- Conformationally restrained chiral analogues of spermine: Chemical synthesis and improvements in DNA triplex stability
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The synthesis of novel chiral analogues of spermine, 11 (2R,4S) and 14 (2S,4R), is reported starting from trans-4-hydroxy-L-proline 3. These cyclic analogues are generated from linear, achiral spermine by incorporating a pyrrolidine ring on the backbone t
- Rajeev,Sanjayan,Ganesh
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- Synthesis and antibacterial activity of 6(R)- and 6(S)-fluoropenibruguieramine As: Fluorine as a probe for testing the powerfulness of memory of chirality (MOC)
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The synthesis of 6(R)- and 6(S)- fluoropenibruguieramine As has been achieved, employing the elegant strategy developed by Kim and co-workers. Single diastereomers were formed via the key intramolecular aldol reaction, and both of the products were unambiguously confirmed by X-ray diffraction crystallography. This reaction shows that the fluorine amide effect could not compete with the memory of chirality (MOC) effect, thus further demonstrating the powerfulness of MOC effect in asymmetric synthesis. The biological testing carried out in this work indicates that the principal of antibacterial activity of the natural extract is probably not penibruguieramine A.
- Liu, Ting,Yan, Nan,Zhao, Hui,Wang, Zhen-Xing,Hu, Xiang-Guo
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- NOVEL AMINO PYRIMIDINE DERIVATIVES
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The present invention describes new amino pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.
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Paragraph 0329; 0330
(2015/06/10)
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- NOVEL AMINO PYRIMIDINE DERIVATIVES
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The present invention describes new amino pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.
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Page/Page column 68; 69; 70
(2015/06/11)
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- Part 2: Design, synthesis and evaluation of hydroxyproline-derived α2δ ligands
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Conformational constraint has been used to design a potent series of α2δ ligands derived from the readily available starting material (2S,4R)-hydroxy-l-proline. The ligands have improved physicochemistry and potency compared to their linear counterparts (described in our earlier publication) and the lead compound has been progressed to clinical development.
- Rawson, David J.,Brugier, Delphine,Harrison, Anthony,Hough, Jo,Newman, Julie,Otterburn, Joe,Maw, Graham N.,Price, Jenny,Thompson, Lisa R.,Turnpenny, Paul,Warren, Andrew N.
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p. 3767 - 3770
(2011/08/06)
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- Synthesis and biological activity of 1-phenylsulfonyl-4-phenylsulfonylaminopyrrolidine derivatives as thromboxane A2 receptor antagonists
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The synthesis and biological activity of novel 1-phenylsulfonyl-4- phenylsulfonylaminopyrrolidine analogues are described. All compounds were produced through modification of the substituent formally corresponding to the 1,3-dioxane ring system and the ω-octenol side chain of thromboxane A2 (TXA2), in reference to the structure of Daltroban. Several compounds were found to be potent TXA2 receptor antagonists. Compound 51a was the most effective inhibitor of 9,11-epoxymethano PGH2 (U-46619)-induced rat aortic strip contraction (IC50 = 0.48 nM).
- Marusawa, Hiroshi,Setoi, Hiroyuki,Sawada, Akihiko,Kuroda, Akio,Seki, Jiro,Motoyama, Yukio,Tanaka, Hirokazu
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p. 1399 - 1415
(2007/10/03)
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