832-68-8Relevant articles and documents
Novel phenanthridine amide analogs as potential anti-leishmanial agents: In vitro and in silico insights
Aggarwal, Himanshu,Bala?a-Fouce, Rafael,Chandra Sekhar, Kondapalli Venkata Gowri,Karan Kumar, Banoth,Melcón-Fernandez, Estela,Murugesan, Sankaranarayanan,Nandikolla, Adinarayana,Pérez-Pertejo, Yolanda,Srinivasarao, Singireddi
, (2021/11/01)
In the current work, sixteen novel amide derivatives of phenanthridine were designed and synthesized using 9-fluorenone, 4-Methoxy benzyl amine, and alkyl/aryl acids. The characterization of the title compounds was performed using LCMS, elemental analysis, 1HNMR, 13CNMR and single crystal XRD pattern was also developed for compounds A8. All the final analogs were screened in vitro for anti-leishmanial activity against promastigote form of L. infantum strain. Among the tested analogs, four compounds (A-06, A-11, A-12, and A-15) exhibited significant anti-leishmanial activity with EC50 value ranges from 8.9 to 21.96 μM against amastigote forms of tested L. infantum strain with SI ranges of 1.0 to 4.3. From the activity results it was found that A-11 was the most active compound in both promastigote and amastigotes forms with EC50 values 8.53 and 8.90 μM respectively. In-silico ADME prediction studies depicted that the titled compounds obeyed Lipinski's rule of five as that of the approved marketed drugs. The predicted in-silico toxicity profile also confirmed that the tested compounds were non-toxic. Finally, molecular docking and molecular dynamics study was also performed for significantly active compound (A-11) in order to study it's putative binding pattern at the active site of the selected leishmanial trypanothione reductase target as well as to understand the stability pattern of target-ligand complex for 100 ns. Single crystal XRD of compound A-08 revealed that the compound crystallizes in monoclinic C2/c space group and showed interesting packing arrangements.
Synthesis of 6-aminophenanthridines via palladium-catalyzed insertion of isocyanides into N-sulfonyl-2-aminobiaryls
Jiang, Huanfeng,Gao, Hanling,Liu, Bifu,Wu, Wanqing
, p. 17222 - 17225 (2014/05/06)
A robust route to a diverse set of 6-aminophenanthridines via palladium-catalyzed C-H activation of N-sulfonyl-2-aminobiaryl and isocyanide insertion is reported. This transformation could also provide an important approach for building core frameworks of conjugated organic polymer materials.
COMPOUNDS AND COMPOSITIONS AS TLR ACTIVITY MODULATORS
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Page/Page column 290; 297, (2009/10/22)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors, including TLR7 and TLR8. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine (formula I) wherein: X3 is N; X4 is N Or CR3; X5 is -CR4=CR5.
