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Welcome to the BioBlocks Bulletin
Welcome to the BioBlocks Bulletin, a source of recent research on key classes of BioBlocks building blocks, combined with current information on pricing and availability. In this issue we describe new products derived from the BioBlocks 4-hydroxy-quinoline-carboxylic acid, 4-amino-quinoline-carboxylic acid and 4-bromo-3-carbonitrile-quinoline series. These compounds have been used only briefly in medicinal chemistry, primarily to define the range of active compounds. We have developed a route to this set of underutilized compounds, and now carry them in stock in San Diego in multigram quantities.
Please scroll down to the bottom of the newsletter to view the references. To order products, shop at
www.bioblocks.com, call (+1) 858 558-5900 or email
sales@bioblocks.com.
Quicklinks:
All 4-Hydroxyquinolines
All 4-Aminoquinolines
All 4-Bromoquinolines
All Quinolines
New building blocks
BioBlocks catalog in
PDF,
SDF, or
XLS
Results-based lead optimization services
Full list of BioBlocks Bulletins
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Application Update
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Core structure in active series of nociceptin antagonists and inhibitors of anaphylatoxin C5a receptor binding:
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Reversed amide synthesis for SAR exploration within the above series:
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1) Shinkai H., et al., J. Med. Chem. 2000, 43, 4667 - 4677
2) Lanza, T. J., et al., J. Med. Chem. 1992, 35, 252 - 258
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Literature References
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| 1. |
Hisashi Shinkai, Takao Ito, Tetsuya Iida, Yuki Kitao, Hideki Yamada, and Itsuo Uchida
4-Aminoquinolines: Novel Nociceptin Antagonists with Analgesic Activity
Shinkai and co-workers report a series of 4-amino-quinoline based nociceptin antagonists which were synthesized in order to examine their therapeutic potential. Elucidation of SAR led to the optimum compounds of which contain an amide moiety at the 6-position of the quinoline core. The reversed amide at the 6-position was also explored, however this change caused a loss of binding affinity. The reversed amide synthesis is achieved through standard amide coupling of BioBlocks QU2320 with aryl, alkyl and benzyl amines. The 4-hydroxy group was then converted to the amine.
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Thomas J. Lanza, Philippe L. Durette, Thomas Rollins, Salvatore Siciliano, Dana N. Cianciarulo, Sumire V. Kobayashi, Charles G. Caldwell, Martin S. Springer, and William K. Hagmann
Substituted 4,6-diaminoquinolines as inhibitors of C5a receptor binding
Lanza and co-workers report the discovery of a series of inhibitors of the anaphylatoxin C5a receptor binding. The authors suggest that blocking the action of C5a on its receptors may represent an intriguing therapeutic target for the treatment of diseases characterized by an excessive activity and recruitment of inflammatory cells. The optimum compounds listed contain a 4-amino-quinoline core with an amide moeity at the 6-position. For expanded SAR, the reversed amide at the 6-position was also explored, however it showed a complete loss of inhibition. The synthesis follows from BioBlocks QU2320 as described in the above reference.
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BioBlocks Inc.
9885 Mesa Rim Road. Suite 101
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