4906-25-6Relevant articles and documents
Pharmacological characterization of a novel nonpeptide antagonist for formyl peptide receptor-like 1?
Zhou, Caihong,Zhang, Song,Nanamori, Masakatsu,Zhang, Yueyun,Liu, Qing,Li, Na,Sun, Meiling,Tian, Jun,Ye, Patrick P.,Cheng, Ni,Ye, Richard D.,Wang, Ming-Wei
, p. 976 - 983 (2007)
A series of quinazolinone derivatives were synthesized based on a hit compound identified from a high-throughput screening campaign targeting the human formyl peptide receptor-like 1 (FPRL1). Based on structure-activity relationship analysis, we found tha
Chemoselective, Scalable Nickel-Electrocatalytic O-Arylation of Alcohols
Baran, Phil S.,Chen, Longrui,Edwards, Jacob T.,Kawamata, Yu,Oderinde, Martins S.,Zhang, Hai-Jun
supporting information, p. 20700 - 20705 (2021/08/17)
The formation of aryl-alkyl ether bonds through cross coupling of alcohols with aryl halides represents a useful strategic departure from classical SN2 methods. Numerous tactics relying on Pd-, Cu-, and Ni-based catalytic systems have emerged over the past several years. Herein we disclose a Ni-catalyzed electrochemically driven protocol to achieve this useful transformation with a broad substrate scope in an operationally simple way. This electrochemical method does not require strong base, exogenous expensive transition metal catalysts (e.g., Ir, Ru), and can easily be scaled up in either a batch or flow setting. Interestingly, e-etherification exhibits an enhanced substrate scope over the mechanistically related photochemical variant as it tolerates tertiary amine functional groups in the alcohol nucleophile.
Synthesis, Antiproliferative and Antioxidant Activity of 3-Mercapto-1,2,4-Triazole Derivatives as Combretastatin A-4 Analogues
Al-Mansury, Sadiq,Balakit, Asim A.,Alkazazz, Fatin Fadhel,Ghaleb, Rana A.
, p. 556 - 565 (2021/09/28)
Two series of 3-mercapto-1,2,4-triazole derivatives containing alkoxy substituents different in size and position were synthesized and their structures were characterized by FT-IR, 1H NMR, 13C NMR spectroscopy and elemental analysis. The synthesized compounds were assessed for their antiproliferative activity against colon cancer cell line (SW480). The results indicated that the size and position of the alkoxy group significantly influenced the antiproliferative activity. The highest cancer cell growth inhibition values were observed for the compounds containing 3,4,5-trimethoxyphenyl groups in their structures (57.74, 54.14 and 60.70% at 50 μM for compounds 5a, 12b and 14, respectively). The synthesized compounds were also subjected to DPPH protocol for evaluating the antioxidant activity. The results showed that all compounds had moderate to high levels of antioxidant capacity as compared to ascorbic acid as standard, the highest free radical scavenging capacity of 75% was observed for compound 4a at 50 μM.
Electro-Oxidative Selective Esterification of Methylarenes and Benzaldehydes
Yu, Congjun,?zkaya, Bünyamin,Patureau, Frederic W.
supporting information, p. 3682 - 3687 (2021/02/01)
A mild and green electro-oxidative protocol to construct aromatic esters from methylarenes and alcohols is herein reported. Importantly, the reaction is free of metals, chemical oxidants, bases, acids, and operates at room temperature. Moreover, the design of the electrolyte was found critical for the oxidation state and structure of the coupling products, a rarely documented effect. This electro-oxidative coupling process also displays exceptional tolerance of many fragile easily oxidized functional groups such as hydroxy, aldehyde, olefin, alkyne, as well as neighboring benzylic positions. The enantiomeric enrichment of some chiral alcohols is moreover preserved during this electro-oxidative coupling reaction, making it overall a promising synthetic tool.
