134575-12-5Relevant academic research and scientific papers
METALLO-BETA-LACTAMASE INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 44-45, (2019/02/06)
The present invention relates to metallo-β-lactamase inhibitor compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Z, RA, X1, X2 and R1 are as defined herein. The present invention also relates to compositions which comprise a metallo-β-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
CANNABINOID RECEPTOR LIGANDS
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Page/Page column 51-52, (2008/06/13)
Compounds of Formula (I) and/or pharmaceutically acceptable salts, solvates or prodrugs thereof, or pharmaceutical compositions containing such compounds exhibit anti-inflammatory and immunomodulatory activity, and can be effective asCB2 receptor ligands in treating cancer and inflammatory, immunomodulatory or respiratory diseases or conditions.
Synthesis of new fluoroquinolones and evaluation of their in vitro activity on Toxoplasma gondii and Plasmodium spp.
Anquetin,Rouquayrol,Mahmoudi,Santillana-Hayat,Gozalbes,Greiner,Farhati,Derouin,Guedj,Vierling
, p. 2773 - 2776 (2007/10/03)
The synthesis of four new computer-designed fluoroquinolones which have been predicted by QSAR analysis to be active against the protozoa Toxoplasma gondii is described. These compounds are inhibitory in vitro for T. gondii. One of these compounds has a remarkably high activity comparable to that of trovafloxacin. It combines the basic cyclopropyl-quinoline structure of gatifloxacin or moxifloxacin with the C-7 6-amino-3-azabicyclo[3.1.0]hexyl side chain of trovafloxacin. The four compounds are also inhibitory for blood stages of Plasmodium falciparum though at high concentration. These results confirm the potential of quinolones as anti-T. gondii and antimalarial drugs but also show that the QSAR models for T. gondii cannot be reliably extended for screening antimalarial activity.
Azabicyclo quinolone carboxylic acids
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, (2008/06/13)
Quinolone carboxylic acids 7-substituted by azabicyclo groups have antibacterial activity., Antibacterial wherein, R1 is hydrogen, a pharmaceutically acceptable cation, or alkyl;, Y, when taken independently, is ethyl, t-butyl, vinyl, cyclopropyl, 2-fluoroethyl, p-fluorophenyl, or o,p-difluorophenyl;, W is hydrogen, F, Cl, Br, alkyl, alkoxy, NH2, NHCH3;, A is CH, CF, CCl, COCH3, C-CH3, C-CN or N; or, A is carbon and is taken together with Y and the carbon and nitrogen to which A and Y are attached to form a five or six membered ring which may contain oxygen or a double bond, and which may have attached thereto R8 which is methyl or methylene; and, R2 is wherein R3, R4, R5, R6, R7, R9, R10 and R25 are each independently H, CH3, CH2NH2, CH2NHCH3 or CH2NHC2H5, and R5, R6, R7, and R9 may also independently be NH2, NHCH3 or NHC2H5.
