868692-49-3Relevant academic research and scientific papers
Chagas Disease Drug Discovery: Multiparametric Lead Optimization against Trypanosoma cruzi in Acylaminobenzothiazole Series
Fleau, Charlotte,Padilla, Angel,Miguel-Siles, Juan,Quesada-Campos, Maria T.,Saiz-Nicolas, Isabel,Cotillo, Ignacio,Cantizani Perez, Juan,Tarleton, Rick L.,Marco, Maria,Courtemanche, Gilles
, p. 10362 - 10375 (2019/11/29)
Acylaminobenzothiazole hits were identified as potential inhibitors of Trypanosoma cruzi replication, a parasite responsible for Chagas disease. We selected compound 1 for lead optimization, aiming to improve in parallel its anti-T. cruzi activity (IC50 = 0.63 μM) and its human metabolic stability (human clearance = 9.57 mL/min/g). A total of 39 analogues of 1 were synthesized and tested in vitro. We established a multiparametric structure-activity relationship, allowing optimization of antiparasite activity, physicochemical parameters, and ADME properties. We identified compound 50 as an advanced lead with an improved anti-T. cruzi activity in vitro (IC50 = 0.079 μM) and an enhanced metabolic stability (human clearance = 0.41 mL/min/g) and opportunity for the oral route of administration. After tolerability assessment, 50 demonstrated a promising in vivo efficacy.
Novel indole derivatives as selective androgen receptor modulators (SARMS)
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Page/Page column 42, (2008/06/13)
The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
Novel indole derivatives as selective androgen receptor modulators (SARMS)
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Page/Page column 43, (2010/02/14)
The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
NOVEL INDOLE DERIVATIVES AS SELECTIVE ANDROGEN RECEPTOR MODULATOR (SARMS)
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Page/Page column 42, (2008/06/13)
The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
