scholarly journals 2-Amido-3-(1H-Indol-3-yl)-N-Substitued-Propanamides as a New Class of Falcipain-2 Inhibitors. 1. Design, Synthesis, Biological Evaluation and Binding Model Studies

Molecules ◽  
2009 ◽  
Vol 14 (1) ◽  
pp. 494-508 ◽  
Author(s):  
Jin Zhu ◽  
Tong Chen ◽  
Lili Chen ◽  
Weiqiang Lu ◽  
Peng Che ◽  
...  
2013 ◽  
Vol 29 (5) ◽  
pp. 639-646 ◽  
Author(s):  
Maksym O. Chekanov ◽  
Olga V. Ostrynska ◽  
Sergii S. Tarnavskyi ◽  
Anatoliy R. Synyugin ◽  
Nadiia V. Briukhovetska ◽  
...  

2014 ◽  
Vol 12 (1) ◽  
pp. 38-45 ◽  
Author(s):  
Kothapally. Beulah ◽  
Akula Kumara ◽  
Boddupally Lingaiah ◽  
Pamulaparthy Rao ◽  
Banda Narsaiah ◽  
...  

2021 ◽  
Author(s):  
Rakesh V. Kusurkar ◽  
Rahul H. Rayani ◽  
Anand G. Vala ◽  
Deepa R. Parmar ◽  
Manoj N Bhoi ◽  
...  

Abstract A new class of β-lactam pharmacophore series of 2-Bromo-N-[4-(2-{[2-(substituted phenyl)-3-chloro-4-oxoazetidin-1-yl] amino}-2-oxoethyl) phenyl] pyridine-4-carboxamide derivatives were designed, prepared, and screened for their antimycobacterial activities. The hydrazone derivatives were first synthesized via conventional and microwave methods, and then the β-lactam ring could be constructed via a [2+2] ketenimine cycloaddition. The structure of all synthesized compounds was characterized by FTIR, 1H NMR, 13C NMR, and Mass spectroscopy techniques. All the newly synthesized derivatives were found to be effective in inhibiting M. tuberculosis H37RV strain infection at concentrations of 12.5, 25.0, and 50.0 µg/mL using the MABA method. Amongst, the compound (6e) was found to be good potent antitubercular activity at 12.5 mg/mL concentration in comparison with the rest of the compounds using the standard therapeutic agent Streptomycin. Molecular dynamics simulation studies and Molecular docking studies have been performed against mycobacterial InhA enzyme to gain an insight into the possible mechanistic action in search of good potent antitubercular candidates.


2020 ◽  
Vol 97 ◽  
pp. 103665 ◽  
Author(s):  
Romeo Romagnoli ◽  
Filippo Prencipe ◽  
Paola Oliva ◽  
Maria Kimatrai Salvador ◽  
Andrea Brancale ◽  
...  

2002 ◽  
Vol 124 (45) ◽  
pp. 13382-13383 ◽  
Author(s):  
Paul A. Wender ◽  
Jonathan B. Rothbard ◽  
Theodore C. Jessop ◽  
Erik L. Kreider ◽  
Bryan L. Wylie

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