摘要:
The invention relates to new compounds having heptose synthesis inhibitory properties, of formula (I) or a pharmaceutically acceptable salt, or prodrug thereof, wherein A is an aryl or heterocycle, optionally substituted by one or several identical or different R such as H, C1-C10 alkyl, C1-C10 alkyl-OR1, C1-C10 alkyl-NR1R1, alkoxy, hydroxy, thioalkyl, aryl, heterocycle, halogen, nitro, cyano, CO2R1, NR1R1, NR1C(O)R1, C(O)NR1R1, NR1C(S)R1, C(S)NR1R1, SO2NR1R1, SO2R1, NR1SO2R1, NR1C(O)NR1R1, NR1C(O)OR1, NR1C(S)NR1R1, NR1C(S)OR1, R1C═NOR1, C(O)R1, aryloxy, thioaryl, alkenyl, alkynyl R1 identical or different is H or C1-C10 alkyl B1, B2, B3 identical or not represent C, N, O, S to form a five-membered aromatic ring wherein from one to three carbon atoms are replaced by a heteroatom selected from S, O, N optionally substituted by one or several identical or different R such as defined above B4 is C or N Y is H, C1-C10 alkyl, alkoxy, thio-alkyl, optionally substituted by one or several identical or different R such as defined above W is C, O or N, substituted or not by one or several C1-C10 alkyl radicals D is an heterocycle optionally substituted by one or several identical or different R such as defined above.
摘要翻译:本发明涉及具有式(I)的肝素合成抑制性质的新化合物或其药学上可接受的盐或前药,其中A是芳基或杂环,任选被一个或多个相同或不同的R如H,C1 C 1 -C 10烷基-OR 1,C 1 -C 10烷基-NR 1 R 1,烷氧基,羟基,硫代烷基,芳基,杂环,卤素,硝基,氰基,CO 2 R 1,NR 1 R 1,NR 1 C(O)R 1,C(O)NR 1 R 1, NR 1 C(S)R 1,C(S)NR 1 R 1,SO 2 NR 1 R 1,SO 2 R 1,NR 1 SO 2 R 1,NR 1 C(O)NR 1 R 1,NR 1 C(O)OR 1,NR 1 C R1,芳氧基,硫代芳基,烯基,炔基R1相同或不同,是H或C1-C10烷基B1,B2,B3相同或不表示C,N,O,S,形成五元芳环,其中一至三碳 原子被选自S,O,N的杂原子替代,任选地被一个或多个相同或不同的R取代,如上定义。B4是C或NY是H,C1-C10烷基,烷氧基,硫代烷基,任选被一个 或几个iden 如W所定义的不同的R是C,O或N,被一个或多个C 1 -C 10烷基取代或不被取代,D是任选被一个或多个相同或不同的R如上所定义的R取代的杂环。
摘要:
The invention relates to Imidazolo-heteroaryl derivatives of formula (I). The compounds inhibit the activity of the Dlta enzyme of Gram-positive bacteria and are useful to treat Gram-positive bacterial infections. Furthermore the application discloses method for assessing the Dlta inhibitory activity of tested molecules and a method for measuring the efficacy of molecules in inhibiting bacteria proliferation in vitro.
摘要:
The invention relates to Imidazolo-heteroaryl derivatives of formula (I). The compounds inhibit the activity of the Dlta enzyme of Gram-positive bacteria and are useful to treat Gram-positive bacterial infections. Furthermore the application discloses method for assessing the Dlta inhibitory activity of tested molecules and a method for measuring the efficacy of molecules in inhibiting bacteria proliferation in vitro.
摘要:
The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
摘要:
The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
摘要:
The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
摘要:
The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
摘要:
Group B streptococcus is an important cause of maternal and neonatal morbidity and mortality in many part of the world. The invention is a method of identification of novel targets for inhibitors preventing septicemic dissemination of Streptococcus agalactiae, a model of Gram positive bacteria, in order to treat bacterial infections using these virulence determinant.
摘要:
The invention relates to a method for identifying and selecting a gene required for the proliferation in vivo of a pathogenic microorganism, comprising: using a strain of the pathogenic microorganism, generating mutants for inactivation in the genes encoding these factors, determining the virulence of these mutants on an expiremental model of infection, and their effect on enteric colonization in an axenic mouse model, and selecting the bacterial genes essential for resistance to serum in vitro, and essential, in the host, for dissemination in the serum. Application to the screening of compounds which inhibit the products of the genes identified, and to the inhibition in vitro of the proliferation of a pathogenic microorganism in serum.
摘要:
Novel antisense sequences to the unspliced or single spliced portions of mRNA transcript from HIV-1 provirus, optionally co-expressed with an inhibitory transdominant mutant HIV-1 protein, are found to be useful in the treatment of HIV-1 infection.