To continue our systematic SAR studies a series of N-phenylamino derivatives of 2-azaspiro[4.4]nonane-, 2-azaspiro[4.5]decane-, 6-methyl-2-azaspiro[4.5]decane-1,3-dione and 3-cyclohexylpyrrolidine-2,5-dione were synthesized and tested for their anticonvulsant activity in the maximum electroshock seizure (MES) and subcutaneous metrazole seizure threshold (sc. Met) tests. Among those molecules th...

The formation of the benzo[a]pyrene (B[a]P) diones (B[a]P-1,6-dione, B[a]P-3,6-dione, B[a]P-6,12-dione) as the main products of oxidative degradation of B[a]P has been observed under atmospheric conditions in air particulate matter. Samples were collected at two different sites in Munich, Germany. Total B[a]P dione concentrations were determined by APCI/LC-MS and ranged between 8 and 605 pg m-3...

The synthesis of C2-symmetrical bis(β-enamino-pyran-2,4-dione) derivative 3 connected via 1,6-hexylene linker was reported for the first time. X-ray structures and Hirshfeld studies new bis- β-enamino-pyran-2,4-dione along with two structurally related pyran-2,4-dione derivatives 2a,b were discussed. A comparative analysis different intermolecular contacts affecting crystal stability presented....

The proliferation of malware in recent years has motivated the need for tools to detect, analyze, and understand intrusions. Though analysis and detection can be difficult, malware fortunately leaves artifacts of its presence on disk. In this paper, we present Dione, a flexible policy-based disk I/O monitoring and analysis infrastructure that can be used to analyze and understand malware behavi...

The one-pot synthesis of three dragmacidin derivatives is reported. Sarcosine anhydride (4) is brominated and immediately reacted with the corresponding indole to produce the products, namely 3,6-bis(5'-methoxy-3'-indolyl)-1,4-dimethylpiperazine-2,5-dione (1), 3,6-bis(7'-methyl-3'-indolyl)-1,4-dimethylpiperazine-2,5-dione (2) and 3,6-bis-(6'-chloro-3'-indolyl)-1,4-dimethylpiperazine-2,5-dione (...

Three new abietane-type diterpenoids, 7a-butoxyabieta-8,12-diene-11,14-dione (1), 6a,7a-dihydroxyabieta-8,12-dien-11,14-dione (2), and 6a,7b-dihydroxyabieta8,12-diene-11,14-dione (3) were isolated from the bark of Cryptomeria japonica D. Don. Their structures were established by means of 1D and 2D NMR, IR, UV, and HR-EI-MS spectra and comparison with the data of known analogues. ã 2016 Publishe...

In order to know the contribution of adrenal and gonadal androgens to the development of the side gland of Suncus murinus, we studied the effects of gonadectomy and adrenalectomy on gland thickness and the plasma levels of testosterone, androstenedione (delta 4-dione) and dehydroepiandrosterone (DHA). In males, castration decreased gland thickness to 71% of the control. The plasma levels of del...

Several steroids occurring in the pathway of corticosteroid biosynthesis were investigated for their ability to exert a fast or delayed feedback inhibition of stress-induced release of corticotrophin. Rats were injected subcutaneously with vehicle or a steroid either 10 min (fast feedback) or 4 h (delayed feedback) before they were subjected to stress which consisted of a 2 min exposure to ethe...

The bacterial degradation of cholic acid under anaerobic conditions by Pseudomonas sp. N.C.I.B. 10590 was studied. The major unsaturated neutral compound was identified as 12 beta-hydroxyandrosta-4,6-diene-3,17-dione, and the major unsaturated acidic metabolite was identified as 12 alpha-hydroxy-3-oxochola-4,6-dien-24-oic acid. Eight minor unsaturated metabolites were isolated and evidence is g...

This paper describes the properties and partial purification from Pseudomonas testosteroni of enzymes concerned with the introduction of unsaturation into ring A of 3-ketosteroids. These enzymes promote the formation of the A1e4-diene-3-one structure from steroids bearing C-19 angular methyl groups and the formation of ring A phenols from lQ-nor-steroids. P. testosteroni is a strict aerobe whic...