CAS: 41744-40-5; Sulbenicillin

该化合物是属于青霉素类的半合成抗生素,主要用于抗菌特性,其特点是乙酯结构,这是其行动机制所必不可少的,抑制细菌细胞壁合成.二苯基辛对一系列克阳性和某些克阴性细菌有效,有助于治疗各种感染.该化合物通常以其钠盐形式施用,以提高溶性性和生物利用率.其药理动力学涉及吸收,分配,代谢和排泄,而肾脏清扫是一个重要的消除途径.由于生产乙酸乳腺,苏苯基宁可能对某些细菌菌株产生抗药性,酶可以对乙酸酯环进行水解.与其他抗生酶一样,必须明智地使用丁基盐,以尽量减少抗药性和生物利用性,并确保其在临床环境中的功效.潜在的副作用可能包括过敏反应,胃肠紊乱和正常植物的改变.总体而言,苯基能工具仍然具有价值.

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      专利信息


      专利号:US-2025002508-A1
      优先权日:2020-05-05
      标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof
      发明人:HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS
      权利人:QPEX BIOPHARMA INC
      摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).

      专利号:US-4684724-A
      优先权日:1981-12-25
      标题:4-Cyano-2-azetidinones and production thereof
      发明人:OCHIAI MICHIHIKO; KISHIMOTO SHOJI; MATSUO TAISUKE
      权利人:TAKEDA CHEMICAL INDUSTRIES LTD
      摘要:4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R 1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R 2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR 3 , --SCOR 3 or --S(O) n --R 3 (R 3 being a hydrocarbyl group and n an integer 1 or 2), R 4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO 3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.

      专利号:US-9839642-B2
      优先权日:2014-05-09
      标 题:Beta-tetrazolyl-propionic acids as metallo-beta-lactamase inhibitors
      发明人:TANG HAIFENG; YANG SHU-WEI; MANDAL MIHIR; SU JING; LI GUOQING; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; PAN JIANPING; HAGMANN WILLIAM; DING FA-XIANG; XIAO LI; PASTERNAK ALEXANDER; HUANG YUHUA; DONG SHUZHI; YANG DEXI
      权利人:MERCK SHARP & DOHME
      摘要:The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

      专利号:US-9708336-B2
      优先权日:2014-01-22
      标题 :Metallo-beta-lactamase inhibitors
      发明人:MANDAL MIHIR; TANG HAIFENG; XIAO LI; SU JING; LI GUOQING; YANG SHU-WEI; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; HICKS JACQUELINE; LOMBARDO MATTHEW; CHU HONG; HAGMANN WILLIAM; PASTERNAK ALEX; GU XIN; JIANG JINLONG; DONG SHUZHI; DING FA-XIANG; LONDON CLARE; BISWAS DIPSHIKHA; YOUNG KATHERINE; HUNTER DAVID N; ZHAO ZHIQIANG; YANG DEXI
      权利人:MERCK SHARP & DOHME
      摘要:The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

      专利号:CN-108421514-A
      优先权日:2017-06-29
      标题:A reaction kettle for one-pot synthesis of sulbenicillin sodium and preferential crystallization

      专利号:US-2005053642-A1
      优先权日:2000-08-23
      标题:Biocompatible materials
      发明人:ULBRICHT MATHIAS; THOM VOLKMAR; JANKOVA KATJA; ALTANKOV GEORGE; JONSSON GUNNAR
      摘要:The present invention teaches a novel approach of creating biocmpatible surfaces, said surfaces being capable of functionally interact with biological material. SAid biocompatible surfaces comrise at least two comonents, such as a hydrophobic substratum and a macromolecule of hydrophilic nature, which, in a cooperativity, form together the novel biocoompatible surfaces. The novel approach is ased on contacting said hydrophobic substratum with a laterally patterned monomolecular layer of said hydrophilic and flexible macromolecules, exhibiting a pronounced excluded volume. The htus formed two component surface is, in respect to polarity and morphology, a molecularly heterogeneous surface. Structural features of said macromolecular monolayer (as e.g. the layer thickness or its lateral density) are determined by: i) the structural features of the layer forming macromolecules (as e.g. their MW or their molecular architecture) and ii) the method of creating said monomolecular layer (as e.g. by physi- or chemisorbing, or by chemically binding said macromolecules). The structural features of the layer forming macromolecules(s) is in turn determined by synthesis. AMount and conformation and thus also biological activity of biological material (as e.g. polypeptides) which contact the novel biocompatible surface, is determined and maintained by the cooperative action of the underlying hydrophobic substratum and the macromolecular layer. In this way it becomes possible to maintain and control biological interactions between said contacted polypeptides and other biological compounds as e.g. cells, antibodies and the like. Consequently, the present invention aims to reduce and/or eliminate the deactivation and/or denaturation associated with the contacting of polypeptides and/or other biological material to a hydrophobic substratum surface.
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      主要参考文献


      1: Ripa S, Mignini F, Patrizi I, Ferrante L, Prenna M, Falcioni E. Sulbenicillin: pharmacokinetics and penetration into bronchial secretion in elderly patients. Chemioterapia. 1987 Aug;6(4):277-81. doi: 10.1002/chem.201405058. Epub 2014 Nov 3.
      6: Hakamata M, Hozawa J, Saito H, Fukuoka K, Yamagami M, Usami S. [Evaluation of clinical efficacy of sulbenicillin following surgery of malignant maxillary tumors. Transport of sulbenicillin to the exudates from the surgical wound of the maxilla and its therapeutic effects]. Jpn J Antibiot. 1982 May;35(5):1254-60. Japanese. Japanese.
      9: Macchioni PL, Del Din G, Filippi G, Baricchi R, Bertani A, Portioli I. Clinical assessment of sulbenicillin in acute respiratory tract infection. Drugs Exp Clin Res. 1985;11(12):879-83. Review. Italian.

      合成参考文献


      摘要:S6 | ITNANTIBIOTIC | Antibiotic List from the ITN MSCA ANSWER | DOI:10.5281/zenodo.2621956
      摘要:Shishido M. [Experimental and clinical studies on cortical and subarachoidal application of antibiotics--an electroencephalographical investigation (author's transl)]. Nihon Geka Hokan. 1980 Jan 01;49(1):37–52.
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