Applications of Hydrolases in Medicinal Chemistry

Dear Colleagues,

The implementation of practical, efficient, atom economical, cost-efficient, scalable and environmentally friendly synthetic methods that enable the rapid preparation of pharmacologically relevant compounds in high chemical and optical purity as well as yields close to quantitative values is of critical interest not only to academic researchers, but particularly to chemists who are responsible for designing industrial or manufacturing syntheses.

In this context, biocatalytic processes based on hydrolases are the method of choice since these relatively inexpensive biocatalysts exhibit mostly excellent regio-, chemo- and enantio-selectivity as well as remarkable catalytic activity even in low-water environments including nearly anhydrous organic solvents, without needing the addition of costly external acceptors and cofactors (NAD(P)H, FADH₂, etc.). Since the 1980s hydrolases have become well-anchored catalysts in plethora of synthetic endeavors and industrial applications, being some of the most common biocatalysts currently in use in organic chemistry. The prestigious status of hydrolases mainly stems from their ability to play an irreplaceable role in chirality inducement, high operational stability under non-physiological conditions, and wide commercial availability in both native and immobilized forms. Hydrolase-based biotransformations have shown to be superior compared to traditional chemical synthesis approaches, especially in C–O functional group chemistry of chiral secondary alcohols and their respective esters. Moreover, thanks to the advantageous structural flexibility of hydrolases, enzymes of this type are also prone to catalyze both the transformation of a wide spectrum of unnatural substrates of highly functionalized structures as well as reactions which are far from their “physiological repertoire”. The so-called “enzyme promiscuity” of hydrolases (in particular lipases) experimentally proven in various types of condensations (cross-aldol, aza-Michael, Morita–Baylis–Hillman, Knoevenagel, Henry-nitroaldol, Phillips etc.), multicomponent reactions (Biginelli, Hantzsch, Mannich, Ugi, Kabachnik–Fields etc.), and many other processes including oxidations (epoxidation of alkenes, Baeyer–Villiger etc.), domino thia-Michael–Henry or Suzuki–Miyaura reactions showed that these enzymes are also valuable biocatalysts in C–C and/or C–heteroatom bond formations. All the abovementioned unique features of hydrolases make it so that these biocatalysts are willingly applied in the synthesis of high-added-value compounds with controlled stereochemical properties, such as pharmaceuticals, agrochemicals, vitamins, flavors and fragrances or bulk products, including nutraceuticals, detergents, cosmetics, biofuels and biodegradable polymers.

We highly encourage potential authors to submit their manuscripts reporting on chemoenzymatic methods for the synthesis of novel compounds of defined biological activities, pharmacologically important chiral building blocks and/or generic active pharmaceutical ingredients (APIs) of known drugs.

Dr. Paweł Borowiecki
Dr. Dominik Koszelewski
Guest Editors

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