How is chemistry used in medicine




















The analytical chemist is able to tell us the composition of each one of the manifold substances that compose this intricate machine. He is able not only to discover the various elements which are present, but also to estimate with considerable precision their exact amounts. He can analyze food, as well as the various parts and secretions of the body, and can determine the relation between the composition of the food which is eaten and the resulting bodily substance.

This is all obviously of great value, for it shows us at once in a general way what elements ought to enter into the food; and moreover, in cases of disease it gives us excellent clues to the manner in which the various functions of the body depart from the normal, and thus confers important aid in diagnosis and the suggestion of suitable treatment. But this is an old and obvious story, hence I will not dwell further upon the analytical side of the application of chemistry to medicine, important as it is.

Let us now turn to the second aspect of the subject: namely, the relation of structural chemistry to medicine. Structural chemistry had its origin in the discovery that two substances might be made up of exactly the same percentage amount of exactly the same elements, and yet be entirely different from each other. This fact, that two things may be exactly alike as to their constituents, but very different in their properties, implies that there must be difference of arrangement of some kind or other.

We can obtain the clearest conception of this idea with the help of the atomic hypothesis. If the smallest particles of any given compound substances are built up of still smaller atoms of the various elements concerned, it is clear that we can conceive of different arrangements of these atoms, and it is reasonable to suppose that the particular arrangements might make considerable difference in the nature of the resulting compounds.

Everywhere in life arrangement is significant. In the case of numbers the combination is very different from , although each contains the same individual signs. Why may not arrangement be significant in the case of atoms? I tis not possible in this brief review to explain exactly how chemists obtain a notion of the arrangement of atoms which build up the particles or molecules of each substance. We depend upon two methods of working: one, the splitting-up of the compound and finding into what groups it decomposes; the other, the attempt to build up from these or similar groups the original compound.

Just as among the fragments of a collapsed building you will find bits enough to show whether it was a dwelling, a stable, or a machine-shop, so among the fragments of a broken-down substance you will find bits of its structure still remaining together, enough to indicate something of the original grouping. If from similar fragments the original substance can be constructed by suitable means, the evidence is strong that some knowledge of the structure has been gained.

As regards the usefulness of structural chemistry to medicine, we cannot but see at once its vast importance. If the binding together of infinitesimal atoms in different ways modifies the properties of the resulting substances differently, it is obvious that the particular mode of binding together every one of the complicated compounds constituting our bodies is of vital importance to us.

Moreover, in the case of our food, the arrangement alone of the atoms may make all the difference between nourishment and poison. It is easy to see why these different structures should have different effect in the body. Living, in the case of animals, is a continual process of breaking down more complicated structures into simpler ones; and it is clear that this breaking down will happen in different ways with different groupings, and thus produce different results.

The knowledge of the atomic arrangement of the various substances composing the body is not only bound to furnish an invaluable guide in the study of physiology, pathology, and hygiene, but has already led to the logical discovery of entirely new medicines, built up artificially in the laboratory to fit the especial needs of particular ailments, and to the rational use of foods.

This view has obvious economic, ethical, and social implications, beyond scientific challenges. All stakeholders will have to take them into account. Policy makers will have to examine all disciplines of regulatory science among which the thorny economics cost-benefit analysis of specific research and development projects are of paramount importance and critical to the development of personalized medicine.

As a corollary, there is as well European Patent question, which looks a bit of a holy grail, and ultimately the most important one: is it cost-effective for the very different health care systems to uptake personalized medicine? Medicinal chemistry comprises several scientific disciplines: organic chemistry, bioorganic chemistry, physical organic chemistry, biochemistry, pharmacology, toxicology, molecular biology, analytical chemistry, engineering, genetics, etc.

Nowadays, this complex approach is significantly developing and allows gaining a novel level — personalized medicine. It means: choice of a drug and its use regime should fit every individual specifically, so efficacy of medicinal treatment would improve significantly.

Such a progress is possible thanks to a novel approach in many branches, eg, nowadays polypharmacology is developing fast. It means that pleiotropic properties of compounds, which were treated negatively for a long time, considered in many cases as side effects, are reconsidered gradually as desirable bioactivities. Therefore, exclusively selective compounds that have been a quest for decades are not any more considered as golden standards.

It is a milestone in the fast development of medicinal chemistry and drug development. This strategic COST conference fits the general mission of the COST goals very well: to pick up novel emerging features and principles in science, to support them, and to bring attention of society on the most important novelties. The conference demonstrated the importance of collaboration of many specialists to create innovative products for health care, and food, vitamins, nutritional supplements, as well as high tech materials 2.

Alain van Gool coordinator Personal medicine, Netherlands Organization for Applied Scientific Research turned attention to the relevance of system biology: to monitor the effect of interventions on the human system as a whole and timely adjust when needed 3.

When organism turns from healthy state to disease eg, diabetes, its complications, including nephropathy, brain disorders, cardiovascular events, etc , gradual disturbances of multiple equilibriums occur. Sapienza, A. Drug Dev. Mullen, R. Priming the pipeline. News 82 , 23—42 Landers, P. Drug industry's big push into technology falls short. Big Trouble for Big Pharma. The Economist 14 16 December Flynn, J. In two generations, drug research sees a big shift.

An account of the careers of Leo Sternbach, inventor of Valium, and his son, Daniel, contrasting their experiences in drug discovery.

Lombardino, J. Delay, J. Excitor-motor syndromes provoked by ataratics. Presse Medicale — , 65 , — Granger, B.

The discovery of haloperidol. Encephale , 25 , 59—66 Hippius, H. A historical perspective of clozapine. Psychiatry 60 Suppl. An account of the development history of the first atypical antipsychotic drug clozapine.

PubMed Google Scholar. Pere, J. Clinical psychopharmacology: the example of clozapine Leponex. Encephale 21 Spec. Glennon, R. Lowe, J. CAS Google Scholar.

Howard, H. An account of the discovery of the atypical antipsychotic drug ziprasidone. Capdeville, R. Glivec STI, imatinib , a rationally developed, targeted anticancer drug. Nature Rev. An account of the design and discovery of the anticancer drug imatinib mesylate Gleevec; Novartis. Schindler, T. Structural mechanism for STI inhibition of abelson tyrosine kinase. Science , — Bell, I. An account of a recent programme to discover novel anticancer agents that inhibit farnesyl transferase.

Some of these data come from reference Download references. You can also search for this author in PubMed Google Scholar. Correspondence to Joseph G. Lombardino or John A. Lowe III. Alzheimer's disease. A chemical structure or series of structures that show activity and selectivity in a pharmacological or biochemically relevant screen.

A medication containing an active ingredient that has not been previously approved for marketing in the United States in any form. Members of the cytochrome P superfamily of haem proteins have a key role in the metabolism of drugs, and so understanding the roles of these enzymes is important for issues such as drug bioavailability and drug—drug interactions. A haematological cancer characterized by excessive proliferation of cells of the myeloid lineage. Sharing certain characteristics with other molecules that act as drugs.

The set of characteristics — such as size, shape and solubility in water and organic solvents — varies depending on who is evaluating the molecules. The fraction or percentage of an administered drug or other substance that becomes available in plasma or to the target tissue after administration. The logarithm of this partition coefficient is called log P.

It provides an estimate of the ability of the compound to pass through a cell membrane. The QT interval is a measure of the total time of ventricular depolarization and repolarization. In recent years, several drugs have been withdrawn from the market because of unexpected reports of sudden cardiac death associated with prolongation of the QT interval.

Blockade of the hERG channel has been linked to this effect. Reprints and Permissions. The role of the medicinal chemist in drug discovery — then and now. Nat Rev Drug Discov 3, — Download citation. Issue Date : October Anyone you share the following link with will be able to read this content:.

Sorry, a shareable link is not currently available for this article. Provided by the Springer Nature SharedIt content-sharing initiative. Journal of Parasitic Diseases Journal of Biomedical Science Comparative Clinical Pathology Malaria Journal Advanced search. Skip to main content Thank you for visiting nature.

Download PDF. Key Points Medicinal chemists paly a crucial role in the drug discovery process through the selection and synthesis of compounds that establish structure—activity relationships and achieve efficacy and safety in preclinical animal testing Many aspects of the medicinal chemist's role have changed since the early era of drug discovery when animal testing and small, informal project teams dominated the process.

Abstract The role of the medicinal chemist in drug discovery has undergone major changes in the past 25 years, mainly because of the introduction of technologies such as combinatorial chemistry and structure-based drug design. The process of drug discovery Inventing and developing a new medicine is a long, complex, costly and highly risky process that has few peers in the commercial world. Figure 1: Stages in the drug discovery process.

Full size image. Box 1 Discovery of piroxicam — The project that produced the novel anti-arthritic and anti-inflammatory agent piroxicam Feldene; Pfizer began in and led to the product launching into key European markets in These objectives were to: seek a structurally novel compound with acidic properties, but not a carboxylic acid.

Box 2 Discovery of ziprasidone — Ziprasidone Geodon; Pfizer was launched in for the treatment of schizophrenia, a debilitating mental disease characterized by delusions, social withdrawal, suicidal behaviour and cognitive decline. Box 4 In vitro tests: 'now' and 'then' The following is a typical battery of tests for a modern drug discovery programme 'today'; those marked with an asterisk were also in use 'then'.

Box 5 Farnesyl transferase inhibitors As one of the oncogenes characterized in the s, RAS has been the target of numerous drug discovery efforts. Google Scholar 3 Chanda, S. Article Google Scholar 7 Lipinski, C. July 30, May 21, May 13, February 16, Feature Articles. An exploration for middle school students November 11, The evolving role of telemedicine in epilepsy care November 9, Emphasising vaccines and immunotherapeutics research worldwide November 9, Latest Publication.

October 8, Latest eBook. Together we create a sustainable supply of skills for a sustainable Quick Launch eBook More Details. November 9,



0コメント

  • 1000 / 1000