COA of Formula: C7H5ClN2SOn November 27, 2019 ,《Chagas Disease Drug Discovery: Multiparametric Lead Optimization against Trypanosoma cruzi in Acylaminobenzothiazole Series》 appeared in Journal of Medicinal Chemistry. The author of the article were 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. The article conveys some information:
Acylaminobenzothiazole hits were identified as potential inhibitors of T. cruzi replication, a parasite responsible for Chagas Disease. We selected compound 1, N-(6-chlorobenzo[d]thiazol-2-yl)cyclopropanecarboxamide, for lead optimization, aiming to improve in parallel its anti-T. cruzi activity (IC50 = 0.630μM) and its human metabolic stability (human clearance = 9.57mL/min/g). A total of 39 analogs of 1 were synthesized and tested in vitro. We established a multiparametric structure activity relationship, allowing optimization of both anti-parasite activity, physicochem. parameters and ADME properties. We identified compound 50, N-(5-Fluoro-6-(trifluoromethyl)benzothiazol-2-yl)cyclopropanecarboxamide, as an advanced lead with an improved anti-T. cruzi activity in vitro (IC50 = 0.079μM), an enhanced metabolic stability (Human Clearance = 0.413mL/min/g) and opportunity for oral route of administration. After tolerability assessment, compound 50 demonstrated a promising in vivo efficacy. In the experiment, the researchers used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9COA of Formula: C7H5ClN2S)
6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.COA of Formula: C7H5ClN2SThiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica