Twenty four derivatives of N-(phenoxyacetyl)-p-aminophenoxyacetic acid have been obtained. The tests of the in vitro inhibition of prostaglandin synthetase revealed that compounds 19 and 24 have the activity similar to that of Naproxen.
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Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis.
J Med Chem
July 2012
Université Lille Nord de France, F-59000 Lille, France.
In this paper, we describe the screening of a 14640-compound library using a novel whole mycobacteria phenotypic assay to discover inhibitors of EthR, a transcriptional repressor implicated in the innate resistance of Mycobacterium tuberculosis to the second-line antituberculosis drug ethionamide. From this screening a new chemical family of EthR inhibitors bearing an N-phenylphenoxyacetamide motif was identified. The X-ray structure of the most potent compound crystallized with EthR inspired the synthesis of a 960-member focused library.
View Article and Find Full Text PDFSynthesis of phenylphenoxyacetamide derivatives with potential antiinflammatory activity.
Pol J Pharmacol Pharm
November 1981
Twenty four derivatives of N-(phenoxyacetyl)-p-aminophenoxyacetic acid have been obtained. The tests of the in vitro inhibition of prostaglandin synthetase revealed that compounds 19 and 24 have the activity similar to that of Naproxen.
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