41223-92-1Relevant articles and documents
Identification of indole inhibitors of human hematopoietic prostaglandin D2 synthase (hH-PGDS)
Edfeldt, Fredrik,Even?s, Johan,Lepist?, Matti,Ward, Alison,Petersen, Jens,Wissler, Lisa,Rohman, Mattias,Sivars, Ulf,Svensson, Karin,Perry, Matthew,Feierberg, Isabella,Zhou, Xiao-Hong,Hansson, Thomas,Narjes, Frank
, p. 2496 - 2500 (2015/06/02)
Abstract Human H-PGDS has shown promise as a potential target for anti-allergic and anti-inflammatory drugs. Here we describe the discovery of a novel class of indole inhibitors, identified through focused screening of 42,000 compounds and evaluated using a series of hit validation assays that included fluorescence polarization binding, 1D NMR, ITC and chromogenic enzymatic assays. Compounds with low nanomolar potency, favorable physico-chemical properties and inhibitory activity in human mast cells have been identified. In addition, our studies suggest that the active site of hH-PGDS can accommodate larger structural diversity than previously thought, such as the introduction of polar groups in the inner part of the binding pocket.
studies on anti-helicobacter pylori agents. Part 2: New cephem derivatives
Yoshida, Yoshiki,Matsuda, Keiji,Sasaki, Hiroshi,Matsumoto, Yoshimi,Matsumoto, Satoru,Tawara, Shuichi,Takasugi, Hisashi
, p. 2317 - 2335 (2007/10/03)
The synthesis and optimization of the anti-Helicobacter pylori activity of a novel series of cephem derivatives are described. Introduction of thio-heterocyclic groups containing N- and S-atoms to the 3-position and phenyl or thienyl acetamido groups to the 7-position of the cephem nucleus dramatically improved the activity. From this series of derivatives, compound 13i was found to have extremely potent in vitro anti-H. pylori activity, superior therapeutic efficacy compared to AMPC and CAM, no cross-resistance between CAM or MNZ and low potential for causing diarrhea due to instability to β-lactamase. Copyright (C) 2000 Elsevier Science Ltd.
1-Oxacephalosporins: Enhancement of β-Lactam Reactivity and Antibacterial Activity
Murakami, Kazuhisa,Takasuka, Mamoru,Motokawa, Kiyoshi,Yoshida, Tadashi
, p. 88 - 93 (2007/10/02)
The effect of replacement of sulfur in the cephem nucleus by oxygen upon the β-lactamase stability, infrared carbonyl frequency of the β-lactam ring, and antibacterial activity was investigated.The replacement reduced the stability of β-lactam compounds t