Optimizing the “Drug-Like” Properties of Leads in Drug Discovery

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In the diversity-oriented synthesis structural diversity and complexity are sought, but the molecules obtained in this way are often large in size and lie in drug like space, so there is little room for optimization. These compounds might be useful as drugs themselves, but not as leads or hits.

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Fragment-based screening fig 2 involves screening small molecules that are not intrinsically drug-like, but that might become subunits fragments of drug-like compounds. Through different approaches, the above mentioned methodologies can efficiently produce drug-like molecules, but they are limited to yield smaller molecules with the desired molecular properties 1 P Despite its recent introduction, an increasing number of groups 5 are focusing on developing new synthetic methods that comply with the concept of obtaining molecules with specific molecular properties.

Roughly, small polar molecules as opposed to currently predominant and easier to make big and apolar lipophilic entities.


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However, obtaining molecules with desired molecular properties at the lead stage is necessary but not sufficient: The optimization process is equally critical to enhance the activity and reduce the undesired effects, while the molecular properties are kept in the drug-like range. The best outcomes are likely to come from both the appropriate optimization and a good starting point, where the concept of lead-oriented synthesis may be of help.

Leave a comment. Figure 1. The central red oval represents the optimal oral drug-like space, and the arrow shows the progression towards more complexity and lipophilicity in the optimization progress. Thus, starting point should be in lead-like or fragment-like space.

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Lead-oriented synthesis: a new concept to aid drug-discovery process

Credit: Nadin et al. Figure 2. Fragment-based screening: Small and structurally diverse molecules circles represent functional groups are screened for a biological target, and they are combined and modified to generate drug-like compounds. Diversity-oriented synthesis: Large collections of structurally diverse and complex molecules are made using a short number of reactions.

The resulting compounds are optimized to produce the drug-like compounds. Credit: P.

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Spring Nature , , , 42— DOI: References C. Lipinski, F. Lombardo, B. Dominy, P. Feeney Adv. Drug Deliv. Hann, G. Nadin, C.


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  • Hattotuwagama, I. British Journal of Pharmacology. Landes Bioscience. Retrieved 20 November Categories : Drug discovery Medicinal chemistry. Hidden categories: Articles with short description. Namespaces Article Talk. Views Read Edit View history.

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