Recently I am researching about DIHYDROFOLATE-REDUCTASE; THYMIDYLATE SYNTHASE; BINDING MODES; LEISHMANIA; IDENTIFICATION; ASSAY; DERIVATIVES; VALIDATION; SOLUBILITY; RESISTANCE, Saw an article supported by the European Union’s Seventh Framework Programme for Research, Technological Development, and Demonstration [603240]; Klaus Tschira Foundation. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Linciano, P; Pozzi, C; dello Iacono, L; di Pisa, F; Landi, G; Bonucci, A; Gul, S; Kuzikov, M; Ellinger, B; Witt, G; Santarem, N; Baptista, C; Franco, C; Moraes, CB; Muller, W; Wittig, U; Luciani, R; Sesenna, A; Quotadamo, A; Ferrari, S; Pohner, I; Cordeiro-Da-Silva, A; Mangani, S; Costantino, L; Costi, MP. The CAS is 91-00-9. Through research, I have a further understanding and discovery of Diphenylmethanamine. Category: amides-buliding-blocks
2-Amino-benzo[d]thiazole was identified as a new scaffold for the development of improved pteridine reductase-1 (PTR1) inhibitors and anti-trypanosomatidic agents. Molecular docking and crystallography guided the design and synthesis of 42 new benzothiazoles. The compounds were assessed for Trypanosoma brucei and Leishmania major PTR1 inhibition and in vitro activity against T. brucei and amastigote Leishmania infantum. We identified several 2-amino-benzo[d]thiazoles with improved enzymatic activity (TbPTR1 IC50 = 0.35 mu M; LmPTR1 IC50 = 1.9 mu M) and low mu M antiparasitic activity against T. brucei. The ten most active compounds against TbPTR1 were able to potentiate the antiparasitic activity of methotrexate when evaluated in combination against T. brucei, with a potentiating index between 1.2 and 2.7. The compound library was profiled for early ADME toxicity, and 2-amino-N-benzylbenzo[d]thiazole-6-carboxamide (4c) was finally identified as a novel potent, safe, and selective anti-trypanocydal agent (EC50 = 7.0 mu M). Formulation of 4c with hydroxypropyl-beta-cyclodextrin yielded good oral bioavailability, encouraging progression to in vivo studies.
Category: amides-buliding-blocks. About Diphenylmethanamine, If you have any questions, you can contact Linciano, P; Pozzi, C; dello Iacono, L; di Pisa, F; Landi, G; Bonucci, A; Gul, S; Kuzikov, M; Ellinger, B; Witt, G; Santarem, N; Baptista, C; Franco, C; Moraes, CB; Muller, W; Wittig, U; Luciani, R; Sesenna, A; Quotadamo, A; Ferrari, S; Pohner, I; Cordeiro-Da-Silva, A; Mangani, S; Costantino, L; Costi, MP or concate me.
Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics