27460-85-1Relevant academic research and scientific papers
Stereoselective synthesis of (?)-cytoxazone and its unnatural congener (+)-5-epi-cytoxazone
Miranda, Izabel Luzia,dos Santos, Pedro Henrique Costa,Kohlhoff, Markus,Purgato, Gislaine Aparecida,Diaz, Marisa Alves Nogueira,Diaz-Mu?oz, Gaspar
, p. 479 - 489 (2021/07/12)
An interesting protocol for stereoselective synthesis of (?)-cytoxazone and its unnatural stereoisomer (+)-5-epi-cytoxazone from d-4-hydroxyphenylglycine in overall yields of 10% and 16%, respectively, is described. The stereoselective addition of cyanide
Structure-based screening for the discovery of 1,2,4-oxadiazoles as promising hits for the development of new anti-inflammatory agents interfering with eicosanoid biosynthesis pathways
Bifulco, Giuseppe,Chini, Maria Giovanna,D'Auria, Maria Valeria,De Marino, Simona,Festa, Carmen,Giordano, Assunta,Hofstetter, Robert Klaus,Maione, Francesco,Potenza, Marianna,Saviano, Anella,Sciarretta, Martina,Werz, Oliver
, (2021/07/28)
The multiple inhibition of biological targets involved in pro-inflammatory eicosanoid biosynthesis represents an innovative strategy for treating inflammatory disorders in light of higher efficacy and safety. Herein, following a multidisciplinary protocol
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts
Le Manach, Claire,Dam, Jean,Woodland, John G.,Kaur, Gurminder,Khonde, Lutete P.,Brunschwig, Christel,Njoroge, Mathew,Wicht, Kathryn J.,Horatscheck, André,Paquet, Tanya,Boyle, Grant A.,Gibhard, Liezl,Taylor, Dale,Lawrence, Nina,Yeo, Tomas,Mok, Sachel,Eastman, Richard T.,Dorjsuren, Dorjbal,Talley, Daniel C.,Guo, Hui,Simeonov, Anton,Reader, Janette,Van Der Watt, Mari?tte,Erlank, Erica,Venter, Nelius,Zawada, Jacek W.,Aswat, Ayesha,Nardini, Luisa,Coetzer, Theresa L.,Lauterbach, Sonja B.,Bezuidenhout, Belinda C.,Theron, Anjo,Mancama, Dalu,Koekemoer, Lizette L.,Birkholtz, Lyn-Marie,Wittlin, Sergio,Delves, Michael,Ottilie, Sabine,Winzeler, Elizabeth A.,Smith, Dennis,Fidock, David A.,Street, Leslie J.,Basarab, Gregory S.,Duffy, James,Chibale, Kelly
supporting information, p. 2291 - 2309 (2021/03/01)
A novel diazaspiro[3.4]octane series was identified from a Plasmodium falciparum whole-cell high-throughput screening campaign. Hits displayed activity against multiple stages of the parasite lifecycle, which together with a novel sp3-rich scaffold provided an attractive starting point for a hit-to-lead medicinal chemistry optimization and biological profiling program. Structure-activity-relationship studies led to the identification of compounds that showed low nanomolar asexual blood-stage activity (50 nM) together with strong gametocyte sterilizing properties that translated to transmission-blocking activity in the standard membrane feeding assay. Mechanistic studies through resistance selection with one of the analogues followed by whole-genome sequencing implicated the P. falciparum cyclic amine resistance locus in the mode of resistance.
Synthesis method of cefprozil
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Paragraph 0011; 0024-0032, (2020/06/24)
The invention discloses a synthesis method of cefprozil. The method comprises the following steps: carrying out a reaction of a compound II and di-tert-butyl dicarbonate ester under the condition of 4-dimethylaminopyridine to prepare a compound III, after reaction between the compound III and oxalyl chloride, carrying out a reaction between the compound III and a compound IV to prepare a compoundV, and performing deprotection to prepare the final product, namely cefprozil (I). The raw materials for the reaction are easily available, the process route is simple, the total yield is high, the byproducts are few and the method is suitable for industrialized production.
POLYMER COMPOSITIONS COMPRISING COMPOUNDS DERIVED FROM BIOLOGY
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Paragraph 0064, (2020/07/21)
A compound comprises a moiety selected from a cyclic dimer of a first and a second amino acid or a 2.5-diketopiperazine made from an amino acid. The moiety can be produced by fermentation. The compound further includes a polymerizable group. Additionally,
PENICILLIN-BINDING PROTEIN INHIBITORS
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Paragraph 00168, (2018/12/13)
Described herein are certain boron-containing compounds, compositions, preparations and their use as modulators of the transpeptidase function of bacterial penicillin-binding proteins and as antibacterial agents. In some embodiments, the compounds described herein inhibit penicillin-binding proteins. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
Synthesis of bicyclic tripeptides inspired by the ABC-ring system of vancomycin through ruthenium-based cyclization chemistries
Yang, Xin,Beroske, Lucas P.,Kemmink, Johan,Rijkers, Dirk T.S.,Liskamp, Rob M.J.
supporting information, p. 4542 - 4546 (2017/10/31)
The synthesis of a bicyclic tripeptide that mimics the ABC ring system of vancomycin is described by using a ring closing metathesis (RCM) – peptide coupling – ruthenium-catalyzed azide-alkyne cycloaddition (RuAAC) strategy.
A facile Fmoc solid phase synthesis strategy to access epimerization-prone biosynthetic intermediates of glycopeptide antibiotics
Brieke, Clara,Cryle, Max J.
supporting information, p. 2454 - 2457 (2014/05/20)
A rapid protocol based on Fmoc-chemistry for the solid phase peptide synthesis of vancomycin- and teicoplanin-type peptides is described. Epimerization of highly racemization-prone arlyglycine derivatives is suppressed through optimized Fmoc-deprotection
Synthesis of optically active conjugated polymers bearing m-terphenylene moieties by acetylenic coupling polymerization: Chiral aggregation and optical properties of the product polymers
Miyagi, Yu,Sogawa, Hiromitsu,Shiotsuki, Masashi,Sanda, Fumio
, p. 1594 - 1603 (2014/04/03)
The acetylenic coupling polymerization of D-hydroxyphenylglycine-derived m-terphenylene diynes 1-5 using Pd/Cu catalyst gave the corresponding polymers [poly(1)-poly(5)] with Mn = 12 000-60 000 in 53-89% yields. The polymers were soluble in THF
Stereocontrolled syntheses of peptide thioesters containing modified seryl residues as probes of antibiotic biosynthesis
Gaudelli, Nicole M.,Townsend, Craig A.
, p. 6412 - 6426 (2013/07/26)
Methods have been developed to synthesize tri- and pentapeptide thioesters containing one or more p-(hydroxyphenyl)glycine (pHPG) residues and l-serine, some where the latter is O-phosphorylated, O-acetylated, or exists as a β-lactam. Selection of orthogo
