PubMed · 14249929
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O HRDY. 1964. [DEXAMETHASONE].. https://pubmed.ncbi.nlm.nih.gov/14249929/
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The successful practice of medicinal chemistry is crucially dependent on the principles of molecular recognition: the first and "fundamental" requirement for a drug is to bind to its target; specificity, or at least selectivity, of binding is also a must. Subsequent optimization steps to develop a lead compound into a drug are a complex mixture of processes that are not yet fully understood or predictable. Fortunately, criteria exist to discard leads that would be intractable for optimization. The concepts of non-lead-likeness and lead-likeness, in respect to drug-likeness and non-drug-likeness, have prompted a rich discussion in the recent medicinal chemistry literature. The fragment approach is an emerging philosophy in the process of lead compound discovery. The basic interactions responsible for binding affinity are defined from the "protein interactions world" and key structural fragments are combined according to the criteria of three-dimensional diversity to find new leads. New techniques in screening are used for the detection of the weaker interactions of fragments with their targets that might be undetectable in classical biological assays.
The concepts of high-throughput (HT) screening and combinatorial synthesis have been integrated into the pharmaceutical discovery process, but are not yet commonplace in the pharmaceutical development arena. Emerging strategies to speed pharmaceutical development and capture solid form diversity of pharmaceutical substances have resulted in the emergence of HT crystallization technologies. The primary type of diversity often refers to polymorphs, which are different crystal forms of the same chemical composition. However, diverse salt forms, co-crystals, hydrates and solvates are also amenable to study in HT crystallization systems. The impact of form diversity encompasses issues of stability and bioavailability, as well as development considerations such as process definition, formulation design, patent protection and regulatory control. This review highlights the opportunities and challenges of HT crystallization technologies as they apply to pharmaceutical research and development.
Robin Ganellin was born in East London and studied chemistry at Queen Mary College, London, receiving a PhD in 1958 under Professor Michael Dewar for his research on tropylium chemistry. He joined Smith Kline & French Laboratories (SK&F) in the UK in 1958 and was one of the co-inventors of the revolutionary drug cimetidine (Tagamet(R)) He subsequently became Vice-President for Research at the company's Welwyn facility. In 1986 he was awarded a DSc from London University for his work on the medicinal chemistry of drugs acting at histamine receptors and was also made a Fellow of the Royal Society and appointed to the SK&F Chair of Medicinal Chemistry at University College London, where he is now Emeritus Professor of Medicinal Chemistry. Professor Ganellin has been honoured extensively, including such awards as the Royal Society of Chemistry Award for Medicinal Chemistry, their Tilden Medal and Lectureship and their Adrien Albert Medal and Lectureship, Le Prix Charles Mentzer de France, the ACS Division of Medicinal Chemistry Award, the Society of Chemical Industry Messel Medal and the Society for Drug Research Award for Drug Discovery. He is a past Chairman of the Society for Drug Research, was President of the Medicinal Chemistry Section of IUPAC, and is currently Chairman of the IUPAC Subcommittee on Medicinal Chemistry and Drug Development.