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PARTICIPATION OF SCAFFOLD HOPPING APROACHES IN DRUG DISCOVERY. Ankur Gera and Sandeep Arora

PARTICIPATION OF SCAFFOLD HOPPING APROACHES IN DRUG DISCOVERY.

Ankur Gera and Sandeep Arora

International Journal of Natural Product Science 2012: Spl Issue 1:131.

Abstract(RBIP-131)

Scaffold hopping or lead hopping is a strategy for discovering structurally novel compounds. The two key components of scaffold hopping: different core structures and similar biological activities of the new compounds relative to the parent compounds. The ultimate aim is to get novel chemotype by modifying the central core structure of the molecule or the side chain that result in compounds with less undesirable features. Scaffold hopping can be done by different means such as heterocycle replacement, ring opening or closure, peptidomimetics, topology based hopping. Scaffold hopping can be done on small, medium and large scale. Small step hops are represented by swapping carbon and nitrogen atoms in an aromatic ring or replacing carbon with other hetero-atoms in a ring, results in a low degree of structural novelty. The transformation from morphine to tramadol by ring opening is one of the earliest examples of scaffold hopping. By breaking six ring bonds and opening up three fused rings, new drug tramadol is more flexible, result in reduced potency and side effects. Ring closure design include converting an alkyl chain to cyclohexane, piperizine or piperidine , convert-ing an o-hydroxylbenzoyl group to quinazoline , and converting an arylamine or arylamide to a fused ring system. Peptidomimetics are compounds whose important element mimics a natural peptide or protein in 3D space while retaining the ability to interact with the biological target and produce the same biological effect. Topology-based hops always lead to a high degree of novelty.
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