The activity of the White Line Inducing Principle (WLIP) and tolaasin I, produced by virulent strains of Pseudomonas reactans and Pseudomonas tolaasii, respectively, was comparatively evaluated on lipid membranes. Both lipodepsipeptides were able to induce the release of calcein from large unila...
White-line-inducing principle (WLIP), a lipodepsipeptide isolated from Lasiosphaera fenzlii Reich., which is one of the puffballs, for the first time, has been reported to exhibit anti-microbial activity. However, there are no reports regarding the anti-tumor effects of WLIP. In this study, we r...
Quantitative structure-activity relationships (QSARs) have been utilized to validate toxicity data to Vibrio fisheri (the acute Microtox test) at each of the 5-, 15- and 30-min endpoints. Statistically robust QSARs were found for chemicals acting by a non-polar narcosis mechanism of action (MOA)...
Quantitative structure property relationships (QSPR) for the pKa of phenols, carboxylic acids and alcohols were developed from descriptors derived from semi-empirical molecular orbital theory quantum chemical calculations. A training set of compounds were used to refine the models and a validati...
Quantitative structure-activity relationships are developed for the toxicity of 166 varied phenol derivatives to the ciliate Tetrahymena pyriformis. A variety of physico-chemical descriptors were calculated but no significant relationship could be obtained for all 166 compounds. When certain che...
Quantitative structure–activity relationships (QSARs) for the toxicity of 200 phenols to the ciliated protozoan Tetrahymena pyriformis, and the validation of the QSARs using a test set of a further 50 compounds, are reported. The phenols are structurally heterogeneous and represent a variety of...
We provide QSAR models for the growth inhibition of the ciliated protozoan Tetrahymena pyriformis by 250 mechanistically diverse phenolic compounds. The simultaneous linear regression analysis on 1338 topological, geometrical, and electronic molecular descriptors over 200 molecules leads to a se...
This paper is the second as part of a study to elucidate cyano group chemistry in the interstellar medium, wherein we present a characterization of the millimeter-wave spectrum of methoxyacetonitrile. Its structural isomer, 2-cyanoethanol was described in paper Braakman and Blake (submitted for ...
Progesterone (P) biphasically modulates follicle-stimulating hormone (FSH) secretion in the rat both in vivo and in vitro with the duration of estrogen priming determining the biphasic nature of the P action, probably through estrogen up-regulation of the anterior pituitary progesterone receptor...
The A189 V inactivating mutation of the human FSH receptor (FSHR) leads to subfertility in men and primary ovarian failure in women. This mutation has previously been associated with intracellular retention of the FSHR and impaired cAMP production. Here, we show that the A189 V FSHR stably expre...
ObjectiveTo report the clinical, hormonal, and molecular features of a female adolescent with selective FSH deficiency. In addition, a complete review of previous cases is provided, focusing on hormonal aspects.
Objective: Congenital FSH deficiency is an exceptional cause of male infertility most often attributed to FSH β gene mutations. The few published cases report azoospermia, severe testicular hypotrophy and normal testosterone levels associated with normal virilization. We report the exploration ...
Bis(propynyl)zirconocene (6a) reacts with tris(pentafluorophenyl)borane to yield the carbon-carbon coupled Cp2M(μ-RC4R)B(C6F5)3 betaine product 4a (M Zr, R CH3). A variety of differently substituted analogs was prepared (M Zr, R = n-butyl, phenyl, cyclohexyl; M Ti, R CH3; M Hf...
The effect of tris(methoxy diethylene glycol) borate (TMDGB) on the coordination structure between ethylene carbonate (EC) solvents with high permittivity and ClO4− anions has been investigated by using a Fourier transform infrared (FT-IR) spectroscopy. The results of FT-IR analyses manifested t...
We have synthesized N-[3-(2′,4′-dichlorophenoxy)-2-18F-fluoropropyl]-N-methylpropargylamine (18F-fluoroclorgyline) as a potential positron emission tomography (PET) radiotracer for monoamine oxidase A (MAO-A). The radiosynthesis was carried out by a 18F-fluoride-for-mesylate substitution react...
The dynamics of insulin secretion stimulated by repaglinide, a glinide, and the combinatorial effects of repaglinide and incretin were investigated. At 4.4 mM glucose, repaglinide induced insulin secretion with a gradually increasing first phase, showing different dynamics from that induced by g...
SummaryRepaglinide (RPG) is a short-acting insulin secretagogue widely prescribed for the treatment of type 2 diabetes. It boosts insulin secretion by inhibiting the pancreatic ATP-sensitive potassium channel (KATP). However, the mechanisms by which RPG binds to the KATP channel are poorly under...
A series of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides bearing the halogens iodine and bromine were synthesised and their binding affinity for the peripheral benzodiazepine binding sites (PBBS) in rat kidney mitochondrial membranes was evaluated using [3H]PK11195. Central benzodiazepine recepto...
To affiliate multiple bioactivities in a compact heteronuclei, two series of benzimidazole based 1,3,4-oxadiazoles were synthesized and assessed in vitro for their efficacy as antimicrobial agents against eight bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aerug...
We have recently identified a region, N-terminus residues 9–30, in the extracellular domain of the follicle-stimulating hormone (FSH) receptor capable of binding FSH, but not luteinizing hormone (LH) or thyroid-stimulating hormone (FSH) (Dattatreyamurty and Reichert (1992) Mol. Cell. Endocrinol...
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