1162684-07-2Relevant academic research and scientific papers
Activity of diphenyl ether benzyl amines against Human African Trypanosomiasis
Anderson, Samuel,Belter, Bret,Cal, Monica,Darner, Grant,Davis, Paul H.,Hagen, James P.,Higgins, Katie,Kaiser, Marcel,Leas, Derek A.,Mashinson, Victoria,Mitra, Ananya,Vera-Esquivel, Carlos,Wallick, Alexander,Warner, Rosalie C.,Wol, Tasloach
, (2020)
Insect-borne parasite Trypanosoma brucei plagues humans and other animals, eliciting the disease Human African trypanosomiasis, also known as African sleeping sickness. This disease poses the biggest threat to the people in Sub-Saharan Africa. Given the high toxicity and difficulties with administration of currently available drugs, a novel treatment is needed. Building on known Human African trypanosomiasis structure–activity relationship (SAR), we now describe a number of functionally simple diphenyl ether analogs which give low micromolar activity (IC50 = 0.16–0.96 μM) against T. b. rhodesiense. The best compound shows favorable selectivity against the L6 cell line (SI = 750) and even greater selectivity (SI = 1200) against four human cell lines. The data herein provides direction for the ongoing optimization of antitrypanosomal diphenyl ethers.
Synthesis and biological evaluation of inhibitors of botulinum neurotoxin metalloprotease
Wang, Chenbo,Widom, Julia,Petronijevic, Filip,Burnett, James C.,Nuss, Jonathan E.,Bavari, Sina,Gussio, Rick,Wipf, Peter
experimental part, p. 487 - 520 (2009/12/24)
Based on the lead therapeutic agent NSC 240898, a new series of heterocyclic inhibitors of the BoNT serotype A metalloprotease has been generated. Highlights of the synthetic sequences include Sonogashira couplings of polysubstituted building blocks and gold-catalyzed indole formations. Preliminary structure-activity relationship studies afford detailed insights into the steric and electrostatic properties of the pharmacophore of this molecular scaffold.
