scholarly journals Diversity‐oriented Synthesis of [2.2]Paracyclophane‐derived Fused Imidazo[1,2‐a]heterocycles by Groebke–Blackburn–Bienaymé Reaction: Accessing Cyclophanyl Imidazole Ligands Library

Author(s):  
Mareen Stahlberger ◽  
Noah Schwarz ◽  
Zahid Hassan ◽  
Christoph Zippel ◽  
Jens Hohmann ◽  
...  
Nature ◽  
2021 ◽  
Vol 592 (7853) ◽  
pp. 225-231
Author(s):  
Miranda J. Baran ◽  
Mark E. Carrington ◽  
Swagat Sahu ◽  
Artem Baskin ◽  
Junhua Song ◽  
...  

2021 ◽  
Vol 20 (1) ◽  
Author(s):  
Akshaykumar Nayak ◽  
Himani Saxena ◽  
Chandramohan Bathula ◽  
Tarkeshwar Kumar ◽  
Souvik Bhattacharjee ◽  
...  

Abstract Background Despite numerous efforts to eradicate the disease, malaria continues to remain one of the most dangerous infectious diseases plaguing the world. In the absence of any effective vaccines and with emerging drug resistance in the parasite against the majority of anti-malarial drugs, the search for new drugs is urgently needed for effective malaria treatment. Methods The goal of the present study was to examine the compound library, based on indoles generated through diversity-oriented synthesis belonging to four different architecture, i.e., 1-aryltetrahydro/dihydro-β-carbolines and piperidine/pyrrolidine-fused indole derivatives, for their in vitro anti-plasmodial activity. Trifluoroacetic acid catalyzed transformation involving tryptamine and various aldehydes/ketones provided the library. Results Among all the compounds screened, 1-aryltetrahydro-β-carbolines 2 and 3 displayed significant anti-plasmodial activity against both the artemisinin-sensitive and artemisinin-resistant strain of Plasmodium falciparum. It was observed that these compounds inhibited the overall parasite growth in intra-erythrocytic developmental cycle (IDC) via reactive oxygen species-mediated parasitic death and thus could be potential anti-malarial compounds. Conclusion Overall the compounds 2 and 3 identified in this study shows promising anti-plasmodial activity that can kill both artemisinin-sensitive and artemisinin-resistant strains of P. falciparum.


2003 ◽  
Vol 125 (48) ◽  
pp. 14670-14671 ◽  
Author(s):  
Kenichiro Itami ◽  
Toshiyuki Kamei ◽  
Jun-ichi Yoshida

ChemInform ◽  
2006 ◽  
Vol 37 (27) ◽  
Author(s):  
Chengxiang Zhou ◽  
Anton V. Dubrovsky ◽  
Richard C. Larock

2011 ◽  
Vol 13 (19) ◽  
pp. 5148-5151 ◽  
Author(s):  
Thiwanka B. Samarakoon ◽  
Joanna K. Loh ◽  
Alan Rolfe ◽  
Lisa S. Le ◽  
Sun Young Yoon ◽  
...  

ChemInform ◽  
2014 ◽  
Vol 45 (18) ◽  
pp. no-no
Author(s):  
Christian Clavette ◽  
Jean-Francois Vincent Rocan ◽  
Andre M. Beauchemin

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