CAS: 82009-34-5; (Z)-7-(((R)-2-Amino-2-Carboxyethyl)Thio)-2-((S)-2,2-Dimethylcyclopropane-1-Carboxamido)Hept-2-Enoic Acid

上下游产品

L-Cysteine (Z)-7-bromo-2 ((2s)-2,2-dimethylcyclopropanecarboxamido)-2-heptenoic acid 1,5-dibromo-pentane 2,2-dimethylcyclopropane-1-carboxylic acid

7-Bromo-2-Oxoheptanoic Acid置于氨,Sodium体系中,用 甲苯 作为反应溶剂,化学反应 0.25H,反应生成 西司他丁
参考文献:Inhibition Of The Mammalian .Beta.-Lactamase Renal Dipeptidase (Dehydropeptidase-I) By Z-2-(Acylamino)-3-Substituted-Propenoic Acids
标题:Inhibition Of The Mammalian .Beta.-Lactamase Renal Dipeptidase (Dehydropeptidase-I) By Z-2-(Acylamino)-3-Substituted-Propenoic Acids
摘要:The Title Enzyme Deactivates The Potent Carbapenem Antibiotic Imipenem In The Kidney,Producing Low Antibiotic Levels In The Urinary Tract. A Series Of (Z)-2-(Acylamino)-3-Substituted-Propenoic Acids (3) Are Specific,Competitive Inhibitors Of The Enzyme Capable Of Increasing The Urinary Concentration Of Imipenem In Vivo. Many Of The Compounds Were Prepared In One Step From An Alpha-Keto Acid And A Primary Amide. The Optimum R2 Groups Are 2,2-Dimethyl,-Dichloro,And-Dibromocyclopropyl. With R2 = 2,2-Dimethylcyclopropyl (Dmcp),A Wide Variety Of R3 Groups Including Alkyl,Oxa-And Thiaalkyl,And Alkyl Groups Containing Acidic,Basic,And Neutral Substituents Give Effective Inhibitors With Ki Values Of 0.02-1 Microm And A Range Of Pharmacokinetic Properties. By Resolution Of Enantiomers And X-Ray Crystallography,The Enzyme-Inhibitory Activity Of The Dmcp Group Was Found To Reside With The 1S Isomer. The Cysteinyl Compound 176 (Cilastatin,Mk-0791) Has The Desired Pharmacological Properties And Has Been Chosen For Combination With Imipenem.
DOI:10.1021/jm00389A018

专利信息

专利号:US-2024197774-A1
优先权日:2021-04-16
标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
发明人：LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
权利人:UNIV TEXAS
摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.

专利号:US-2023286915-A1
优先权日:2020-10-07
标 题 :Synthesis of pyrrole acid derivatives
发明人：WILKINSON ANDREW; COOPER LAN; ORR DAVID; FINLAYSON JONATHAN; BUNT ADAM; KIRKHAM JAMES; LYTH DAVID; BLADES KEVIN
权利人:INFEX THERAPEUTICS LTD
摘要:This invention relates to the synthesis of compounds that can be used to treat bacterial infections in combination with other antibacterial agents, and more specifically in combination with a class of antibacterial agents known as carbapenems. The compounds resulting from the novel methods of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.

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:US-8557979-B2
优先权日:2004-06-10
标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
发明人：CHOI WOO-BAEG; KOWALIK EWA
权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-10933051-B2
优先权日:2017-06-09
标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections
发明人：CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN
权利人:FOB SYNTHESIS INC
摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.