645393-01-7Relevant academic research and scientific papers
Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides
Russell, Stephanie,Rahmani, Rapha?l,Jones, Amy J.,Newson, Harriet L.,Neilde, Kevin,Cotillo, Ignacio,Rahmani Khajouei, Marzieh,Ferrins, Lori,Qureishi, Sana,Nguyen, Nghi,Martinez-Martinez, Maria S.,Weaver, Donald F.,Kaiser, Marcel,Riley, Jennifer,Thomas, John,De Rycker, Manu,Read, Kevin D.,Flematti, Gavin R.,Ryan, Eileen,Tanghe, Scott,Rodriguez, Ana,Charman, Susan A.,Kessler, Albane,Avery, Vicky M.,Baell, Jonathan B.,Piggott, Matthew J.
, p. 9686 - 9720 (2016/11/19)
The parasitic trypanosomes Trypanosoma brucei and T. cruzi are responsible for significant human suffering in the form of human African trypanosomiasis (HAT) and Chagas disease. Drugs currently available to treat these neglected diseases leave much to be
HETEROCYCLIC COMPOUNDS AND USE OF SAME
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Paragraph 00143; 00148, (2016/01/08)
Novel heterocyclic compounds are provided which display useful efficacy in the treatment of diseases caused by trypanosomatids. Particularly, the compounds of the invention are useful in the treatment of HAT and/or Chagas disease and/or Animal African trypanosomiasis (AAT).
Histamine H1 receptor ligands. Part I. Novel thiazol-4-ylethanamine derivatives: Synthesis and in vitro pharmacology
Walczynski,Timmerman,Zuiderveld,Zhang,Glinka
, p. 533 - 541 (2007/10/03)
A series of 2-substituted thiazol-4-ylethanamines have been synthesized and tested for their histaminergic H1-receptor activities. The compounds with 2-phenyl substitution, regardless of the different physicochemical properties of the meta-substituents at the phenyl ring, showed weak H1-agonistic activity with pD2 values ranging from 4.35 to 5.36. When the phenyl group was replaced by a benzyl group, the resulting compounds all exhibited weak H1-antagonistic activity (pA2: 4.14-4.82). Copyright (C) 1999 Elsevier Science S.A.
