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Prestwick Chemical Privileged Building Blocks^®

Prestwick Chemical Inc. facilitates and accelerates chemical research in providing original pyridazine building blocks as privileged pharmacophores.

About 70% of all the drug molecules used in therapy are heterocycles. As well for synthetic as for natural compounds, Medicinal Chemistry mainly deals with nitrogen-derived heterocycles. An evident reason for that is that the great majority of the targeted endogenous ligands are themselves heterocyclic nitrogenous metabolites of amino acids. Moreover, heterocycles allow the insertion of elements capable to give interactions where the carbocycles do not give and they allow a greater number of combinations (it becomes therefore easier to be original). Within the nitrogenous heterocycles, the diazines are of particular interest as they represent an isosteric relationship to the phenyl ring.

Why pyridazines ?

Pyridazines represent privileged structures for medicinal chemistry:

• Pyridazines can be used for isosteric replacements: they are surrogates of phenyl or heteroaromatic rings (which are present in more than fifty percent of all drugs).
• Pyridazines improve the physico-chemical properties of the drug molecules by:
  • increasing their water solubility (replacement of a carbocycle by a pyridazine will decrease Log D through direct solvatation or salt formation without increasing the molecular weight),
  • creating additional interactions and/or binding possibilities thanks to their hydrogen bond acceptor properties (and therefore favours better interactions with the target proteins). Their dipole moment gives them a high complexing capacity.
• Pyridazines are known ingredients of drug molecules.
  Generally the presence of a pyridazine in a bioactive molecule confers good bioavailabilty, especially into the CNS, and notably reduces the toxicity. In addition, the pyridazine pharmacophore is known to lead to a great variety of pharmacologically active compounds. Thus, pyridazines can be considered as privileged structures.

Prestwick pyridazine building blocks

Prestwick offers various pyridazine building blocks which are not commonly available in catalogues. Some of them are functionalized 6-aryl-pyridazines and thus are bioisosteric to the biphenyl motif. Others are bifunctional pyridazine scaffolds with high pharmacophoric potential.
All pyridazines listed in our pyridazine catalogue exceed 90% chemical purity (they are commonly available in a range of 100 mg to 5g).
Moreover Pr C. G. Wermuth, founder of the Company, President and CSO has more than 30 years experience in the chemistry of pyridazines and the Prestwick team would be pleased to meet your needs and to consider any specific request (confidentiality guaranteed).