2566-22-5Relevant articles and documents
An expedient synthesis of N-(1-(5-mercapto-4-((substituted benzylidene)amino)-4H-1,2,4-triazol-3-yl)-2-phenylethyl)benzamides as jack bean urease inhibitors and free radical scavengers: Kinetic mechanism and molecular docking studies
Saeed, Aamer,Larik, Fayaz Ali,Channar, Pervaiz Ali,Mehfooz, Haroon,Ashraf, Mohammad Haseeb,Abbas, Qamar,Hassan, Mubashir,Seo, Sung-Yum
, p. 764 - 777 (2017)
In this study, some new azomethine-triazole hybrids 5a–5l derived from N-benzoyl-L-phenylalanine were synthesized and characterized. The synthesized compounds showed first-rate, urease inhibition, and compounds 5c and 5e were found to be most effective inhibitors with 0.0137?±?0.00082?μm and 0.0183?±?0.00068?μm, respectively (thiourea 15.151?±?1.27?μm). The kinetic mechanism of urease inhibition revealed the compounds 5c and 5e to be non-competitive inhibitors, whereas compounds 5d and 5j were found to be of mixed-type inhibitors. Docking studies also indicated better interaction patterns with urease enzyme. The results of enzyme inhibition, kinetic mechanism and molecular docking suggest that these compounds can serve as lead compounds in the design of more effective urease inhibitors.
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Onuma et al.
, p. 3163,3164,3166 (1979)
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OCCURRENCE AND BIOSYNTHESIS OF ASPERPHENAMATE IN SOLID CULTURES OF PENICILLIUM BREVICOMPACTUM
Bird, Bruce A.,Campbell, Iain M.
, p. 2405 - 2406 (1982)
The ester of N-benzoylphenylalanine and N-benzoylphenylalaninol, asperphenamate, was isolated from solid cultures of Penicillium brevicompactum.Isotope from L-phenylalanine was well incorporated into both benzoyl groups and into the phenylalanine and phenylalaninol moieties.Isotope from benzoic acid was also well incorporated into asperphenamate.Key Word Index-Penicillium brevicompactum; Hyphomycetes; fungus; biosynthesis; asperphenamate; phenylalanine derivatives.
Electrophilic Sulfonium-Promoted Peptide and Protein Amidation in Aqueous Media
Wan, Chuan,Feng, Yuan,Hou, Zhanfeng,Lian, Chenshan,Zhang, Liang,An, Yuhao,Sun, Jinming,Yang, Dongyan,Jiang, Chenran,Yin, Feng,Wang, Rui,Li, Zigang
supporting information, p. 581 - 586 (2022/01/20)
A novel amidation strategy using electrophilic sulfonium, which is soluble and stable in aqueous conditions, was developed. The sulfoniums could activate thioacid and carboxyl acid to efficiently react with amines to afford amides. This method enables applications in amidation in both aqueous media and solid-phase peptide synthesis, peptide/protein modifications, and reactive lysines of a proteome at pH 10 with activity-based protein profiling. A peptide ligand-directed labeling of the USP7-UBL2 domain was also performed using this method.
Nickel-Catalyzed Multicomponent Coupling: Synthesis of α-Chiral Ketones by Reductive Hydrocarbonylation of Alkenes
Chen, Jian,Zhu, Shaolin
supporting information, p. 14089 - 14096 (2021/09/13)
A nickel-catalyzed, multicomponent regio- and enantioselective coupling via sequential hydroformylation and carbonylation from readily available starting materials has been developed. This modular multicomponent hydrofunctionalization strategy enables the straightforward reductive hydrocarbonylation of a broad range of unactivated alkenes to produce a wide variety of unsymmetrical dialkyl ketones bearing a functionalized α-stereocenter, including enantioenriched chiral α-aryl ketones and α-amino ketones. It uses chiral bisoxazoline as a ligand, silane as a reductant, chloroformate as a safe CO source, and a racemic secondary benzyl chloride or an N-hydroxyphthalimide (NHP) ester of a protected α-amino acid as the alkylation reagent. The benign nature of this process renders this method suitable for late-stage functionalization of complex molecules.
On the intrinsic reactivity of highly potent trypanocidal cruzain inhibitors
Batista, Pedro Henrique Jatai,Bonatto, Vinicius,Cedron, Rodrigo,Cianni, Lorenzo,De Vita, Daniela,Franco, Caio Haddad,Montanari, Carlos A.,Moraes, Carolina Borsoi,Silva, Daniel G.,Tezuka, Daiane Y.,De Albuquerque, Sérgio,Lameira, Jer?nimo,Leit?o, Andrei
supporting information, p. 1275 - 1284 (2020/12/01)
The cysteine protease cruzipain is considered to be a validated target for therapeutic intervention in the treatment of Chagas disease. Hence, peptidomimetic cruzipain inhibitors having a reactive group (known as warhead) are subject to continuous studies