This article introduces the Topliss tree and Topliss schemes for analog synthesis, illustrates when they might be useful, and provides easy-to-use posters or "cheat sheets" of the original schemes. By Christian Kuttruff Why are the Topliss Tree and Topliss Schemes Useful? Imagine you’re on a new project that has just conducted a chemical [...]
The 2024 edition of MCR (Medicinal Chemistry Reviews), edited by Joachim Rudolph and Will Watkins, has just been published by the American Chemical Society MEDI Division. Featuring contributions from a global team of section editors and authors, MCR offers concise updates on a broad range of contemporary drug discovery topics, making it an invaluable resource for both aspiring and experienced medicinal chemists.
While biologic drugs currently dominate in immunology by sales , small molecule immunomodulators (SMIMs) are making a comeback fueled by better understanding of intracellular signaling pathways and new hit finding technologies. SMIMs can be grouped into two categories: those that engage large molecule (LM) targets in a new [...]
With increasingly tight timelines between bench and clinic, considering formulation strategies early on can give your program a competitive edge. This succinct formulations guide provides specific clinically-used examples of common formulations, and can help you select a formulation strategy most likely to succeed based on the properties of your compound.
In this article, we highlight the importance of p K a values in medicinal chemistry and drug discovery and provide a reference poster of p K a values of common amines’ conjugate bases. Since amines are often a part of marketed drugs, knowledge of their p K a s can provide guidance in the selection of basic moieties to match the desired [...]
