128255-31-2Relevant articles and documents
Design and synthesis of chiral urea-derived iodoarenes and their assessment in the enantioselective dearomatizing cyclization of a naphthyl amide
Tariq, M.Umair,Moran, Wesley J.
, (2020)
A novel family of urea-derived chiral iodoarenes was designed and synthesized for use in enantioselective iodine(I/III) catalysis. Their preparation required the development of a bidirectional synthetic strategy. These new chiral iodoarenes were assessed as catalysts in the dearomatizing cyclization of a naphthyl amide and provided moderate yields of product in some cases with low enantioselectivities.
Synthesis and structure-activity relationship study of pyrrolidine-oxadiazoles as anthelmintics against Haemonchus contortus
Ruan, Banfeng,Zhang, Yuezhou,Tadesse, Solomon,Preston, Sarah,Taki, Aya C.,Jabbar, Abdul,Hofmann, Andreas,Jiao, Yaqing,Garcia-Bustos, Jose,Harjani, Jitendra,Le, Thuy Giang,Varghese, Swapna,Teguh, Silvia,Xie, Yiyue,Odiba, Jephthah,Hu, Min,Gasser, Robin B.,Baell, Jonathan
supporting information, (2020/02/04)
Parasitic roundworms (nematodes) are significant pathogens of humans and animals and cause substantive socioeconomic losses due to the diseases that they cause. The control of nematodes in livestock animals relies heavily on the use of anthelmintic drugs. However, their extensive use has led to a widespread problem of drug resistance in these worms. Thus, the discovery and development of novel chemical entities for the treatment of parasitic worms of humans and animals is needed. Herein, we describe our medicinal chemistry optimization efforts of a phenotypic hit against Haemonchus contortus based on a pyrrolidine-oxadiazole scaffold. This led to the identification of compounds with potent inhibitory activities (IC50 = 0.78–22.4 μM) on the motility and development of parasitic stages of H. contortus, and which were found to be highly selective in a mammalian cell counter-screen. These compounds could be used as suitable chemical tools for drug target identification or as lead compounds for further optimization.
NOVEL ALKENE OXINDOLE DERIVATIVES
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Page/Page column 35, (2011/04/18)
The present invention provides compounds of formula (I), as well as pharmaceutical acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases tha
