202825-61-4Relevant articles and documents
Synthesis and structure activity relationships of cyanopyridone based anti-tuberculosis agents
Boshoff, Helena I. M.,Caljon, Guy,Forbes, He Eun,Hulpia, Fabian,Jian, Yanlin,Munier-Lehmann, Héle?ne,Risseeuw, Martijn D. P.,Van Calenbergh, Serge
, (2020/07/06)
Mycobacterium tuberculosis, the causative agent of tuberculosis, relies on thymidylate kinase (MtbTMPK) for the synthesis of thymidine triphosphates and thus also DNA synthesis. Therefore, this enzyme constitutes a potential Achilles heel of the pathogen. Based on a previously reported MtbTMPK 6-aryl-substituted pyridone inhibitor and guided by two co-crystal structures of MtbTMPK with pyridone- and thymine-based inhibitors, we report the synthesis of a series of aryl-shifted cyanopyridone analogues. These compounds generally lacked significant MtbTMPK inhibitory potency, but some analogues did exhibit promising antitubercular activity. Analogue 11i demonstrated a 10-fold increased antitubercular activity (MIC H37Rv, 1.2 μM) compared to literature compound 5. Many analogues with whole-cell antimycobacterial activity were devoid of significant cytotoxicity.
Ruthenium porphyrin-catalyzed aerobic oxidation of terminal aryl alkenes to aldehydes by a tandem epoxidation-isomerization pathway
Jiang, Gaoxi,Chen, Jian,Thu, Hung-Yat,Huang, Jie-Sheng,Zhu, Nianyong,Che, Chi-Ming
supporting information; experimental part, p. 6638 - 6642 (2009/03/12)
(Figure Presented) Catalytic oxidation of 1-alkenes to aldehydes by an epoxidation-isomerization pathway with air or dioxygen as terminal oxidant has been realized for bulky ruthenium(VI) porphyrin catalysts. For the new, recyclable catalyst [RuVI(tmttp)O2], product yields of up to 99% and total turnover numbers of up to 1144 were obtained.
