175353-91-0Relevant academic research and scientific papers
Solution-phase combinatorial synthesis via the olefin metathesis reaction
Boger, Dale L.,Chai, Wenying,Ozer, Rachel S.,Andersson, Carl-Magnus
, p. 463 - 468 (1997)
The preparation of C2-symmetric and unsymmetric chemical libraries by solution-phase techniques including the use of the olefin metathesis reaction to join and combinatorially randomize the length of a linking tether is detailed.
Rigid Scaffolds: Synthesis of 2,6-Bridged Piperazines with Functional Groups in all three Bridges
Gao, Donglin,Penno, Christian,Wünsch, Bernhard
, p. 874 - 889 (2020/09/02)
The activity of pharmacologically active compounds can be increased by presenting a drug in a defined conformation, which fits exactly into the binding pocket of its target. Herein, the piperazine scaffold was conformationally restricted by substituted C
Synthesis and evaluation of (4-chlorobenzhydryl) piperazine amides as sodium channel Nav1.7 inhibitors
Back, Seung Keun,Kam, Yoo Lim,Oh, Jung Ae,Na, Heung Sik,Ih, Uhtaek,Park Choo, Hea-Young
, p. 2290 - 2297 (2015/09/22)
Blockage of voltage-gated sodium channels is used to treat neuropathic pain which is chronic and can become debilitating. Sodium channels Nav1.7-1.9 are especially attractive targets for drug discovery because of the broad therapeutic potential of their m
Solution-phase combinatorial synthesis of nonpeptide bradykinin antagonists
Kam, Yoo Lim,Rhee, Soo-Jin,Choo, Hea-Young P.
, p. 3543 - 3552 (2007/10/03)
We describe the solution-phase combinatorial synthesis and pharmacological effect of fifty N,N′-substituted-N″-1-(4- chlorobenzhydryl)piperazine iminodiacetic acid triamide derivatives as nonpeptide B2 antagonists. The synthesized compounds wer
Solution-phase combinatorial synthesis: Convergent multiplication of diversity via the olefin metathesis reaction
Boger, Dale L.,Chai, Wenying
, p. 3955 - 3970 (2007/10/03)
The solution-phase synthesis of iminodiacetic acid diamides functionalized with ω-alkenes and their dimerization via the olefin metathesis reaction in the preparation of mixture libraries are detailed. Libraries containing as many as 113,232 compounds prepared from only N-BOC- iminodiacetic acid anhydride (1), 15 amines, and 4 ω-alkene carboxylic acids illustrate the diversity that may be achieved by a convergent versus divergent combination of a small number of monomer building blocks that provides the multiplication of diversity typically associated with linear library syntheses including peptides, oligonucleotides and sequential template functionalizations. Unlike the divergent synthesis of such libraries which is amenable to solid-phase synthesis techniques, the convergent synthesis is especially well suited for solution-phase synthesis and is precluded by solid-phase techniques since the combining components typically would be on mutually exclusive phases.
Novel solution phase strategy for the synthesis of chemical libraries containing small organic molecules
Cheng,Cheng, Soan,Comer,Comer, Daniel D.,Williams,Williams, John P.,Myers,Myers, Peter L.,Boger,Boger, Dale L.
, p. 2567 - 2573 (2007/10/03)
A simple, versatile, and general approach to the solution phase, parallel synthesis of chemical libraries conducted on a generalized or universal template, which allows the preparation of multi-milligram quantities of each individual member, is described.
