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Sulfamates of various estrogens are prodrugs with increased systemic and reduced hepatic estrogenicity at oral application
TLDR
Oral therapy with natural or synthetic estrogens, like ethinylestradiol, suffers from low, suboptimally defined bioavailability and excess hepatic estrogen actions, so N,N-alkylated and non-alksylated sulfamates of ethinylstradio, estradiol and estrone overcome these deficiencies and represent a new strategy of oral hormone administration. Expand
Estradiol, testosterone, dehydroepiandrosterone and androstenedione: novel derivatives and enantiomers. Interactions with rat liver microsomal cytochrome P450 and antioxidant/radical scavenger
Interactions of 27 steroids, among them 17 derivatives such as ethers, sulfates and amidosulfonates derived from 17 beta- and 17 alpha-estradiol, from testosterone and alpha- andExpand
A three-step procedure for the conversion of γ-lactones into δ-lactones
γ-Lactones with a wide range of functional groups are transformed by a three-step procedure into the corresponding δ-lactones in an overall yield of up to 55%. The novel methodology involves theExpand
Prostaglandins and Prostaglandin Intermediates. XVII [1]. Synthesis of the Main Metabolite of the PGF2α Analogue Cloprostenol
The δ-lactone 5, the main metabolite of the PGF2α analogue cloprostenol, is prepared in four steps from the homologous γ-lactone 1 in an overall yield of 42% by conversion into the γ-lactol 3, whichExpand
Novel “scavestrogens” and their radical scavenging effects, iron-chelating, and total antioxidative activities: Δ 8,9-dehydro derivatives of 17α-estradiol and 17β-estradiol
Abstract Antioxidant effects of Δ8,9-dehydro derivatives of 17α-estradiol and 17β-estradiol were investigated using four different in vitro models: rat synaptosomal lipid peroxidation induced byExpand
Novel estrogens and their radical scavenging effects, iron-chelating, and total antioxidative activities: 17α-substituted analogs of Δ 9(11)-dehydro-17β-estradiol
Abstract Antioxidant effects of N,N-dimethyl-p-toluidine, p-cresol, and p-(hydroxy)thioanisol 17α-substituted analogs of 17β-estradiol and their Δ9(11)-dehydro homologs were investigated using fourExpand
Synthesis of 13-ethyl-11-methylene-18,19-dinor-17α-pregn-4-en-20-yn-17-ol (desogestrel) and its main metabolite 3-oxo desogestrel☆
Abstract A synthesis of the steroid hormone desogestrel (25) from the 18a-homo steroid 1 is described. 25 was transformed into 3-oxo desogestrel (28) by allyl oxidation.
Synthesis of estrogen sulfamates: Compounds with a novel endocrinological profile
TLDR
A new synthesis of estrone sulfamate on a 100-g scale was developed using dimethylformamide as the solvent and base and circumvent the nonselective formation of esters and side reactions by in situ generated azasulfenes. Expand
Effects of estradiol and estradiol sulfamate on the uterus of ovariectomized or ovariectomized and hypophysectomized rats
TLDR
There are no major differences in the uterine response to treatment with J995 or E2 with respect to the effects on ER and ERalpha mRNA levels, and the IGF-I mRNA level though, is more affected by J995 than by E2 after 7 days of treatment, indicating a prolonged effect of J995. Expand
The Oxidation of Primary Trimethylsilyl Ethers to Aldehydes – a selective conversion of a primary hydroxy group into an aldehyde group in the presence of a secondary hydroxy group
Secondary trimethylsilyl ethers (2a–d) are not affected by Collins reagent in dichloromethane at 0°C. Primary trimethylsilyl ethers (4a–e), however, are smoothly oxidized to aldehydes (5a–e) underExpand
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