132502-56-8Relevant academic research and scientific papers
Expansion of antibacterial spectrum of muraymycins toward pseudomonas aeruginosa
Takeoka, Yusuke,Tanino, Tetsuya,Sekiguchi, Mitsuaki,Yonezawa, Shuji,Sakagami, Masahiro,Takahashi, Fumiyo,Togame, Hiroko,Tanaka, Yoshikazu,Takemoto, Hiroshi,Ichikawa, Satoshi,Matsuda, Akira
supporting information, p. 556 - 560 (2014/06/09)
It is urgent to develop novel anti-Pseudomonas agents that should also be active against multidrug resistant P. aeruginosa. Expanding the antibacterial spectrum of muraymycins toward P. aeruginosa was investigated by the systematic structure-activity relationship study. It was revealed that two functional groups, a lipophilic side chain and a guanidino group, at the accessory moiety of muraymycins were important for the anti-Pseudomonas activity, and analogue 29 exhibited antibacterial activity against a range of P. aeruginosa strains with the minimum inhibitory concentration values of 4-8 μg/mL.
Structure-activity relationship study on α1 adrenergic receptor antagonists from beer
Wakimoto, Toshiyuki,Nitta, Makoto,Kasahara, Kana,Chiba, Taketo,Yiping, Ye,Tsuji, Kuniro,Kan, Toshiyuki,Nukaya, Haruo,Ishiguro, Masaji,Koike, Minako,Yokoo, Yoshiaki,Suwa, Yoshihide
scheme or table, p. 5905 - 5908 (2010/06/13)
Hordatine A and aperidine have been previously isolated from beer as active ingredients, which bind to muscarinic M3 receptor. In addition, these compounds have exhibited antagonist activity against the α1A adrenoceptor. Although the relative structures of these two molecules have previously been determined, the absolute stereochemistry was unclear. Hence, to elucidate the absolute stereochemistry of natural hordatine A, we synthesized each enantiomer of hordatine A and aperidine from optically pure dehydrodi-p-coumaric acid. Several additional related compounds were also synthesized for structure-activity relationship studies. Chiral column HPLC analysis demonstrated that the absolute stereochemistry of natural hordatine A is (2S,3S), while based on the isomerization mechanism, the stereochemistry of aperidine is (2R,3S). The α1A adrenoceptor binding activity of (2R,3R)-hordatine A is the most potent among the enantiomeric pairs of hordatines and aperidines. Furthermore, the related, synthetic compound, (2R,3R)-methyl benzofurancarboxylate exhibits antagonist activity against the α1A adrenoceptor at a lower concentration than that of hordatine A.
Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors
Wagner, Jürgen,Kallen, J?rg,Ehrhardt, Claus,Evenou, Jean-Pierre,Wagner, Dieter
, p. 3664 - 3674 (2007/10/03)
We have designed, synthesized, and tested in vitro a novel class of noncovalent thrombin inhibitors. The main feature of these inhibitors is a 6,5-fused bicyclic core structure that fills the S2 pocket of the active site of thrombin. The bicycl
