The macrophage migration inhibitory factor has been implicated in a number ofimmune and inflammatory processes. MIF presents particular opportunities for drug design anddevelopment with potential therapeutic applicati...The macrophage migration inhibitory factor has been implicated in a number ofimmune and inflammatory processes. MIF presents particular opportunities for drug design anddevelopment with potential therapeutic applications. Drug design strategies taking intoconsideration of specific stereochemical and tautomeric requirements in the interaction of MIF withsubstrates and inhibitors allow several novel structures to be designed. Our investigationssuccessfully explored the tautomeric and stereochemical aspects of new compounds of the2-phenylpyruvic acid type, both experimentally, through synthesis and structural investigations andcomputationally, through molecular mechanics and quantum mechanics calculations.展开更多
The aldol reaction of the silyl enol ether of cyclopent-2-enone with aldehydes is mediated by various Lewis acids.Threo isomers are the major diastereoisomers formed in most cases.A reverse diastereoselectivity was ob...The aldol reaction of the silyl enol ether of cyclopent-2-enone with aldehydes is mediated by various Lewis acids.Threo isomers are the major diastereoisomers formed in most cases.A reverse diastereoselectivity was observed when the reaction was mediated by TBAF.The results have been discussed in detail by structure and transition state analysis.展开更多
文摘The macrophage migration inhibitory factor has been implicated in a number ofimmune and inflammatory processes. MIF presents particular opportunities for drug design anddevelopment with potential therapeutic applications. Drug design strategies taking intoconsideration of specific stereochemical and tautomeric requirements in the interaction of MIF withsubstrates and inhibitors allow several novel structures to be designed. Our investigationssuccessfully explored the tautomeric and stereochemical aspects of new compounds of the2-phenylpyruvic acid type, both experimentally, through synthesis and structural investigations andcomputationally, through molecular mechanics and quantum mechanics calculations.
文摘The aldol reaction of the silyl enol ether of cyclopent-2-enone with aldehydes is mediated by various Lewis acids.Threo isomers are the major diastereoisomers formed in most cases.A reverse diastereoselectivity was observed when the reaction was mediated by TBAF.The results have been discussed in detail by structure and transition state analysis.
