- Design, synthesis, and characterization of novel tetrahydropyran-based bacterial topoisomerase inhibitors with potent anti-gram-positive activity
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There is an urgent need for new antibacterial drugs that are effective against infections caused by multidrug-resistant pathogens. Novel nonfluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) have the potential
- Surivet, Jean-Philippe,Zumbrunn, Cornelia,Rueedi, Georg,Hubschwerlen, Christian,Bur, Daniel,Bruyère, Thierry,Locher, Hans,Ritz, Daniel,Keck, Wolfgang,Seiler, Peter,Kohl, Christopher,Gauvin, Jean-Christophe,Mirre, Azely,Kaegi, Verena,Dos Santos, Marina,Gaertner, Mika,Delers, Jonathan,Enderlin-Paput, Michel,Boehme, Maria
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supporting information
p. 7396 - 7415
(2013/10/21)
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- 5-Quinoline derivatives having an anti-bacterial activity
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The present invention describes novel anti-bacterial compounds of the formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase and topoisomerases, for example of topoisomerase II and IV.
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Page/Page column 8
(2010/12/31)
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- CYCLOHEXYL OR PIPERIDINYL CARBOXAMIDE ANTIBIOTIC DERIVATIVES
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The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl;one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom;either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH═CH or CH2CH2;each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine;and to salts of such compounds of formula (I).
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Page/Page column 29
(2009/05/29)
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- ETHANOL OR 1,2-ETHANEDIOL CYCLOHEXYL ANTIBIOTIC DERIVATIVES
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The invention relates to antibiotic ethanol or 1,2-ethanediol cyclohexyl derivatives of formula (I) wherein R1 represents (C1-C4)alkoxy; one or two of U, V, W and X represent(s) N and the remaining represent each independently CH or, in the case of V or X
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Page/Page column 37-38
(2008/06/13)
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- CYCLOHEXYL OR PIPERIDINYL CARBOXAMIDE ANTIBIOTIC DERIVATIVES
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The invention relates to antibiotic cyclohexyl or piperidinyl carboxamide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRx, Rx being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH=CH or CH2CH2; each of R3, R4, R5, R6, R7 and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9-COOH is a naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).
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Page/Page column 74-75
(2008/06/13)
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- New Piperidine Antibiotics
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The invention relates to novel, antibacterially active piperidine derivatives of the formula wherein one of U and V represents N, the other represents N or CH; M represents CH2CH2, CH═CH, CH(OH)CH(OH), CH(OH)CH2, CH(NHsub
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Page/Page column 15
(2010/11/28)
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- TETRAHYDROPYRANE ANTIBIOTICS
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The invention relates to antibiotic tetrahydro rane derivatives of formula (I).
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Page/Page column 71
(2010/11/28)
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- ANTIBIOTIC COMPOUNDS
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The invention relates to selected antibiotics of formula (Al) wherein R1 represents alkyl, alkoxy, haloalkoxy, halogen or cyano; one or two of U, V, W and X represent(s) N, the remaining represent CH, or, in case of U, V and/or W, may also repr
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Page/Page column 22-23
(2010/11/28)
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- NOVEL COMPOUNDS HAVING AN ANTI-BACTERIAL ACTIVITY
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The present invention describes novel anti-bacterial compounds of formula (I). These compounds are, amongst others, of interest as inhibitors of DNA gyrase.
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Page/Page column 75-76
(2010/10/20)
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- NEW PIPERIDINE ANTIBIOTICS
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The invention relates to novel, antibacterially active piperidine derivatives of the formula (I) wherein one of U and V represents N, the other represents N or CH; M represents CH2CH2, CH=CH, CH(OH)CH(OH), CH(OH)CH2, CH(NH
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Page/Page column 34
(2010/10/20)
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- BETA-AMINOALCOHOL ANTIBIOTICS
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This invention concerns antimicrobially active compounds of the formula (I) wherein R1 represents alkyl, alkoxy, halogen or cyano; R2 represents hydrogen or halogen; R3 represents hydrogen or halogen; one of the symbols W1 and W2 represents CH and the other represents CH or N; U represents oxygen or sulphur; and V represents CO or CH2; as well as their optically pure enantiomers, mixtures of enantiomers, racemates, optically pure diastereoisomers, mixtures of diastereoisomers, diastereoisomeric racemates, mixture of diastereoisomeric racemates, meso forms, pharmaceutically acceptable acid addition salts, solvent complexes and morphological forms thereof.
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Page/Page column 18-19
(2010/11/24)
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- NOVEL COMPOUNDS HAVING AN ANTIBACTERIAL ACTIVITY
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The invention relates to novel antibacterial compounds of formula (I). Said compounds are of interest, inter alia, as topoisomerase IV (topo IV) and DNA gyrase inhibitors.
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Page/Page column 28-30
(2010/02/09)
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- PREPARATION OF 3-SUBSTITUTED QUINOLINES. II. PREPARATION AND CYCLODEHYDRATION OF α-ALKYL- AND α-PHENYL-β-ARYLAMINOACROLEIN DERIVATIVES
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α-Methyl-β-arylaminoacroleins were prepared by the hydrolysis of 2-methyl-1-arylamino-3-arylimino-1-propene derivatives. α-Ethyl- and α-phenyl-β-arylaminoacroleins were prepared by the reaction of arylamine and 2-substituted 1,1,3,3-tetraethoxypropane derivatives. 3-Methyl, 3-ethyl- and 3-phenylquinolines were obtained from α-methyl-, α-ethyl and α-phenyl-β-arylaminoacroleins on heating with aluminum bromide in good yields. α-Bromo-β-anilinoacrolein (9b) was prepared by the reaction of β-anilinoacrolein (6b) and N-bromosuccinimide.Reaction of 9b and aluminum bromide did not afford 3-bromoquinoline.
- Todoriki, Reiko,Ono, Machiko,Tamura, Shinzo
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p. 755 - 769
(2007/10/02)
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