- Marinopyrrole derivatives as potential antibiotic agents against methicillin-resistant Staphylococcus aureus (III)
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The marine natural product, marinopyrrole A (1), was previously shown to have significant antibiotic activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). Although compound (1) exhibits a significant reduction in MRSA activity in the presence of human serum, we have identified key modifications that partially restore activity. We previously reported our discovery of a chloro-derivative of marinopyrrole A (1a) featuring a 2-4 fold improved minimum inhibitory concentration (MIC) against MRSA, significantly less susceptibility to serum inhibition and rapid and concentration-dependent killing of MRSA. Here, we report a novel fluoro-derivative of marinopyrrole A (1e) showing an improved profile of potency, less susceptibility to serum inhibition, as well as rapid and concentration-dependent killing of MRSA.
- Liu, Yan,Haste, Nina M.,Thienphrapa, Wdee,Li, Jerry,Nizet, Victor,Hensler, Mary,Li, Rongshi
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Read Online
- Preparation method of 1-alkyl-2-phenyl-4-quinolones
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Provided is a novel method for synthesizing 1-alkyl-2-phenyl-4-quinolones from 2-halobenzoates. The synthesizing method in the present invention has advantages capable of synthesizing 1-alkyl-2-phenyl-4-quinolones in high yield through a simplified stage in a simple reaction condition by means of 2-halobenzoates as an inexpensive starting material.COPYRIGHT KIPO 2015
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Paragraph 0023-0026
(2016/10/17)
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- Novel one-pot synthesis of xanthones via sequential fluoride ion-promoted fries-type rearrangement and nucleophilic aromatic substitution
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A novel and efficient synthesis of xanthones is described. 2-(Trimethylsilyl)phenyl 2-fluorobenzoate derivatives undergo Fries-type rearrangement and intramolecular SNAr reaction in a one-pot sequential manner under fluoride ion-promoted mild conditions. The method provides efficient access to xanthones that have significant steric congestion around the C9 carbonyl, which are not readily available by conventional methods. Georg Thieme Verlag Stuttgart · New York.
- Fujimoto, Yuuki,Itakura, Ryohei,Hoshi, Hiroki,Yanai, Hikaru,Ando, Yoshio,Suzuki, Keisuke,Matsumoto, Takashi
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supporting information
p. 2575 - 2580
(2013/12/04)
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- 7-Substituted Purine Derivatives for Immunosuppression
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The present invention provides novel purinone and related derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formula III:
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Page/Page column 34
(2008/12/05)
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- 7-SUBSTITUTED PURINE DERIVATIVES FOR IMMUNOSUPPRESSION
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The present invention provides novel purinone and related derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formula (III).
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Page/Page column 80
(2008/12/05)
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- PURINE AND IMIDAZOPYRIDINE DERIVATIVES FOR IMMUNOSUPPRESSION
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The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulas ( I ) and ( II ).
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Page/Page column 105
(2010/11/24)
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- A versatile synthesis of poly- and diversely substituted isoindolin-1- ones
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A variety of diversely substituted isoindolin-1-ones have been prepared by alkaline cleavage of the C-P bond in the corresponding phosphorylated lactams obtained by base-induced aryne-mediated cyclization of o-halogeno-N- (phosphinylmethyl)benzamide derivatives.
- Hoarau, Christophe,Couture, Axel,Deniau, Eric,Grandclaudon, Pierre
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p. 655 - 660
(2007/10/03)
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- Novel quinolizidine salicylamide influenza fusion inhibitors
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A novel series of quinolizidine salicylamides was synthesized as specific inhibitors of the H1 subtype of influenza A viruses. These inhibitors inhibit the pH-induced fusion process, thereby blocking viral entry into host cells. Compound 16 was the most active inhibitor in this series with an EC50 of 0.25 μg/mL in plaque reduction assay. The synthesis and the SAR of these compounds are discussed.
- Yu, Kuo-Long,Ruediger, Edward,Luo, Guangxiang,Cianci, Christopher,Danetz, Stephanie,Tiley, Laurence,Trehan, Ashok K.,Monkovic, Ivo,Pearce, Bradley,Martel, Alain,Krystal, Mark,Meanwell, Nicholas A.
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p. 2177 - 2180
(2007/10/03)
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- A Complex Induced Proximity Effect in the Anionic Fries Rearrangement of o-Iodophenyl Benzoates: Synthesis of Dihydro-O-methylsterigmatocystin and Other Xanthones
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The success of an anionic Fries rearrangement, used to synthesise dihydro-O-methylsterigmatocystin and other xanthones, is dependent on the presence of a remote methoxyl substituent.
- Horne, Stephen,Rodrigo, Russell
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p. 4520 - 4522
(2007/10/02)
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