889945-78-2Relevant academic research and scientific papers
Imidazolopiperazines: Hit to lead optimization of new antimalarial agents
Wu, Tao,Nagle, Advait,Kuhen, Kelli,Gagaring, Kerstin,Borboa, Rachel,Francek, Caroline,Chen, Zhong,Plouffe, David,Goh, Anne,Lakshminarayana, Suresh B.,Wu, Jeanette,Ang, Hui Qing,Zeng, Peiting,Kang, Min Low,Tan, William,Tan, Maria,Ye, Nicole,Lin, Xuena,Caldwell, Christopher,Ek, Jared,Skolnik, Suzanne,Liu, Fenghua,Wang, Jianling,Chang, Jonathan,Li, Chun,Hollenbeck, Thomas,Tuntland, Tove,Isbell, John,Fischli, Christoph,Brun, Reto,Rottmann, Matthias,Dartois, Veronique,Keller, Thomas,Diagana, Thierry,Winzeler, Elizabeth,Glynne, Richard,Tully, David C.,Chatterjee, Arnab K.
, p. 5116 - 5130 (2011)
Starting from a hit series from a GNF compound library collection and based on a cell-based proliferation assay of Plasmodium falciparum, a novel imidazolopiperazine scaffold was optimized. SAR for this series of compounds is discussed, focusing on optimi
A chemoselective Ugi-type reaction in water using TMSCN as a functional isonitrile equivalent: Generation of heteroaromatic molecular diversity
Guchhait, Sankar Kumar,Chaudhary, Vikas,Madaan, Chetna
, p. 9271 - 9277,7 (2012/12/12)
KF-mediated nucleophilic activation of TMSCN as a functional isonitrile equivalent establishes an efficient and chemoselective Ugi-type multicomponent reaction of a heterocyclic amidine and aldehyde with TMSCN in water. In this approach, the use of isocyanide is circumvented, known competing reactions are virtually eliminated, pure products are obtained by a non-chromatographic method, and therapeutically relevant and diverse N-fused 3-aminoimidazoles can be prepared from a wide variety of aldehydes and heterocyclic amidines. This reaction coupling with cascade cyclization provides various privileged tetracyclic heteroaromatic scaffolds.
