1621-66-5Relevant articles and documents
Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition
Shyam, Mousumi,Verma, Harshita,Bhattacharje, Gourab,Mukherjee, Piyali,Singh, Samsher,Kamilya, Sujit,Jalani, Pushpendu,Das, Swetarka,Dasgupta, Arunava,Mondal, Abhishake,Das, Amit Kumar,Singh, Amit,Brucoli, Federico,Bagnéris, Claire,Dickman, Rachael,Basavanakatti, Vinay N.,Naresh Babu, Patibandla,Sankaran, Vadivelan,Dev, Abhimanyu,Sinha, Barij Nayan,Bhakta, Sanjib,Jayaprakash, Venkatesan
, p. 234 - 256 (2022/01/20)
In this study, we have designed and synthesized pyrazoline analogues that partially mimic the structure of mycobactin, to address the requirement of novel therapeutics to tackle the emerging global challenge of antimicrobial resistance (AMR). Our investigation resulted in the identification of novel lead compounds 44 and 49 as potential mycobactin biosynthesis inhibitors against mycobacteria. Moreover, candidates efficiently eradicated intracellularly surviving mycobacteria. Thermofluorimetric analysis and molecular dynamics simulations suggested that compounds 44 and 49 bind to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway. To the best of our knowledge, these are the first rationally designed mycobactin inhibitors to demonstrate an excellent in vivo pharmacokinetic profile. In addition, these compounds also exhibited more potent whole-cell efflux pump inhibition than known efflux pump inhibitors verapamil and chlorpromazine. Results from this study pave the way for the development of 3-(2-hydroxyphenyl)-5-(aryl)-pyrazolines as a new weapon against superbug-associated AMR challenges.
Design, synthesis and biological activity of flavonoid derivatives as selective agonists for neuromedin U 2 receptor
Ma, Ming-Liang,Li, Ming,Gou, Jiao-Jiao,Ruan, Tian-Yu,Jin, Hai-Shan,Zhang, Ling-Hong,Wu, Liang-Chun,Li, Xiao-Yan,Hu, Ying-He,Wen, Ke,Zhao, Zheng
, p. 6117 - 6123 (2015/02/02)
Central neuromedin U 2 receptor (NMU2R) plays important roles in the regulation of food intake and body weight. Identification of NMU2R agonists may lead to the development of pharmaceutical agents to treat obesity. Based on the structure of rutin, a typi
3,4-Dihydroxychalcones as potent 5-lipoxygenase and cyclooxygenase inhibitors
Sogawa,Nihro,Ueda,Izumi,Miki,Matsumoto,Satoh
, p. 3904 - 3909 (2007/10/02)
A novel series of 3,4-dihydroxychalcones was synthesized to evaluate their effects against 5-lipoxygenase and cyclooxygenase. Almost all compounds exhibited potent inhibitory effects on 5-lipoxygenase with antioxidative effects, and some also inhibited cyclooxygenase. The 2',5'-disubstituted 3,4- dihydroxychalcones with hydroxy or alkoxy groups exhibited optimal inhibition of cyclooxygenase. We found that 2',5'-dimethoxy-3,4-dihydroxychalcone (37; HX-0836) inhibited cyclooxygenase to the same degree as flufenamic acid and 5-lipoxygenase, more than quercetin. Finally, these active inhibitors of 5- lipoxygenase inhibited arachidonic acid-induced mouse ear edema more than phenidone.
