5.4 The medical chemistry strategy

The strategy adopted was to start from first principles. Since prazosin is an alpha1 antagonist, it must compete with the agonist, noradrenaline, for the alpha1 receptor. So the Pfizer scientists decided to compare the structures of the two molecules and look for common structural features that might provide an insight into the way in which they bind to the receptor. One important observation was the fact that, at physiological pH, both compounds would be protonated, nor
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

5.3 Project initiation

In the early 1970s a discovery was made independently by two different researchers, Klaus Starke in Germany and Salomon Langer in Argentina. Their results showed that there were two types of alpha receptor. The first type, which they called alpha1 is the one already described that is found on the blood vessel wall. The second type, which they called alpha2, is located on the nerve-ending itself. Noradrenaline binds to the alpha2 receptors when the alpha
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

4 Summary of video

At the beginning of the video clip, Dr Simon Campbell pointed out that, in the development of any drug, there are a number of criteria that must be satisfied. There must be a clinical need – a medical condition or disease that requires effective treatment. Secondly, there has to be a commercial opportunity; because drug development is so expensive, pharmaceutical companies are less likely to invest resources in developing new therapeutic agents where there is already an adequate range of su
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

3 Reading activity

You will shortly be asked to read through a research paper published in the Journal of Medicinal Chemistry, in which the synthesis and structure–activity relationships of doxazosin and related compounds are described. It has been provided:
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

2 Video activity

The video clip included in this section looks at the development of one particular drug. It examines the complex multidisciplinary process that was involved in its discovery. Before you watch the video, read through the Pre-viewing notes.


Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

1 The chemical industry

The chemical industry is one of the major contributors to the economies of advanced industrial nations.

The importance of organic chemistry in the pharmaceutical industry becomes apparent in the light of the fact that in the UK alone some £2.2b was spent in 1997 on research and development. Literally thousands of different compounds have to be synthesised and tested in the search for the one that will prove to be a successful and valuable therapeutic agent. As a result, the average cos
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

Introduction

This unit examines how organic chemistry is used within the pharmaceutical industry to develop new drugs. You will investigate the process of drug development by following one new product through the intial process and research programme.

This unit is from our archive and it is an adapted extract from Organic chemistry: A synthesis approach (S344) which is no longer in presentation. If you wish to study formally at The Open University, you may wish to explore the courses we offer
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

Acknowledgements

Except for third party materials and otherwise stated (see terms and conditions), this content is made available under a Creative Commons Attribution-NonCommercial-ShareAlike 2.0 Licence

Grateful acknowledgement is made to the following sources for permission to reproduce material in this unit:

Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

2.14 Summing up

Activity 13

0 hours 5 minutes

Dr. Peterson concludes the audio sequence with a summary of all the points covered.

Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

2.11 Consequences of human / chimp pairing

Activity 10

0 hours 10 minutes

This clip refers back to the table of molecular characters, which is shown again here (Figure 9). It explains the consequences of human / chimp pairing in terms of homol
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

2.9 Conflicting morphological characters

Activity 8

0 hours 10 minutes

This clip looks at conflicting morphological characters and at how it is possible to resolve them, with the aid of a table of molecular characters (Figure 9).

Dr
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

2.7 Inferring relationships of common ancestry

Activity 6

0 hours 10 minutes

This clip addresses the question of how one might go about building a tree, or inferring relationships of common ancestry, by recognising evolutionary novelties, or share
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

4.3 Metallic bonding

Two familiar properties of metals point to a simple model of metallic bonding. Firstly, metals have a strong tendency to form positive ions. Thus, when sodium reacts with water, and when magnesium and aluminium react with acids, hydrogen gas is evolved and the ions Na+(aq), Mg2+(aq) and Al3+(aq), respectively, are formed. Secondly, metals are good conductors of electricity: when a voltage difference is applied
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

2.1 Chemical periodicity

The chemistry of the elements is immensely varied. But amidst that variety there are patterns, and the best known and most useful is chemical periodicity: if the elements are laid out in order of atomic number, similar elements occur at regular intervals.

The discovery of chemical periodicity is particularly associated with the nineteenth-century Russian chemist Dmitri Ivanovich Mendeléev (Figure 16). The periodicity is represented graphically by Periodic Tables. Author(s): The Open University

5.1 Arithmetic with real numbers

At the end of Section 1, we discussed the decimals and asked whether it is possible to add and multiply these numbers to obtain another real number. We now explain how this can be done using the Least Upper Bound Property of Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

7 Unit summary

This unit presents an understanding of ‘ethics’ as something related with ‘good’ and ‘bad’. There are other derivative words like ‘optimal’ that might also be used, and there are parochial words which are related to particular communities. When we talk about ethical things, we are liable to confront cultural differences that are reflected in differences in vocabulary. But there are other kinds of differences too. Things have different properties; for example, ‘appearance’
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

4.5 Torture

The question of torture is also raised in the play. Herrenvolk claims that he does not do the torture; it is some Uzbekistan outfit that does it. He actually gives them a justification by saying, in a rather glib way, that it is a lot easier to open a human being than an encrypted laptop. Of course, the question is, is it ever ‘right’ to exploit this as a means of finding things out? I suspect most of us would say ‘no’.


Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

1.2 Ethical examples

But is this a tenable position? In other words, is it only the people who use the technologies who carry the ethical burden? Conversely, is ethics of any interest to engineers, programmers and scientists? What, in the first place, constitutes an ethical issue? To begin examining these questions, let's look at some examples.

Example 1: Th
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share

References

Collins, S., Ghey, J. and Mills, G. (1989) The Professional Engineer in Society, London: Jessica Kingsley Publishers.
Foster, J., with Corby, L. (illustrator) (1996) How to Get Ideas, San Francisco: Berrett-Koehler Publishers, Inc.
Haaland, J., Wingert, J. and Olson, B. A. (1963) ‘Force required to activate switches, maximum finger pushing force, and coeffici
Author(s): The Open University

License information
Related content

Except for third party materials and/or otherwise stated (see terms and conditions) the content in OpenLearn is released for use under the terms of the Creative Commons Attribution-NonCommercial-Share