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10.1021/ml5005156

http://scihub22266oqcxt.onion/10.1021/ml5005156
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suck abstract from ncbi


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pmid25893048      ACS+Med+Chem+Lett 2015 ; 6 (4): 450-4
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  • Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development #MMPMID25893048
  • Letavic MA; Aluisio L; Apodaca R; Bajpai M; Barbier AJ; Bonneville A; Bonaventure P; Carruthers NI; Dugovic C; Fraser IC; Kramer ML; Lord B; Lovenberg TW; Li LY; Ly KS; Mcallister H; Mani NS; Morton KL; Ndifor A; Nepomuceno SD; Pandit CR; Sands SB; Shah CR; Shelton JE; Snook SS; Swanson DM; Xiao W
  • ACS Med Chem Lett 2015[Apr]; 6 (4): 450-4 PMID25893048show ga
  • The preclinical characterization of novel phenyl(piperazin-1-yl)methanones that are histamine H3 receptor antagonists is described. The compounds described are high affinity histamine H3 antagonists. Optimization of the physical properties of these histamine H3 antagonists led to the discovery of several promising lead compounds, and extensive preclinical profiling aided in the identification of compounds with optimal duration of action for wake promoting activity. This led to the discovery of two development candidates for Phase I and Phase II clinical trials.
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