- A template-directed synthetic approach to halogen-bridged mixed-valence platinum complexes on artificial peptides in solution
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A template-directed synthetic approach to halogen-bridged mixed-valence platinum complexes has been performed in organic media using, for instance, a synthetic peptide bearing two bis(ethylenediamine)-based Pt(iv) complexes with two axial bromide anionic ligands, [1a(Pt(iv)Br2(en)) 2](RSO3)4, and a [Pt(ii)(en) 2](RSO3)2 complex (R = (C12H 25OCH2)2CHO(CH2)3-). The Royal Society of Chemistry.
- Tanaka, Kentaro,Kaneko, Kenji,Watanabe, Yusuke,Shionoya, Mitsuhiko
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- Tetrahydroimidazo[1,2-a]pyrazine Derivatives: Synthesis and Evaluation as Gαq-Protein Ligands
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The 5,6,7,8-tetrahydroimidazo[1,2-a]pyrazine derivative BIM-46174 and its dimeric form BIM-46187 (1) are heterocyclized dipeptides that belong to the very few cell-permeable compounds known to preferentially silence Gαq proteins. To explore the chemical space of Gαq inhibitors of the BIM chemotype, a combinatorial approach was conducted towards a library of BIM molecules. This library was evaluated in a second messenger-based fluorescence assay to analyze the activity of Gαq proteins through the determination of intracellular myo-inositol 1-phosphate. Structure–activity relationships were deduced and structural requirements for biological activity obtained, which were (i) a redox reactive thiol/disulfane substructure, (ii) an N-terminal basic amino group, (iii) a cyclohexylalanine moiety, and (iv) a bicyclic skeleton. Active compounds exhibited cellular toxicity, which was investigated in detail for the prototypical inhibitor 1. This compound affects the structural cytoskeletal dynamics in a Gαq/11-independent manner.
- Küppers, Jim,Benkel, Tobias,Annala, Suvi,Kimura, Kenichi,Reinelt, Lisa,Fleischmann, Bernd K.,Kostenis, Evi,Gütschow, Michael
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supporting information
p. 12615 - 12623
(2020/09/09)
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- Synthesis and nematicidal activity of piperazinedione derivatives based on the natural product Barettin
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Nematodes are serious constraints of crop production worldwide. However, the traditional nematicides suffer from the side-effects, including environmental and human toxicity. Herein, more than 70 novel piperazinedione derivatives based on the natural product Barettin were synthesized and evaluated against the root-knot nematode Meloidogyne incognita (M. incognita). While most of synthesized compounds exhibited certain nematicidal activity at high concentration, the best one showed a nematicidal activity of 75% at 2.4 μmol/L.
- Sun, Haiyang,Li, Hui,Wang, Jiayi,Song, Gonghua
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p. 977 - 980
(2017/11/16)
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- Monovalent and bivalent fibrin-specific MRI contrast agents for detection of thrombus
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Probing in contrast: Four gadolinium-DTPA moieties (DTPA = diethylenetriaminepentaacetic acid) and two fibrin-specific cyclic peptides are linked by a compact triethylenetetraamine core (see scheme) to create a highly sensitive probe for molecular MR imaging of thrombosis. The contrast agent has a high molecular relaxivity, and the dual peptide construct provides five-fold higher fibrin affinity than the monovalent analogue. This bivalent probe showed significant specific thrombus uptake in an in vivo model of thrombosis. (Figure Presented).
- Nair, Shrikumar A.,Kolodziej, Andrew F.,Bhole, Gandhali,Greenfield, Matthew T.,McMurry, Thomas J.,Caravan, Peter
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supporting information; experimental part
p. 4918 - 4921
(2009/02/08)
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- Relationship between Taste and Structure of O-Aminoacyl Sugars Containing Basic Amino Acids
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To study the relationship between taste and structure of O-aminoacyl sugars, a number of O-aminoacyl sugars containing basic amino acids were prepared.Taste quality of O-aminoacyl sugars was dependent on the side chain length of basic amino acids that were introduced into sugars.O-Aminoacyl sugars had an excellent sodium ion diet effect that could reduce sodium ion intake to 10 percent.
- Tamura, Masahiro,Nakamura, Kozo,Kinomura, Keisuke,Okai, Hideo
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