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Second-generation sulfonamide inhibitors of d-glutamic acid-adding enzyme: activity optimisation with conformationally rigid analogues of d-glutamic acidSosič, Izidor ...D-Glutamic acid-adding enzyme (MurD) catalyses the essential addition of D-glutamic acid to the cytoplasmic peptidoglycan precursor UDP-N-acetylmuramoyl-L-alanine, and as such it represents an ... important antibacterial drug-discovery target enzyme. Based on a series of naphthalene-N-sulfonyl-DGlu derivatives synthesised recently, we synthesised two series of new, optimised sulfonamide inhibitors of MurD that incorporate rigidified mimetics of D-Glu. The compounds that contained either constrained D-Glu or related rigid D-Glu mimetics showed significantly better inhibitory activities than the parent compounds, thereby confirming the advantage of molecular rigidisation in the design of MurD inhibitors. The binding modes of the best inhibitors were examined with high-resolution NMR spectroscopy and X-ray crystallography. We have solved a new crystal structure of the complex of MurD with an inhibitor bearing a 4-aminocyclohexane-1,3-dicarboxyl moiety. These data provide an additional step towards the development of sulfonamide inhibitors with potential antibacterial activities.Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 46, no. 7, 2011, str. 2880-2894)Type of material - article, component partPublish date - 2011Language - englishCOBISS.SI-ID - 3001457
Author
Sosič, Izidor |
Barreteau, Hélene |
Simčič, Mihael |
Šink, Roman |
Cesar, Jožko |
Zega, Anamarija |
Golič Grdadolnik, Simona |
Contreras Martel, Carlos |
Dessen, Andréa |
Amoroso, Ana |
Joris, Bernard |
Blanot, Didier |
Gobec, Stanislav, 1970-
Topics
MurD inhibitorji |
ko-kristalne strukture |
optimizacija |
D-glutaminska kislina |
antibakterijsko delovanje
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Sosič, Izidor | 30816 |
Barreteau, Hélene | |
Simčič, Mihael | 28554 |
Šink, Roman | 28862 |
Cesar, Jožko | 19062 |
Zega, Anamarija | 18633 |
Golič Grdadolnik, Simona | 08329 |
Contreras Martel, Carlos | |
Dessen, Andréa | |
Amoroso, Ana | |
Joris, Bernard | |
Blanot, Didier | |
Gobec, Stanislav, 1970- | 15284 |
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