56681-66-4Relevant articles and documents
Ambroxol derivative, and preparation method, medicinal composition and application thereof
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Paragraph 0075; 0077-0080, (2019/12/29)
The invention relates to the field of medicinal chemistry, and concretely relates to an ambroxol derivative or pharmaceutically acceptable salts thereof, and a preparation method, a medicinal composition and a medical application thereof. The ambroxol derivative is a compound with a structure represented by formula I shown in the specification, and R in the formula I is defined in claims.
Synthesis of Two Natural Furan-Cyclized Diarylheptanoids via 2-Furaldehyde
Se?inti, Hatice,Se?en, Hasan
, p. 938 - 944 (2015/11/23)
Two natural diarylheptanoids, 2-benzyl-5-(2-phenylethyl)furan (1) and 2-methoxy-4-{[5-(2-phenylethyl)furan-2-yl]methyl}phenol (2), were synthesized starting from 2-furaldehyde. A Wittig reaction of 2-furaldehyde with benzyltriphenylphosphonium bromide followed by reduction of the alkene C=C bond with Mg gave 2-(2-phenylethyl)furan (5). Lithiation of 5 with BuLi at -78 followed by alkylation with benzyl bromide gave natural product 1. In another approach, Friedel-Crafts acylation of compound 5 with benzoyl chloride followed by deoxygenation of the C=O group afforded 1. The natural product 2 was also synthesized by acylation of 5 with 4-acetoxy-3-methoxybenzoyl chloride (16) followed by deoxygenation and deacetylation.
Pharmacological validation of trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness
Bland, Nicholas D.,Wang, Cuihua,Tallman, Craig,Gustafson, Alden E.,Wang, Zhouxi,Ashton, Trent D.,Ochiana, Stefan O.,McAllister, Gregory,Cotter, Kristina,Fang, Anna P.,Gechijian, Lara,Garceau, Norman,Gangurde, Rajiv,Ortenberg, Ron,Ondrechen, Mary Jo,Campbell, Robert K.,Pollastri, Michael P.
experimental part, p. 8188 - 8194 (2012/01/13)
Neglected tropical disease drug discovery requires application of pragmatic and efficient methods for development of new therapeutic agents. In this report, we describe our target repurposing efforts for the essential phosphodiesterase (PDE) enzymes TbrPDEB1 and TbrPDEB2 of Trypanosoma brucei, the causative agent for human African trypanosomiasis (HAT). We describe protein expression and purification, assay development, and benchmark screening of a collection of 20 established human PDE inhibitors. We disclose that the human PDE4 inhibitor piclamilast, and some of its analogues, show modest inhibition of TbrPDEB1 and B2 and quickly kill the bloodstream form of the subspecies T. brucei brucei. We also report the development of a homology model of TbrPDEB1 that is useful for understanding the compound-enzyme interactions and for comparing the parasitic and human enzymes. Our profiling and early medicinal chemistry results strongly suggest that human PDE4 chemotypes represent a better starting point for optimization of TbrPDEB inhibitors than those that target any other human PDEs.
