CAS: 129791-92-0; Rifalazil

该化合物是麻风素类的合成抗生素,主要以抗菌素特性著称,其特点是能够抑制RNA合成细菌,使其对一系列抗菌性细菌和某些抗菌性细菌有效,该化合物因其针对肺结核的诱因性诱因 ----子细胞肺结核的活动而特别引人注目,并因其在治疗各种细菌感染方面的潜在用途而受到调查.Rifalazil口服生物利用率良好,在肝脏中新陈代谢,其药用植物受到年龄和肝功能等因素的影响.其行动机制涉及对RNA菌性聚合酶的约束,从而防止转录.尽管它在临床应用中表现出希望,但抗药性发育是人们关注的问题,正如许多抗生素一样.此外,其安全情况和副作用是治疗用途中的重要考虑因素.

结构式图片

MSDS等安全信息

    上下游产品

    1-isobutylpiperazine 3'-tert-butyldimethylsilyloxybenzoxazinorifamycin 3'-hydroxy-benzoxazinorifamycin 2-aminoresorcinol hydr°Chloride

    合成工艺路线路线简述

      海关参考信息

      专利信息


      专利号:US-11744867-B2
      优先权日:2017-02-14
      标 题 :Modulation of microbial synthesis of 4-ethylphenol and 4-ethylphenyl sulfate in behavior and disease
      发明人:NEEDHAM BRITTANY D; MAZMANIAN SARKIS K; SHARON GIL; FUNABASHI MASANORI; FISCHBACH MICHAEL A; HSIAO ELAINE Y; PATTERSON PAUL H
      权利人:CALIFORNIA INST OF TECHN; UNIV CALIFORNIA
      摘要:Some embodiments relate to genetically engineered bacterial strains for modulation of levels of the bacterial metabolite 4-ethylphenol (4EP) and its sulfated form, 4-ethylphenyl sulfate (4EPS). In some embodiments, the bacteria reduce or inhibit production of 4EP or 4EPS in the gut of a subject. The bacteria can ameliorate, delay the onset, or reduce the likelihood of one or more symptoms associated with anxiety and/or autism spectrum disorder (ASD) in the subject.

      专利号:WO-2018152133-A1
      优先权日:2017-02-14
      标题 :Modulation of microbial synthesis of 4-etylphenol and 4-ethylphenol sulfate in behavior and disease

      专利号:US-11224624-B2
      优先权日:2017-02-14
      标 题 :Modulation of microbial synthesis of 4-etylphenol and 4-ethylphenyl sulfate in behavior and disease

      专利号:US-2022096575-A1
      优先权日:2017-02-14
      标 题 :Modulation of microbial synthesis of 4-ethylphenol and 4-ethylphenyl sulfate in behavior and disease

      专利号:US-2023226197-A1
      优先权日:2020-06-18
      标 题:Composition and method for new therapeutic agents including guanidinium-presenting dendrimers and branched structures
      发明人:WENDER PAUL; CEGELSKI LYNETTE; BRCIC JASNA; CHOSY MADELINE; RAHN HARRISON P; Sun jiuzhi
      权利人:UNIV LELAND STANFORD JUNIOR
      摘要:The design, synthesis, and biological evaluation of a new family of highly effective conjugate compounds, including dendrimeric moieties and branched structures, are described. Pharmaceutical compositions including the subject dendrimeric conjugates and methods of using the same are also provided. Methods of using the subject dendrimeric conjugates include delivering a cargo moiety conjugated to the dendrimeric moieties and branched structures to a cell under suitable conditions. In certain embodiments, the cell is a bacterial cell population, and the subject compounds reduce the bacterial cell population. In certain embodiments of the methods, the subject compound is capable of eradicating one or more of Gram-positive bacteria, mycobacteria, and Gram-negative bacteria. In certain embodiments of the methods, the subject compound is capable of eradicating bacterial biofilms. Methods of using the subject dendrimeric conjugates include treating a subject for a disease or condition. In certain embodiments, the disease or conditions an infectious disease.
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      主要参考文献


      1: Geisler WM, Pascual ML, Mathew J, Koltun WD, Morgan F, Batteiger BE, Mayes A, Tao S, Hurwitz SJ, Sayada C, Schinazi RF. Randomized, double-blind, multicenter safety and efficacy study of rifalazil compared with azithromycin for treatment of uncomplicated genital Chlamydia trachomatis infection in women. Antimicrob Agents Chemother. 2014 Jul;58(7):4014-9. doi: 10.1128/AAC.02521-14. Epub 2014 May 5.
      2: Jaff MR, Dale RA, Creager MA, Lipicky RJ, Constant J, Campbell LA, Hiatt WR. Anti-chlamydial antibiotic therapy for symptom improvement in peripheral artery disease: prospective evaluation of rifalazil effect on vascular symptoms of intermittent claudication and other endpoints in Chlamydia pneumoniae seropositive patients (PROVIDENCE-1). Circulation. 2009 Jan 27;119(3):452-8. doi: 10.1161/CIRCULATIONAHA.108.815308. Epub 2009 Jan 12. doi: 10.1038/ja.2008.65. doi: 10.1038/ja.2008.64. doi: 10.1124/dmd.108.021832. Epub 2008 Jul 7. doi: 10.1016/S1472-9792(08)70023-4. Review. Epub 2007 Sep 12. Epub 2007 Sep 15. Review. Epub 2007 Apr 26. A randomized, double-blind study comparing single-dose rifalazil with single-dose azithromycin for the empirical treatment of nongonococcal urethritis in men. Sex Transm Dis. 2007 Aug;34(8):545-52. Review.
      18: Labro MT, Ollivier V, Babin-Chevaye C. Interaction of rifalazil with oxidant-generating systems of human polymorphonuclear neutrophils. Antimicrob Agents Chemother. 2005 Dec;49(12):5018-23.

      合成参考文献


      参考文献:10.1248/cpb.41.148
      摘要:Yamane T, Hashizume T, Yamashita K, Konishi E, Hosoe K, Hidaka T, Watanabe K, Kawaharada H, Yamamoto T, Kuze F. Synthesis and biological activity of 3'-hydroxy-5'-aminobenzoxazinorifamycin derivatives. Chem Pharm Bull (Tokyo). 1993 Jan;41(1):148–55. doi: 10.1248/cpb.41.148.
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