- TRICYCLIC ANTIBIOTICS
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Compounds of formula (I), wherein A1 represents -0-, -S- or -CH2-; A2 represents -CH2- or -0-; A3 represents C3-C8cycloalkylene; saturated or unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen or oxygen, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, -C(=0)-; G represents aryl or heteroaryl, which is unsubstituted or substituted; X1 represents a nitrogen atom or CR1; R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom; m is 0 or 1; n is 1; the -(CH2)n- group is unsubstituted or substituted; p is 0 or 1; or pharmaceutically acceptable salts thereof are valuable for use as a medicament for the treatment of bacterial infections.
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Page/Page column 58
(2013/02/28)
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- TRICYCLIC ANTIBIOTICS
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Compound of formula (I): wherein A1 represents -O-, -S- or -N-R3; A2 represents -CH2-, -O-, -N-R4, -C(=O)- or -CH(O-R4)-; A3 represents C3-C8cycloalkylene; saturated and unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, C2-C4alkenylene, >C=O or a group selected from - C2H4NH-, -C2H4O-, and -C2H4S- being linked to the adjacent NR5-group via the carbon atom; and G represents aryl or heteroaryl, which is unsubstituted or substituted and R1 and R2 independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylcarbonyloxy, C1-C6alkylsulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclylcarbonyloxy, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted; R3, R4 and R5 independently of one another, represent hydrogen or C1-C6alkyl; X1 and X2 independently of one another, represent a nitrogen atom or CR2, with the proviso that at least one of Xl and X2 represents a nitrogen atom; m is 1; and the (CH2)m moiety is optionally substituted by C1-C4alkyl; halogen, carboxy, hydroxy, C1-C4alkoxy, C1-C4-alkylcarbonyloxy, amino, mono- or di-(C1-C4alkyl)amino or acylamino n is 0, 1 or 2 or pharmaceutically acceptable salt thereof are valuable for use as a medicament for the treatment of bacterial infections.
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Page/Page column 56
(2011/07/07)
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- Chemistry of Diazopolycarbonyl Compounds. I. Synthesis and Chemical Properties of Alkyl 3-Diazo-2-oxopropionates
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Alkyl esters of 3-diazo-2-oxopropionic acid have been synthesized.Their aminolysis gives rise to substituted 3-diazo-2-oxopropionamides.The occurrence of cis-trans isomerism in the series of the diazo esters and diazo amides was established by spectral methods and quantum-chemical calculations.The compounds prepared and 1,4-bis(diazo)-2,3-butanedione undergo cyclization into 1-amino-1,2,5,6-tetrahydro-1,2,3-triazine-5,6-dione under the action of hydrazine hydrate.When treated with sodium ethoxide, N-benzyl-3-diazo-2-oxopropionamide undergoes ring closure into 1-benzyl-1,2,5,6-tetrahydro-1,2,3-triazine-5,6-dione, whereas the diazo esters are converted into 3-diazo-2-oxopropionic acid sodium salt.
- Zalesov, V. V.,Vyaznikova, N. G.,Shurov, S. N.,Andreichikov, Yu. S.
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p. 1005 - 1010
(2007/10/03)
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