Synthetic oligoureas of metaphenylenediamine mimic host defence peptides in their antimicrobial behaviour: Sarah R. Dennison, David A. Phoenix, and Timothy J. Snape,* Bioorg. Med. Chem. Lett., 2013, In Press
Additional expertise includes computer-aided drug design. This is being applied in the search for novel dopamine selective ligands, phosphodiesterase inhibitors and retinoic acid derivatives. Compounds identified are synthesised and subsequently screened for pharmacological activity.
STEREOCHEMISTRY AND ITS ROLE IN DRUG DESIGN 11, 12, 13, 14, 15
We are also interested in exploiting molecular conformation in the design and preparation of diagnostic probes to detect enzymes over-expressed in disease and the biomembrane interaction of novel nanosized drug delivery systems.
A+ analogue synthesis in drug design | OnlineDrug☀
In recent years drug stereochemistry has become a significant issue for both the pharmaceutical industry and the regulatory authorities. The significance of stereoisomerism in antimicrobial agents is addressed in this review using examples drawn from the β-lactams, as being representative of semisynthetic agents, and the quinolones, as examples of synthetic agents. Within these two groups of compounds it is clear that stereochemical considerations are of significance for an understanding of concentration effect relationships, selectivity in both action and inactivation and for an appreciation of the mode of action at a molecular level.
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A survey of 1675 drugs carried out in the early 1980s, indicated that 1200 (71.6%) could be classified as synthetic and 475 (28.4%) as natural products or semisynthetic agents. Four hundred and eighty (28.7%) of the synthetic compounds were chiral and of these 58 (3.5%) were marketed as single isomers; the remainder (25.2%) were marketed as racemates. In contrast 469 (28%) of the natural or semisynthetic products were chiral and of these 98.3% (461) were marketed as single isomers. More recent surveys have indicated that the position with respect to natural/ semisynthetic products has not changed greatly but that the proportion of synthetic single isomer drugs increased considerably up to 1991.
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Preclinical development encompasses the activities that link drug discovery in the laboratory to initiation of human clinical trials. Preclinical studies can be designed to identify a lead candidate from several hits; develop the best procedure for new drug scale-up; select the best formulation; determine the route, frequency, and duration of exposure; and ultimately support the intended clinical trial design. Concurrent preclinical development activities include developing a clinical plan and preparing the new drug product, including associated documentation to meet stringent FDA Good Manufacturing Practices and regulatory guidelines.