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Synthesis
DOI: 10.1055/s-0029-1218656

Abstract

New synthetic procedures for the trifluoromethyl-substituted
triazoles, 3-(trifluoromethyl)-4-1,2,4-triazole
and 4-(trifluoromethyl)-1-1,2,3-triazole,
have been elaborated. The target compounds were prepared from commercially
available trifluoro­acethydrazide (one step) and methyl
propiolate (three steps), respectively.
[...]

© Georg Thieme Verlag
Stuttgart ˙ New York

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Synthesis
DOI: 10.1055/s-0029-1218653

Abstract

A facile and efficient 1,4-addition of MeSiCN to
enones has been achieved with perfect regioselectivity using CsCO as
catalyst. Thus, with 0.5 mol% of CsCO and
4 equivalents of HO as the additive excellent yields
(81-99%) of β-cyanoketones are obtained
within one to five hours. Both aromatic and aliphatic enones are
found suitable substrates for this protocol.
[...]

© Georg Thieme Verlag
Stuttgart ˙ New York

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Synthesis
DOI: 10.1055/s-0029-1218655

Abstract

A new two-step synthesis of N,N′-disubstituted 2,2′-biimidazoles
from bisimidoyl chlorides is reported. The bisimidoyl chlorides
react smoothly with (2,2-dimethoxyethyl)amine to give bisamidines
that are subsequently cyclized to give the corresponding biimidazoles.
[...]

© Georg Thieme Verlag
Stuttgart ˙ New York

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Synthesis
DOI: 10.1055/s-0029-1218658

Abstract

Secondary benzylic or aliphatic α-hydroxydithianes – rearrange
to α-thioketones when treated with acid. Related tertiary alcohols – eliminate
to dithioketene ketals (e.g., ), which
are ring-opened to thiols in some cases (, ). Allylic α-hydroxydithianes and form
the thioesters and (homologation), and
the tertiary alcohols and undergo deoxygenation to and .
[...]

© Georg Thieme Verlag
Stuttgart ˙ New York

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Synthesis
DOI: 10.1055/s-0029-1218657

Abstract

2-(Trifluoroacetyl)-1,3-azoles reacted with 3-aminopyrazoles
to give the corresponding trifluoromethyl-substituted alcohols.
The conditions required for the reaction and the yields of the products
were highly dependent on the electronic nature of the both the 1,3-azole
and the 3-aminopyrazole units.
[...]

© Georg Thieme Verlag
Stuttgart ˙ New York

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Synthesis
DOI: 10.1055/s-0029-1218654

Abstract

A general method for synthesizing bifunctional hydroxamic acids
containing carboxylic acid or amino functionalities is reported.
Various products from simple alkyl to complex dendrimer-like structures
are described. Such molecules have recently been used in ligand-exchange
reactions for the hydrophilic stabilization of originally oleic
acid protected iron oxide nanoparticles.
[...]

© Georg Thieme Verlag
Stuttgart ˙ New York

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Publication year: 2010
Source: Bioorganic & Medicinal Chemistry, In Press, Accepted Manuscript, Available online 28 January 2010

Baratali, Mashkani , Renate, Griffith , Leonie K., Ashman

Imatinib, dasatinib, sunitinib, CEP-701, and PKC-412, ATP-competitive small molecule inhibitors of type III receptor tyrosine kinases c-KIT and/or FLT3, were evaluated for binding to the closely related receptor, FMS, by docking into models of inactive and active conformations of the FMS kinase domain. To confirm the docking predictions, the drugs were tested for their activity and selectivity in inhibiting cell proliferation and FMS phosphorylation upon stimulation by the FMS ligand, CSF-1. All 5 drugs inhibited FMS activity. Imatinib, dasatinib and CEP-701 represent three different types of interactions determining drug potency and selectivity.

Graphical abstract

Publication year: 2010
Source: Bioorganic & Medicinal Chemistry, In Press, Accepted Manuscript, Available online 28 January 2010

Henrik, Johansson , Olov, Svartström , Prasad, Phadnis , Lars, Engman , Marjam Karlsson, Ott

The organoselenium antioxidant 1 was previously found to act as a catalytic antioxidant in a two-phase lipid peroxidation system. In aqueous environment, selenide 1 quenched ABTS-radicals more efficiently than Trolox and ascorbic acid. The selenide dose-dependently scavenged reactive oxygen- and nitrogen species more efficiently than Trolox for neutrophils and PMA-stimulated macrophages, with 50% inhibitory concentrations in the low micromolar range. In addition no sign of toxicity or effect on cell viability was seen when culturing five human cell lines in concentrations up to 200 μM of selenide 1 for up to seven days. We therefore feel that the compound would…

Graphical abstract

Organoselenium antioxidant 1 efficiently quenched ROS production from neutrophils and macrophages. It showed minimal toxicity in five human cell lines and is proposed for antioxidant pharmacotherapy.

Publication year: 2010
Source: Bioorganic & Medicinal Chemistry, In Press, Accepted Manuscript, Available online 28 January 2010

Deju, Ye , Yu, Zhang , Fei, Wang , Mingfang, Zheng , Xu, Zhang , …

A series of novel thiophene derivatives was designed, synthesized and their activities as competitive inhibitors of protein tyrosine phosphatase (PTPs) 1B (PTP1B) inhibitors were evaluated. All the compounds showed inhibitory potencies, and 10 of these exhibited moderate inhibitory activities with IC50 values less than 10 μM. The activity of the most potent compound P28 (IC50 = 2.1 μM) was 15 times higher than that of the hit compound P01. Further, 4 representative compounds (P19, P22, P28, and P31) demonstrated remarkably high selectivities against other PTPs (e.g., PTPα, LAR, CD45, and TCPTP); P19 exhibited greater than 6-fold selectivity over highly homologous…

Graphical abstract

A series of novel thiophene derivatives as competitive PTP1B inhibitors were designed, synthesized and bioassay. The selectivity against other PTPs and the cellular activity of selected compounds were also investigated.

Publication year: 2010
Source: Bioorganic & Medicinal Chemistry, In Press, Accepted Manuscript, Available online 28 January 2010

Tao, Bing , Xiaojuan, Yang , Hongcheng, Mei , Zehui, Cao , Dihua, Shangguan

Aptamers that are selected in vitro from random pools of DNA or RNA molecules by SELEX (Systematic evolution of ligands by exponential enrichment) technique have been extensively explored for analytical and biomedical applications. Although many aptamers with high affinity and specificity against specific ligands have been reported, there is still a lack of well characterized DNA aptamers. Here we report the selection of a group of aptamer candidates (85 mer) against streptavidin. Through comparing the predicted secondary structures of all the candidates, a conservative bulge-hairpin structure section (about 29 mer) was found, and then it was determined to be the…

Graphical abstract