Search results for "medicinal"
showing 10 items of 2966 documents
Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis
2019
This paper describes an optimization strategy of the highly active vinyl ketone 3 which was recognized as a strong inhibitor of rhodesain of Trypanosoma brucei rhodesiense, endowed with a ksecond v...
Development of Novel Benzodiazepine-Based Peptidomimetics as Inhibitors of Rhodesain from Trypanosoma brucei rhodesiense.
2020
Starting from the reversible rhodesain inhibitors 1 a-c, which have Ki values towards the target protease in the low-micromolar range, we have designed a series of peptidomimetics, 2 a-g, that contain a benzodiazepine scaffold as a β-turn mimetic; they are characterized by a specific peptide sequence for the inhibition of rhodesain. Considering that irreversible inhibition is strongly desirable in the case of a parasitic target, a vinyl ester moiety acting as Michael-acceptor was introduced as the warhead; this portion was functionalized in order to evaluate the size of corresponding enzyme pocket that could accommodate this substituent. With this investigation, we identified an irreversibl…
Dioxomolybdenum(VI) and -tungsten(VI) complexes with tetradentate aminobis(phenol)s
2006
Abstract Aminobis(phenol) ligands (H2Ln) carrying either a dimethylamino, a pyridyl or a methoxy sidearm donor were used in the preparation of new tungsten and molybdenum complexes. Treatment of [W(eg)3] (eg = 1,2-ethanediolate dianion) with H2Ln under hydrolytic conditions in a CHCl3–MeOH mixture gave the cis-dioxotungsten(VI) complexes [WO2(Ln)] in good yields. The corresponding molybdenum complexes [MoO2(Ln)] were prepared from [MoO2(acac)2] and respective ligands. The solid-state structures of two molybdenum and one tungsten compounds were determined by single crystal X-ray diffraction, which revealed that the dianionic aminobis(phenolate) backbones of the ligands have coordinated to th…
Antiproliferative activity against leukemia cells of sesquiterpene lactones from the Turkish endemic plant Centaurea drabifolia subsp. detonsa
2017
The apolar organic extract obtained from aerial parts of Centaurea drabifolia Sibth. & Sm. subsp. detonsa (Bornm.) Wagenitz, growing wild in Turkey, was investigated for the first time for its secondary metabolite composition. Seven sesquiterpene lactones belonging to the guaiane class (1-7), including the new compound 4, along with a fatty acid lactone derivative (8), were isolated. The structures of these compounds were established by spectroscopic analysis, including 2D NMR spectroscopic techniques, with the stereostructure of the new guaiane 4 determined with the help of MTPA derivatization. Cytotoxic activities of compounds 1-7 were evaluated against two cancer cell lines, namely acute…
Chionaeosides A–D, Triterpene Saponins from Paronychia chionaea
2007
Four new triterpenoid saponins, chionaeosides A-D (1-4) were isolated from the roots of Paronychia chionaea. On the basis of their spectroscopic data, the structures of the new saponins were established as 3-O-alpha-L-arabinopyranosylgypsogenic acid 28-O-beta-D-glucopyranosyl-(1--3)-beta-D-glucopyranosyl-(1--6)-beta-D-glucopyranoside (1), 3-O-alpha-L-arabinopyranosylgypsogenic acid 28-O-beta-D-glucopyranosyl-(1--6)-beta-D-glucopyranoside (2), 3-O-alpha-L-arabinopyranosylgypsogenic acid 28-O-beta-D-glucopyranoside (3), and 3-O-alpha-L-arabinopyranosylgypsogenic acid (4).
Triterpene Glycosides from the Roots of Astragalus flavescens
2007
Six new triterpene saponins, 3-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-xylopyranosyl-(1-->2)-beta-D-glucuronopyranosyl-21-epi-kudzusapogenol A (1), 3-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl-(1-->2)-beta-D-glucuronopyranosyl-21-epi-kudzusapogenol A (2), 3-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-xylopyranosyl-(1-->2)-beta-D-glucuronopyranosyl-22-O-beta-D-glucopyranosyl-21-epi-kudzusapogenol A (3), 3-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-glucopyranosyl-(1-->2)-beta-D-glucuronopyranosyl-22-O-beta-D-glucopyranosyl-21-epi-kudzusapogenol A (4), 3-O-alpha-L-rhamnopyranosyl-(1-->2)-beta-D-xylopyranosyl-(1-->2)-beta-D-glucuronopyranosyl-22-O-alpha-L-arabinopyranosyl-21-epi-kudzus…
A Short Synthesis of Polysubstituted Pyrrolidines via α-(Alkylideneamino)nitriles
2004
α-(Alkylideneamino)nitriles can be deprotonated under mild conditions. Their conjugated anions react with enones in a 1,4-addition to yield δ-keto-α-(alkylideneamino)nitriles which in turn can be reduced to form pyrrolidines in a one-pot reaction sequence.
Protonation equilibria of some ortho-substituted and annelated aryl and thiophen-2-yl and -3-yl ketones
2001
For some phenyl- (1–8) and thiophen-2-yl (9–11) and thiophen-3-yl (12–14) ketones quantum-mechanical (PM3) calculations have been performed, and for compounds 2, 3, 5–8, 10–14 protonation equilibria have been determined. Phenyl ketones have similar values for the m* parameter and show good linear correlation between the proton affinities calculated in the gas phase and the measured pKBH+ values, which in turn parallel the trend for the calculated carbonyl–phenyl ring dihedral angle. It appears that the differences in basicity are governed essentially by “internal” factors (carbonyl–ring conjugation), while the base–conjugate acid differential solvation is not significantly affected by struc…
Los balnearios de Castelló: el primer turismo conocido en el norte del País Valenciano
1988
EL ARTICULO ANALIZA EL ORIGEN Y EVOLUCION DE LOS BALNEARIOS DE LA MONTAÑA DE CASTELLO, Y SOBRE TODO, EL DE LA FONT D'EN SEGURES DE BENASSAL, QUE ES EL MAS IMPORTANTE DEL PAIS VALENCIANO, ATENDIENDO AL VOLUMEN DE VERANEANTES Y DE EMBOTELLAMIENTO DE AGUA. SUS PERIODOS DE CONSTRUCCION, LAS CARACTERISTICAS POBLACIONALES DEL LUGAR Y DE LOS AGUISTAS, EL MODO DE EXPLOTACION DEL MANANTIAL Y LAS CONSECUENCIAS SOCIO-ECONOMICAS QUE EL BALNEARIO OCASIONA, SON LOS PRINCIPALES APARTADOS ESTUDIADOS. (A)
Spectrophotometric investigation of the binding of vitamin E to water-containing reversed micelles.
2002
The distribution constants of vitamin E partitioned between apolar organic phase and water-containing reversed micelles of sodium bis (2-ethylhexyl) sulfosuccinate (AOT), didodecyldimethylammonium bromide (DDAB), soybean phosphatidylcholine (lecithin) and tetraethylene glycol monododecyl ether (C12E4) have been evaluated by a spectrophotometric method. The results suggest that in the presence of domains from apolar organic solvent to surfactant and to water, vitamin E is partitioned between the micellar palisade layer and the organic solvent and also that its binding strength to reversed micelles depends mainly by specific interactions between the head group of vitamin E and that of the sur…