Mechanism of action studies

Stmcture-activity and mechanism of action studies indicate that the requirements for chloramphenicol activity are the D-threo-configuration, the... 

Medicinal chemists have a distinct advantage in pursuing mechanism-of-action studies because it is possible to synthesize a series of structurally related congeners and measure their biological activity. A correlation between activity and particular structural features not only helps to identify the pharmacophore, or active moiety imbedded within the molecule, but also may establish critical requirements or complementarity for the biological target or receptor for the particular drug class. 

Application of GenomicsTtechniques as Tools for Hypothesis Generation and Mechanism of Action Studies... 

Mechanism of action studies including drug receptor interactions and specific enzyme inhibitions. 

Both cell cultures and animal studies have shown that many of the naturally occurring mono-, sesqui-, di-, sester-, and meroterpenoids as well as retinoids possess potentially chemopreventive activities. Terpenoids are minor but ubiquitous components of our diet, and have the advantage of being non-toxic or relatively non-toxic to humans. More mechanistic-oriented basic research is needed to elucidate the mechanisms of action. Studies of derivatives of these naturally occurring terpenoids are also necessary to elucidate the structure-activity relationship and to guide the development of novel chemopreventive agents. 

Xu, D. et al. 2007. Genome-wide fitness test and mechanism-of-action studies of inhibitory compounds in Candida albicans. PLoS Pathog. 3, e92. 

Several naturally occurring triterpenes have been reported to show anti-HIV activity, e.g. betulinic acid, platanic acid, glycyrrhizin, mimusopic acid, gano-deriol and geumonoid.16 20 These active compounds hold the potential to serve as hits or leads for anti-HIV drug development.21,22 The focus of this chapter is bevirimat, the first in a new class of compounds termed HIV maturation inhibitors (Mis). Our discussion covers modification, structure-activity relationship (SAR), mechanism of action studies and clinical trials of bevirimat. 

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