199536-01-1Relevant academic research and scientific papers
Evaluation of the Synthetic Potential of an AHBA Knockout Mutant of the Rifamycin Producer Amycolatopsis mediterranei
Bu?yszko, Ilona,Dr?ger, Gerald,Klenge, Anja,Kirschning, Andreas
supporting information, p. 19231 - 19242 (2016/01/26)
Supplementing an AHBA(-) mutant strain of Amycolatopsis mediterranei, the rifamycin producer, with a series of benzoic acid derivatives yielded new tetraketides containing different phenyl groups. These mutasynthetic studies revealed unique reductive properties of A. mediterranei towards nitro- and azidoarenes, leading to the corresponding anilines. In selected cases, the yields of mutaproducts (fermentation products isolated after feeding bacteria with chemically prepared analogs of natural building blocks) obtained are in a range (up to 118 mg L-1) that renders them useful as chiral building blocks for further synthetic endeavors. The configuration of the stereogenic centers at C6 and C7 was determined to be 6R,7S for one representative tetraketide. Importantly, processing beyond the tetraketide stage is not always blocked when the formation of the bicyclic naphthalene precursor cannot occur. This was proven by formation of a bromo undecaketide, an observation that has implications regarding the evolutionary development of rifamycin biosynthesis.
CYTOKINE INHIBITORS
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Page/Page column 55, (2011/11/30)
Provided is a compound of Formula (I): and/or at least one pharmaceutically acceptable salt thereof. Also provided are a method of inhibiting the activity of at least one protein chosen from TNFα, IL-1β, NF-κB, IL-10 and iNOS, a method of decreasing a lev
CYTOKINE INHIBITORS
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Page/Page column 29, (2009/05/28)
A compound of Formula I: Each variable is defined in the specification. This invention relates to a method of decreasing a level of a cytokine (e.g., TNFα or interlukine such as IL-1β) in a subject with a compound of Formula I. It also relates to a method
Improving implant materials by coating with nonpeptidic, highly specific integrin ligands
Dahmen, Claudia,Auernheimer, Joerg,Meyer, Axel,Enderle, Anja,Goodman, Simon L.,Kessler, Horst
, p. 6649 - 6652 (2007/10/03)
Giving cells some stick: Osteoblast adhesion to titanium, a common material for implants, is stimulated by coating with an optimized and highly specific nonpeptidic ligand for the αvβ3 integrin (see picture). This new technology is advantageous to conventional coating by peptides or proteins in many practical aspects (selectivity and activity, stability against enzymatic degradation, sterilization, costs).
Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
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, (2008/06/13)
The present invention provides compounds and pharmaceutical compositions that act as antagonists at metabotropic glutamate receptors, and that are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.
Design and synthesis of benzoic acid derivatives as influenza neuraminidase inhibitors using structure-based drug design
Chand, Pooran,Babu, Yarlagadda S.,Bantia, Shanta,Chu, Naiming,Cole, L. Brent,Kotian, Pravin L.,Laver, W. Graeme,Montgomery, John A.,Pathak, Ved P.,Petty, Sandra L.,Shrout, David P.,Walsh, David A.,Walsh, Gerald M.
, p. 4030 - 4052 (2007/10/03)
A series of 94 benzoic acid derivatives was synthesized and tested for its ability to inhibit influenza neuraminidase. The enzyme-inhibitor complex structure was determined by X-ray crystallographic analysis for compounds which inhibited the enzyme. The most potent compound tested in vitro, 5 (4- (acetylamino)-3-guanidinobenzoic acid), had an IC50 = 2.5 x 10-6 M against N9 neuraminidase. Compound 5 was oriented in the active site of the neuraminidase in a manner that was not predicted from the reported active site binding of GANA (4) with neuraminidase. In a mouse model of influenza, 5 did not protect the mice from weight loss due to the influenza virus when dosed intranasally.
