Combinatorial Chemistry in the Drug Discovery Process

Combinatorial Chemistry: Libraries from Libraries, the Art of the Diversity-Oriented Transformation of Resin-Bound Peptides and Chiral Polyamides to Low Molecular Weight Acyclic and Heterocyclic Compounds

“…These libraries have been successfully used for the de novo identification of potent analgesics, − antimicrobial agents, , enzyme inhibitors, and highly specific antigenic determinants of B-cells and T-cells . Along with linear peptide sequences, our laboratory and other groups have also synthesized combinatorial libraries of cyclic peptides. − In the past decade, the focus of combinatorial chemistry has shifted to libraries of small molecule compounds having molecular weights of 500 Da or less. − Employing a “toolbox” of various chemical transformations, including alkylation, oxidation, reduction, acylation, and the use of a variety of multifunctional reagents, we present examples of the use of the “libraries from libraries” 46-48 concept for the development and generation of an ever-expanding, structurally varied series of organic chemical libraries.…”

Designing and Developing Therapeutic Interventions in the Bioinformatics Era

“…From the fore-going, it is evident that laboratory-based clinical investigations remain pivotal in the successful hunting of any therapeutic intervention. However, these investigations are found to be resource-consuming, expensive and time-wasting [3]. Since serendipity has eluded discovery and designing of therapies, clinical approaches are irrational, and computing knowledge as well as application of artificial intelligence have escalated [1], computer-assisted approaches and robotic devices have therefore crept into the processes of discovery, design and development of therapeutic interventions.…”