxy-5 alpha-estran-17-one. Monoketodihydroxy and/or trihydroxy metabolites were also detected in the bile. 相似文献
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M V Diurno E Piscopo O Mazzoni A Calignano 《Bollettino della Società italiana di biologia sperimentale》1991,67(12):1067-1072
The following 2-substituted phenyl-3-(N,N-dimethylaminopropyl)-1,3-thiazolidin-4-one of general formula (A): [formula: see text] where: X = H (I), 3-F (II), 3-Cl (III), 3-Br (IV), 3-CH3 (V), 3-OCH3 (VI), 3-NO2 (VII), 4-F (VIII), 4-Cl (IX), 4-Br (X), 4-CH3 (XI), 4-OCH3 (XII), 4-NO2 (XIII) were prepared and tested for antihistamine activity. The synthetic procedure involves the cyclocondensation of the appropriate Schiff base with thioglycolic acid in refluxing dry benzene. The compounds herein presented were tested for their ability to inhibit the contraction inducted by histamine 5.10(-7) M "in vitro", on guinea pig ileum. The results are reported as contraction of test compound causing 50% of submaximal contraction induced by histamine (IC50), and related to mepyramine as control. The results of the antihistamine tests showed an interesting degree of activity of some of the new thiazolidinone-derivatives. Compounds II, III, V, X, and XI showed IC50 values near the value of the control, compound XI being the most active. These compounds seem to be worthy of further investigation. 相似文献
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Schmeda-Hirschmann G 《Zeitschrift für Naturforschung. C, Journal of biosciences》2006,61(7-8):592-594
Insects of the genus Agathemera (Phasmatidae) live in the Chilean Andes over 1500 m above sea level. On disturbing, the insects release a spray that can cause temporary blindness in humans. Very little is known on the composition of chemicals used for defense by South American phasmids. Here we show that both female and male defensive secretion of Agathemera elegans is made up of 4-methyl-1-hepten-3-one. The compound is reported for the first time as a natural product. 相似文献
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Tatsuji Chuman Masahiro Kohno Kunio Kato Masao Noguchi Hiroko Nomi Kenji Mori 《Bioscience, biotechnology, and biochemistry》2013,77(9):2019-2023
A stereoselective synthesis of erythro-serricornin [(4RS,6R,7S)-4,6-dimethyl-7-hydroxynonan-3-one] was completed starting from l-(+)-tartaric acid. The relative configuration of C(6)-methyl and C(7)-hydroxyl groups in naturally occurring serricornin was threo. 相似文献
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2-Chloro-4-amino-1,3,5-triazine-6(5H)-one: a new intermediate in the biodegradation of chlorinated s-triazines.
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Pseudomonas sp. strain A grew with 2-chloro-1,3,5-triazine-4,6-diamine as the sole and growth-limiting source of nitrogen. The substrate was utilized quantitatively and concomitantly with growth and with excretion of a product which was identified as 2-chloro-4-amino-1,3,5-triazine-6(5H)-one. The reaction yielded 1 mol of organic product and 1 mol of NH4+ per mol of substrate. 相似文献
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《Journal of enzyme inhibition and medicinal chemistry》2013,28(4):472-479
A new series of pyrazolo[3,4-d]pyrimidine-6-one derivatives (2a–2j) were prepared by using the Biginelli multicomponent cyclocondensation of 3-methyl-1-phenyl-1H-pyrazol-5(4H)-one (1a), different aromatic aldehydes, and urea with a catalytic amount of HCl at reflux temperature. These compounds were characterized by IR, 1H NMR, 13C NMR, and Mass spectral data. In vitro antiamoebic activity was performed against HM1:IMSS strain of Entamoeba histolytica. The results showed that the compounds 2b, 2i, and 2j with IC50 values of 0.37 µM, 0.04 µM, and 0.06 µM, respectively, exhibited better antiamoebic activity than the standard drug metronidazole (IC50?=?1.33 µM). The toxicological studies of these compounds on human breast cancer MCF-7 cell line showed that the compounds 2b, 2i, and 2j exhibited >80% viability at the concentration range of 1.56–50 µM. 相似文献
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Sotelo E Fraiz N Yáñez M Laguna R Cano E Brea J Raviña E 《Bioorganic & medicinal chemistry letters》2002,12(12):1575-1577
The synthesis and anti-platelet activity of several 5-alkylidene-6-phenyl-3(2H)-pyridazinones are described. The most active compounds are those that contain oxygenated functions (COOR, COMe) on the alkylidene fragment (6a, 6b and 6c). 相似文献
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Hayat F Salahuddin A Azam A 《Journal of enzyme inhibition and medicinal chemistry》2011,26(4):472-479
A new series of pyrazolo[3,4-d]pyrimidine-6-one derivatives (2a-2j) were prepared by using the Biginelli multicomponent cyclocondensation of 3-methyl-1-phenyl-1H-pyrazol-5(4H)-one (1a), different aromatic aldehydes, and urea with a catalytic amount of HCl at reflux temperature. These compounds were characterized by IR, (1)H NMR, (13)C NMR, and Mass spectral data. In vitro antiamoebic activity was performed against HM1:IMSS strain of Entamoeba histolytica. The results showed that the compounds 2b, 2i, and 2j with IC(50) values of 0.37 μM, 0.04 μM, and 0.06 μM, respectively, exhibited better antiamoebic activity than the standard drug metronidazole (IC(50)?=?1.33 μM). The toxicological studies of these compounds on human breast cancer MCF-7 cell line showed that the compounds 2b, 2i, and 2j exhibited >80% viability at the concentration range of 1.56-50 μM. 相似文献
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Dana Griffin 《Brittonia》1980,32(2):214-216
Daltonia fenestrellata Griffin was collected by A. M. Cleef in the Andes of Colombia in 1973. It is characterized by the cuspidate, incurved or recurved leaf tips, the elongated juxtacostal cells and the apically scabrous seta. It seems most closely allied toD. gomezii Crosby of Costa Rica. 相似文献
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