Roles of the medicinal chemist

Lombardino JG, Lowe JA. The role of the medicinal chemist in drug discovery—then and now. Nat Rev Drug Discov 2004 3 853-62. 

Bioassays have been likened to analytical machines insofar as pharmacologists use them to assign biological properties to compounds in the same way a chemist measures the physical-chemical properties of molecules. If the fundamental role of the medicinal chemist is to optimize the pharmaceutical properties of so-called lead compounds by structural modification, then the role of the pharmacologist in the drug discovery process is to select, develop, and apply bioassays to provide relevant robust data that inform the medicinal chemist of the impact of the modifications he makes. 

Middleton, D. The Role of the Medicinal Chemist in Drug Discovery Controlling the Controllables. 230th National Meeting of the American Chemical Society, 2005 August 28-September 1, Washington, DC. 

The role of the medicinal chemist is to design and synthesize a drug structure that has the maximum beneficial effects with a minimum of toxic side effects. This design has to take into account the stereoelectronic characteristics of the target active or receptor site and also such factors as the drug s stability in situ,... 

Box 11.3 Some Roles of the Medicinal Chemist in New Drug Discovery... 

An outstanding review of industry changes and their effects on the job of a medicinal chemist can be found in Lombardino, J.G., Lowe III, J.A. The role of the medicinal chemist in drug discovery—then and now. Nat. Rev. Drug Discov. 2004, 3, 853-862. 

With the generally increasing concerns about the environment, chemical pollution, and green issues, GSK and other pharmaceutical and chemical companies have made significant efforts to incorporate sustainable business prachces and procedures in the manufacture of Ac live Pharmaceutical Ingredients (API) used in pharmaceutical products. This has placed greater emphasis on the role of the process chemist as they seek to discover commercially viable and environmentally sustainable processes for the manufacture of the new medicines. 

Structural Modification of Antibiotics. Historical Review. Writing in 1945, Waksman (7) set forth in prophetic terms the role that the medicinal chemist was to play in the antibiotic field. 

Few topics are closer to the heart of the medicinal chemist than heterocycles. Heterocyclic compoxmds form the centerpiece of the most important classes of antibiotics, such as the beta-lactams (penicillin), macrolide lactones (erythromycin), and more recently the quinolones, but the reach of heterocyclic structures in bioactive molecules goes far beyond these examples. One needs to only consider the antimalarials quinine and artemisinin, the anti-HIV reverse-transcriptase inhibitors (e.g., AZT and 3TC), and the important anticancer agents— vincristine and pemetrexed— to begin to see the role that heterocycles play in our world today. 

Overview of Hit to Lead The Medicinal Chemist s Role from HTS Retest to Lead Optimization Hand Off. 1... 

This research has progressed only because the science was willing to allow Nature s biomolecules to intervene earlier than is usual for medicinal chemistry protocols. The role of biomolecules has been elevated from spectator to key player, to guide and instruct the synthesis of potent inhibitor molecules, while the medicinal chemist acts to facilitate this process. The in situ selection and assembly of fragments could in principle be screened by an activity assay or by any number of analytical techniques for drug discovery, however, it is a... 

The final chapter, The Role of the Membrane Actions of Phenothiazines and Flavonoids as Functional Modulators by K. Michalak, O. Wesolowska, N. Motohashi and A. B. Hendrich, presents a very comprehensive review on important biological effects of phenothiazines and flavonoids due to interactions with membrane proteins and the lipid phase of membranes. The discussion includes the influence of these heterocycles on model and natural membranes, modulation of MDR transporters by these heterocycles, and the effects of these hetero cycles on ion channel properties. This review may attract much interest from medicinal and pharmaceutical chemists as well as heterocyclic chemists in the life science fields. 

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