Silicon-containing compounds have been largely ignored in drug design until recently. Silicon can be considered a bioisostere of carbon and hence offers an innovative avenue in drug discovery. For example, C/Si exchange in drug-like scaffolds provides an exciting approach in medicinal chemistry to improve ADME/Tox profile and to enhance potency of the biologically active compounds. Herein we have designed and synthesized a library of silicon-containing building blocks for drug design.
Case studies
Advantages of “Silicon Switch”:
- Bond length C–C = 1.54 Å, C–Si = 1.87 Å → changes in the interactions with specific proteins;
- Increase in lipophilicity;
- Si prefers higher coordination numbers → access to compounds for which corresponding carbon analogs are not available.
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More than 30 of silicon-containing building blocks from stock on a 5-10 g scale.
Epoxides are important heterocyclic units found in various naturally occurring molecules, some with potential bioactivities. At least fourteen drugs on the market are epoxide-containing. In addition, epoxides are valuable building blocks in medicinal chemistry. They react with nucleophiles in a ring-opening process to form new C-C, C-O and C-N bonds. Herein we have designed and synthesized a library of small heteroaliphatic epoxides for drug design.
Design
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>100 unique epoxides on a 5-50 g scale from stock.
More than 100 FDA-approved drugs contain pyridine ring and another 100 have been in clinical trials. Examples containing CF3-pyridine moiety include the antiviral drug Tipranavir and drug candidates Taranabant, Velneperit, SB-705498. Besides, CF3-pyridine containing compounds have been playing a fundamental role in agrochemistry. The introduction of fluorine-containing group alters important pharmacokinetic properties of molecular scaffolds. Herein we have designed and synthesized a library of CF3-substituted pyridine analogues for drug design and agrochemistry.
Design
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>100 unique CF3-pyridine analogues on a 5-50 g scale from stock
More than 100 FDA-approved drugs contain the piperazine moiety. Piperazine-based analogues may advantageously alter important pharmacokinetic properties when grafted onto molecular scaffolds. In 2018, chemists showed that replacing a piperazine ring in the drug Olaparib with the spirodiamine analogue beneficially affected activity and reduced cytotoxicity of the parent compound. Herein we have designed and synthesized a library of piperazine analogues for drug design.
Design
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>100 unique piperazine analogues on a 5-50 g scale from stock.
Saturated azaheterocycles are popular in modern drug discovery programs. More than 50 FDA-approved drugs containing a fragment of pyrrolidine and piperidine have appeared on the market. Pyrrolidine/piperidine-based azasugars and their analogues are potent glycosidase inhibitors. These unique molecules promise a new generation of iminosugar-based medicines for a wide range of diseases. For example, a bioactive azasugar includes the anti-diabetic drug Glyset. In this context, herein we have designed and synthesized a library of sugar-like derivatives for drug design.
Design
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>50 unique sugar-like derivatives on a 5-50 g scale in stock.
