35095-45-5Relevant academic research and scientific papers
The first synthesis of podocarflavone A and its analogs and evaluation of their antimycobacterial potential against Mycobacterium tuberculosis with the support of virtual screening
Puranik, Ninad V.,Swami, Sagar,Misar, Ashwini V.,Mamgain, Ritu,Gulawani, Swapnaja S.,Sarkar, Dhiman,Srivastava, Pratibha,Srivastava, Pratibha
supporting information, (2021/03/15)
The first synthetic route developed for Podocarflavone A reported from Podocarpus macrophyllus and its analogs in 7 steps. Computational analysis for binding with the pantothenate kinase (3AVO) of Mycobacterium tuberculosis showed their docking score (ds) in the range of ?8.9 to ?9.3 Kcal/mol. MD simulations delineated the stability of the protein-ligand complexes in the TIP3P model. MMGBSA and MMPBSA values of 8d were ?42.46 Kcal/mol and ?14.58 Kcal/mol, respectively. Further in-vitro antitubercular screening of compounds 8a, 8d, and 8e against M. tuberculosis H37Ra using XRMA protocol exhibited promising antimycobacterial activity with IC50 values 21.82μg/mL, 15.55 μg/mL, and 16.56 μg/mL, respectively. Compounds 8a, 8d, and 8e showed antibacterial activity with IC50 values 41.56 μg/mL, 24.72 μg/mL, and 72.45 μg/mL respectively against the Staphylococcus aureus. 8a and 8d showed inhibition with IC50 values 39.6 μg/mL and 27.64 μg/mL, respectively, against Bacillus subtilis. The present study could help in the further development of lead molecules against tuberculosis.
Regioselective monobromination of (E)-1-(2′-hydroxy-4′, 6′-dimethoxyphenyl)-3-aryl-2-propen-1-ones using bromodimethylsulfonium bromide and synthesis of 8-bromoflavones and 7-bromoaurones
Khan, Abu T.,Choudhury, Abhik,Ali, Shahzad,Musawwer Khan, Md.
experimental part, p. 4852 - 4857 (2012/09/07)
A wide variety of monobrominated compounds 2a-l have been prepared in good yields from (E)-1-(2′-hydroxy-4′,6′-dimethoxyphenyl)-3-aryl-2- propen-1-ones (1a-l) through regioselective ring bromination using 1.5 equiv of bromodimethylsulfonium bromide (BDMS)
Efficient synthesis of polyoxygenated flavones from naturally occurring flavanones
Bovicelli, Paolo,D'Angelo, Vittoria,Collalto, Daniela,Verzina, Antonio,D'Antona, Nicola,Lambusta, Daniela
, p. 1697 - 1701 (2008/03/11)
Flavonoids are constituents of the human diet (they are present in many beverages and food), and in organisms they are responsible for several biological functions, including that of antioxidant. Because of the increasing interest in these molecules, methods for their synthesis and structural modification are of great importance; studies on the biological activities of many of these compounds are insufficient because of their scarcity and/or high cost. We have developed an expeditious synthesis of polyoxygenated flavones, starting from available and inexpensive flavanones, using a bromination- methoxylation procedure. A series of flavonoids that are not otherwise accessible can be prepared using this method. As an example, 3′-demethoxysudachitin, a limited flavone possessing antimicrobial activity against methicillin-resistant Staphylococcus aureus and Helicobacter pylori and acting as a 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenger, was prepared in fairly satisfactory yield.
A highly efficient and environmentally benign synthesis of 6,8-dibromoflavones, 8-bromoflavones, 5,7-dibromoaurones and 7-bromoaurones
Khan, Abu T.,Goswami, Papori
, p. 4937 - 4940 (2007/10/03)
Various ring substituted 6,8-dibromoflavones (3a-e) as well as 8-bromoflavones (3f-j) can be synthesized easily from the corresponding 2′-hydroxychalcones (1a-j) in good yields and in two steps under environmentally benign reaction conditions. This can be
