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Fragment-based Lead Preparation in Drug Discovery and Development

FBDD is a powerful approach in drug design. To identify the fragment hits, various screening methods are employed. Transformation of the promising fragments into larger ligands with higher affinity and activity against the target (hit-to-lead optimization) can be realized via several strategies.

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09 december 2021, 14:29    Svitlana Kondovych Computational Chemistry

Functionalized (-)-Cytisine Derivatives for Medicinal Chemistry and Organic Synthesis

Naturally occurring alkaloid ()-cytisine is an efficient acetylcholine agonist possessing a strong affinity to nicotinic acetylcholine receptors (nAChRs). Its various chemical modifications were applied to obtain novel bicyclic compounds for rational drug discovery. Life Chemicals offers derivatives of ()-cytisine including those involving chromone, coumarin, and other heterocyclic substructures.

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10 november 2021, 13:26    Oleg Lukin Building Blocks

Functionalized Pyridines as Valuable Building Blocks in Organic Synthesis and Medicinal Chemistry

The structural unit of substituted pyridine occurs in numerous important compounds including natural products such as vitamins, coenzymes, and alkaloids as well as synthetic pharmaceuticals and agrochemicals.

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12 october 2021, 16:29    Oleg Lukin Building Blocks

Peptidomimetics in Modern Drug Discovery

Peptidomimetics are synthetic molecules created to mimic natural peptides in three-dimensional form so that they retain the same biological activity while reducing the risks of their natural counterparts, including stability, proteolysis resistance, and bioavailability.

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15 september 2021, 16:41    Andrew Golub Computational Chemistry

Conformationally Restricted Diamines in Medicinal Chemistry and Drug Discovery

Conformationally restricted diamines (CRDAs) are especially attractive scaffolds for drug discovery because they offer the potential of the wide variability in the relative spatial arrangement of functional groups.

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26 august 2021, 14:22    Oleg Lukin Building Blocks
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