Search results for "Amide"
showing 10 items of 3119 documents
CCDC 1972054: Experimental Crystal Structure Determination
2020
Related Article: Andreas Heilmann, Jamie Hicks, Petra Vasko, Jose M. Goicoechea, Simon Aldridge|2020|Angew.Chem.,Int.Ed.|59|4897|doi:10.1002/anie.201916073
Long-term outcome of antiandrogen monotherapy in advanced prostate carcinoma. Twelve-year’s results of a phase II study.
2003
OBJECTIVE: To present the long-term outcome of patients with locally advanced or metastatic prostate carcinoma treated by first-line antiandrogen monotherapy. PATIENTS AND METHODS: From 1983 to 1990, 41 patients with advanced prostate carcinoma were treated with flutamide monotherapy until progression or the appearance of toxicity. Twenty-five patients (61%) had T3-T4N0M0 and 16 (39%) T2-4N0-3M1 prostate carcinoma. Consensus criteria were adopted to evaluate the response. Plasma testosterone and sexual function were recorded for the first 3 years. RESULTS: Flutamide was administered for up to 147 months; seven patients (17%) interrupted the treatment because of toxicity. There was an object…
Interaction of mushroom tyrosinase with aromatic amines, o-diamines and o-aminophenols
2004
3-Amino-L-tyrosine was found to be a substrate of mushroom tyrosinase, contrary to what had previously been reported in the literature. A series of amino derivatives of benzoic acid were tested as substrates and inhibitors of the enzyme. 3-Amino-4-hydroxybenzoic acid, 4-amino-3-hydroxybenzoic acid and 3,4-diaminobenzoic acid were oxidized by this enzyme, as previously reported for Neurospora crassa tyrosinase, but 4-aminobenzoic acid and 3-aminobenzoic acid were not. Interestingly, 3-amino-4-hydroxybenzoic acid was oxidized five times faster than 4-amino-3-hydroxybenzoic acid, confirming the importance of proton transfer from the hydroxyl group at C-4 position. All compounds inhibited the m…
Pyrazole amino acids: hydrogen bonding directed conformations of 3-amino-1H-pyrazole-5-carboxylic acid residue
2017
A series of model compounds containing 3-amino-1H-pyrazole-5-carboxylic acid residue with N-terminal amide/urethane and C-terminal amide/hydrazide/ester groups were investigated by using NMR, Fourier transform infrared, and single-crystal X-ray diffraction methods, additionally supported by theoretical calculations. The studies demonstrate that the most preferred is the extended conformation with torsion angles ϕ and ψ close to ±180°. The studied 1H-pyrazole with N-terminal amide/urethane and C-terminal amide/hydrazide groups solely adopts this energetically favored conformation confirming rigidity of that structural motif. However, when the C-terminal ester group is present, the second con…
Rac1-Regulated Endothelial Radiation Response Stimulates Extravasation and Metastasis That Can Be Blocked by HMG-CoA Reductase Inhibitors
2011
Radiotherapy (RT) plays a key role in cancer treatment. Although the benefit of ionizing radiation (IR) is well established, some findings raise the possibility that irradiation of the primary tumor not only triggers a killing response but also increases the metastatic potential of surviving tumor cells. Here we addressed the question of whether irradiation of normal cells outside of the primary tumor augments metastasis by stimulating the extravasation of circulating tumor cells. We show that IR exposure of human endothelial cells (EC), tumor cells (TC) or both increases TC-EC adhesion in vitro. IR-stimulated TC-EC adhesion was blocked by the HMG-CoA reductase inhibitor lovastatin. Glycyrr…
Kinetics of Renal Function during Induction in Newly Diagnosed Multiple Myeloma: Results of Two Prospective Studies by the German Myeloma Study Group…
2021
Background: Preservation of kidney function in newly diagnosed (ND) multiple myeloma (MM) helps to prevent excess toxicity. Patients (pts) from two prospective trials were analyzed, provided postinduction (PInd) restaging was performed. Pts received three cycles with bortezomib (btz), cyclophosphamide, and dexamethasone (dex
4812 - A0028 Gangliosides in the retina: a comparative inventory with brain and other ocular structures
2016
Purpose: Gangliosides (GG) make an extremely diverse family of glycosphingolipids particularly abundant in the brain and neural tissues. While it is known that alterations in GG metabolism are associated with visual defects, the precise biological roles of these compounds in the retina are still largely unknown. In this context, we performed an exhaustive inventory and thorough characterization of the human eye GG aiming to reveal specificities and common features of the retina compared to other ocular tissues and brain.Methods: Retina, RPE/Choroid, ciliary body, optic nerve and brain samples were collected from deceased human donors (N=7). GG were extracted and analysed by a comprehensive …
Co-crystals of an agrochemical active – A pyridine-amine synthon for a thioamide group
2011
Five novel co-crystals of thiophanate-ethyl (TE), an agrochemical active, with di(2-pyridyl)ketone (1), 2-benzoylpyridine (2), 3-benzoylpyridine (3), 4-phenylpyridine (4) and biphenyl (5) were found and crystal structures of four of them (TE1–TE3, TE5) solved by single crystal X-ray diffraction. Three of the co-crystals (TE1–TE3) form by way of a reliable pyridine-amine hydrogen bond synthon and one (TE5) because of close packing effects. The fifth co-crystal was identified by X-ray powder diffraction. The work demonstrates the usage of a reliable supramolecular synthon for crystal engineering, while concurrently reminds that the close packing of even very similar molecules cannot be fully …
N-{4-[(3-Methylphenyl)sulfamoyl]phenyl}benzamide
2011
In the title compound, C20H18N2O3S, the dihedral angle between the central benzene ring and the amide group is 24.1 (3) and that between this ring and the aromatic ring of the tolyl group is 68.2 (16). In the crystal, adjacent molecules are linked by N—HO hydrogen bonds into a linear chain running along [100]. Weak C—HO contacts also occur. Extensive weak – interactions exist from both face-to-face and face-to-edge interactions occur between the aromatic rings [centroid–centroid distances = 3.612 (2) and 4.843 (2) A˚ ]. Related peerReviewed
Tenapanor for the treatment of irritable bowel syndrome with constipation.
2020
Introduction: Irritable bowel syndrome with constipation is associated with higher rates of functional impairment, as compared to other subtypes of the syndrome. Conventional laxative-based pharmacologic therapy of IBS-C, which is mostly symptom-based, is often unsatisfactory. Tenapanor represents a first-in-class orally available inhibitor of NHE3, which is minimally absorbed in the GI tract, what constitutes a significant therapeutic benefit, as it may act on the drug target. Areas covered: Aim of this article is to sum up the evidences about pharmacodynamics and pharmacokinetics of tenapanor, focusing on animal models and in vitro studies, but also discuss clinical trials on tenapanor's …