1,721,201 research outputs found
Polycondensed heterocycles. VIII. Synthesis of 11-aryl-5H,11H-Pyrrolo[2,1-c][1,4]benzothiazepines by Pummerer rearrangement-cyclization reaction
No full text11-Phenyl-5Hl1H-pyrrolo[2,1-c][1,4]benzothiazepine has been prepared by an intramolecular nucleophilic displacement reaction. The same compound, as well as some analogues thereof, were more conveniently obtained by Pummerer rearrangement-cyclization of sulfinyl precursors. The latter method was also effective for the synthesis of 4-phenyl-4H-pyrrolo[2,1-c][1,4]benzothiazine. © 1992
Synthesis and acetylcholinesterase inhibitory activity of several pyrimidone analogues of huperzine A
No full textSyntheses of four new pyrimidone analogues of the acetylcholinesterase (AChE) inhibitor huperzine A are reported together with the inhibitory potencies of these compounds for foetal bovine calf serum AChE; β-lactone formation followed by a thermal cycloreversion reaction serves as the key step for introduction of the ethylidene appendage of 12 in the stereochemically correct form
Polycondensed heterocycles. V. Synthesis of 5H,11H-Pyrrolo[2,1-c][1,4]benzothiazepine
No full textThe 5H,11H-pyrrolo [2, 1-c][1,4] benzothiazepine ring system has been prepared by two synthetic pathways, involving the intramolecular nucleophilic displacement on 1-(2-fluorobenzyl)-2-mercaptomethylpyrrole or the Pummerer rearrangement of 1-(2-ethoxycarbonylmethylsulfinyl-benzyl)pyrrole followed by in situ cyclization, respectively. © 1990
Expression, Purification, Structural and Functional Characterization of Recombinant Human Parvulin 17
Full text linkParvulins, peptidyl-prolyl isomerase enzymes (PPIase), catalyze the cis-trans isomerization of prolyl bonds in polypeptides, contributing to folding and function regulation of many proteins. Among Parvulins, Par17, exclusively expressed in hominids, is the least examined in terms of structure, catalytic function and cellular activity. Setting the conditions for the preparation of recombinant active Par17 may therefore significantly foster future studies. Here, we comparatively evaluated the impact of several parameters, including host strains, culture media, isopropyl ss-D-1-thiogalactopyranoside concentration, post-induction incubation time and temperature, on the overexpression of Par17 in E. coli cells. A similar approach was also comparatively adopted for the preparation of the recombinant full-length Pin1 protein, the most representative Parvulin, and the catalytic domains of both enzymes. Proteins were efficiently expressed and purified to homogeneity and were subjected to a structural characterization by Size Exclusion Chromatography and Circular Dichroism. Moreover, a single-step homogeneous protease-based fluorimetric assay, potentially scalable in HTS format, has been developed for determining the peptidyl-prolyl cis-trans isomerase activity of recombinant Parvulins. Results obtained show that proteins are folded and active. These new data mark an important milestone for progressing the investigation of Parvulins
The 1-(2,3-dichlorophenyl)-piperazine-to-aripiprazole ratio at steady state in rats and schizophrenic patients
No full textComparative Molecular Field Analysis (CoMFA) di Calcio Antagonisti a Struttura Benzotiazinica
No full textPolycondensed heterocycles. X. A new method for the preparation of pyrrolo[2,1-c][1,4]benzothiazepines by intramolecular mitsunobu cyclisation
No full textA modified Mitsunobu reaction of 2-hydroxymethylpyrrole and suitable thiophenol derivatives lead to intermediates which can be easily elaborated and eventually cyclised to the title compounds. The cyclisation step consists of another Mitsunobu reaction variation by which an 'activated' pyrrole is N- alkylated intramolecularly, under very mild conditions
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