Diazole-based Peptide Bond Surrogates

The high sensitivity of peptide therapeutics to endopeptidases can be addressed by replacing peptide bonds with isosteric surrogates. Azoles, naturally occurring compounds commonly found in the backbone of bioactive peptides, offer one such alternative. In the 2010s, several direct-acting antivirals containing diazole surrogates for peptide bonds were approved for the treatment of HCV, including ledipasvir (2014), daclatasvir (2015), elbasvir (2016), and velpatasvir (2016). As leaders in chemical science, our specialists have curated a range of diazole- and benzodiazole-based structures to replace peptide bonds in peptidomimetics, aiming to optimize activity and pharmacokinetic properties.

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Over 100 diazole-based dipeptide surrogates from stock on 5-10 gram scale.

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