Peptide-mimetic drugs

Other than RIF and Taxol, many other commonly used clinical drugs have also been shown to activate PXR. These include peptide-mimetic HIV protease inhibitors [53], the cholesterol-lowering lovastatin and the anti-inflammatory dexamethasone [54]. A more comprehensive analysis of the effect of commonly used clinical drugs on PXR activation has recently been published by Sinz and colleagues [55]. 

Green Processes for Peptide Mimetic Diabetic Drugs... 

Figure 9.3 Peptide mimetic diabetic drug candidates.

I 9 Green Processes for Peptide Mimetic Diabetic Drugs COjH (COCI)2, cat. DMF... 

B. Weidmann, Renin inhibitors, from transition state analogs and peptide mimetics to blood pressure lowering drugs, Chimia 1991, 45, 367-376. 

The power of the Passerini and Ugi reactions in constructing polyfunctional molecules has been well appreciated since the early studies. The classical Passerini and Ugi reactions afford a-acyloxy carboxamides and a-acylamino amides respectively, that can be easily manipulated by post-condensation reactions, generating molecular diversity for drug discovery and natural product synthesis [22], This strategy has been widely applied to the synthesis of natural peptides and open-chain peptide mimetics covered in this section. 

Peptide mimetics have been defined as moiecuies that mimic the action of peptides, have no peptide bonds (i.e., no amide bonds between amino acids), and a moiecuiar weight of less than 700 Daltons. In comparison with peptide drugs, peptide mimetics have numerous pharmaceutical advantages. Foremost among these are increased bloavallablllty and Increased duration of action. The majority of known peptide mimetics have been discovered by random screening techniques however, this process is costly, labor intensive, and unpredictable. 

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