We present a comprehensive analysis of all ring systems (both heterocyclic and
nonheterocyclic) in clinical trial compounds and FDA-approved drugs. We show 67% of …

We have analyzed the rings, ring systems, and frameworks in drugs listed in the FDA
Orange Book to understand the frequency, timelines, molecular property space, and the …

Covering: up to 2021 The structural core of most small-molecule drugs is formed by a ring
system, often derived from natural products. However, despite the importance of natural …

Contemporary medicinal chemistry faces diverse challenges from several directions,
including the need for both potency and specificity of any therapeutic agent; the increasingly …

Small aromatic ring systems are of central importance in the development of novel synthetic
protein ligands. Here we generate a complete list of 24847 such ring systems. We call this …

Bioactive molecules only contain a relatively limited number of unique ring types. To identify
those ring properties and structural characteristics that are necessary for biological activity, a …

Medium-sized rings have much promise in medicinal chemistry, but are difficult to make
using direct cyclisation methods. In this minireview, we highlight the value of ring expansion …

Using small, flat aromatic rings as components of fragments or molecules is a common
practice in fragment‐based drug discovery and lead optimization. With an increasing focus …

We have analyzed FDA-approved macrocyclic drugs, clinical candidates, and the recent
literature to understand how macrocycles are used in drug discovery. Current drugs are …

Enables researchers to fully realize the potential to discover new pharmaceuticals among
heterocyclic compounds Integrating heterocyclic chemistry and drug discovery, this …