1303786-06-2Relevant academic research and scientific papers
Design, synthesis and SARs of novel salicylanilides as potent inhibitors of RANKL-induced osteoclastogenesis and bone resorption
Chen, Chun-Liang,Lee, Chia-Chung,Liu, Fei-Lan,Chen, Tsung-Chih,Ahmed Ali, Ahmed Atef,Chang, Deh-Ming,Huang, Hsu-Shan
, p. 70 - 84 (2016/04/26)
Inhibiting osteoclastogenesis is a promising therapeutic target for treating osteoclast-related diseases. Herein, we synthesized a series of modified salicylanilides and their corresponding 3-phenyl-2H-benzo[e][1,3]oxazine-2,4(3H)-dione and 10-phenyldiben
Method of use of pharmaceutical formulations for the treatment of apicomplexan diseases in animals
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Paragraph 0090; 0091, (2014/01/07)
The present invention is directed to the method of use of effective pharmaceutical formulations for the treatment of diseases caused by apicomplexan parasites, said formulation comprised of a salicylanilide or salicylanilide derivative, disclosed herein,
Salicylanilide inhibitors of Toxoplasma gondii
Fomovska, Alina,Mui, Ernest,McLeod, Rima,Wood, Richard D.,Welsh, William J.,Dubey, Jitenter P.,Ferreira, Leandra R.,Hickman, Mark R.,Lee, Patricia J.,Leed, Susan E.,Auschwitz, Jennifer M.,Sommerville, Caroline,Woods, Stuart,Roberts, Craig
, p. 8375 - 8391,17 (2020/09/15)
Toxoplasma gondii (T. gondii) is an apicomplexan parasite that can cause eye disease, brain disease, and death, especially in congenitally infected and immune-compromised people. Novel medicines effective against both active and latent forms of the parasite are greatly needed. The current study focused on the discovery of such medicines by exploring a family of potential inhibitors whose antiapicomplexan activity has not been previously reported. Initial screening efforts revealed that niclosamide, a drug approved for anthelmintic use, possessed promising activity in vitro against T. gondii. This observation inspired the evaluation of the activity of a series of salicylanilides and derivatives. Several inhibitors with activities in the nanomolar range with no appreciable in vitro toxicity to human cells were identified. An initial structure-activity relationship was explored. Four compounds were selected for evaluation in an in vivo model of infection, and two derivatives with potentially enhanced pharmacological parameters demonstrated the best activity profiles.
