CAS: 102507-71-1; Tigemonam

该化合物是属于乙型乳母抗生素类的合成抗生素,特别是单体,其特点是对各种克己型阴性细菌广泛开展抗生素活动,使其成为治疗这些病原体感染的宝贵选择;提格蒙禁止细菌细胞墙合成,最终导致细胞分解和死亡;其独特结构使其能够避开细菌产生的一些常见乙型乳母,增强抗抗菌菌株的功效;提格蒙通常通过注射进行,并研究其药用植物基因学,显示人体组织内的分布良好;虽然对一系列感染有效,但其使用可能因潜在副作用和细菌抗药性出现而受到限制;与其他抗生素一样,必须明智地使用提格蒙来保持其效力和尽量减少抗药性的发展.

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CAS号80543-73-3 (Z)-2-(2-aminot...

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    📜(Z)-2-氨基-α-[[[[[(二苯基甲基)氧]羰基]甲基]氧]亚胺]-4-噻唑乙酸置于三正丁胺,苯甲醚,N,N'-二环己基碳二亚胺,三氟乙酸体系中,用 二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应生成替吉莫南
    参考文献:氨基噻唑(亚胺氧乙酸)乙酸的区域选择性活化:单环内酰胺氨曲南的高效合成
    标题:氨基噻唑(亚胺氧乙酸)乙酸的区域选择性活化:单环内酰胺氨曲南的高效合成
    摘要:单环内酰胺氨曲南的有效合成[[2S-[2α,3β(Z)]]-3[[(2-氨基-4-噻唑基)[(1-羧基-1-甲基乙氧基)亚氨基]乙酰基]氨基]-2-甲基-4-氧代-1-氮杂环丁烷磺酸] (1) 描述了用区域选择性活化的氨基噻唑亚胺氧基乙酸二酸 15 或 18 酰化 α-氨基氮杂环丁酮 22.二苯甲基酯 10 与 N-羟基苯并三唑和二环己基碳二亚胺反应,然后酯脱保护形成一元酸酰胺 15.或者,二酸 9 的化学选择性瞬时甲硅烷基化,然后用 N-羟基琥珀酰亚胺活化形成活性酯 18.α-氨基氮杂环丁酮 22 用酰胺酰化15 或酯 18 以 75-85% 的收率产生氨曲南 (1).
    Doi:10.1021/op025572D

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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-2016326157-A1
    优先权日:2014-01-06
    标 题:Monobactams and methods of their synthesis and use
    发明人:MYERS ANDREW G; Seiple lan Bass; SUSSMAN ROBIN JUDITH
    权利人:HARVARD COLLEGE
    摘要:Described herein are monobactam antibiotics of Formula (I), (I′), (II), and (II′), along with methods and intermediates for preparing these compounds. Pharmaceutical compositions and methods of treating infectious diseases using the monobactams are also provided.

    专利号:US-9149445-B2
    优先权日:2009-07-27
    标 题:Inhibition of glycerol-3-phosphate acyltransferase (GPAT) and associated enzymes for treatment of viral infections
    发明人:LIU SEAN; RABINOWITZ JOSHUA D; SHENK THOMAS
    权利人:LIU SEAN; RABINOWITZ JOSHUA D; SHENK THOMAS; UNIV PRINCETON
    摘要:A method of treating or preventing a viral infection in a mammal by administering a compound or pharmaceutically acceptable derivative thereof that inhibits a phosphatidic acid synthesis enzyme.

    专利号:US-2015150995-A1
    优先权日:2012-08-09
    标题:Conjugated anti-microbial compounds and conjugated anti-cancer compounds and uses thereof
    发明人:TAFT III KARL MILTON; ENGELKING JARRED ROY
    权利人:PONO CORP
    摘要:Disclosed herein are synthesis methods for generation of conjugated anti-microbial compounds and conjugated anti-cancer compounds. Several embodiments, related to the uses of such compounds in the treatment of infections, in particular those caused by drug-resistant bacteria. Some embodiments relate to targeting cancer based on the metabolic signature of tumor cells.

    专利号:US-2014315720-A1
    优先权日:2012-10-24
    标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
    发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
    权利人:CELANESE ACETATE LLC
    摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

    专利号:WO-2015103583-A1
    优先权日:2014-01-06
    标 题 :Monobactams and methods of their synthesis and use

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    主要参考文献


    1: Nélet F, Gutmann L, Kitzis MD, Acar JF. Tigemonam activity against clinical isolates of Enterobacteriaceae and Enterobacteriaceae with known mechanisms of resistance to beta-lactam antibiotics. J Antimicrob Chemother. 1989 Aug;24(2):173-81.
    4: Chin NX, Neu HC. Tigemonam, an oral monobactam. Antimicrob Agents Chemother. 1988 Jan;32(1):84-91.
    5: Fuchs PC, Jones RN, Barry AL. In vitro antimicrobial activity of tigemonam, a new orally administered monobactam. Antimicrob Agents Chemother. 1988 Mar;32(3):346-9.

    合成参考文献


    摘要:Cocuzza G, Raimondi A. Comparative antibacterial activity of the new oral monobactam tigemonam (SQ 30836) against urinary isolates. J Chemother. 1989 Jul;1(4 Suppl):126–8.
    摘要:Mironidou M, Giala M, Papaioannidou P, Karakiulakis G, Zachariades B, Paradelis AG. Antimicrobial agents and neuromuscular blockade. J Chemother. 1989 Jul;1(4 Suppl):602–3.
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