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Preface [Hot topic: Modern Aspects in the Design And Discovery of Novel Antihypertensive Drugs (Guest Editor: Thomas Mavromoustakos)]

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Modern Aspects in the Design And Discovery of Novel Antihypertensive Drugs

This issue is dedicated to cardiovascular diseases and mainly to hypertension, an undesired symptom associated with an increase in workload for the heart leading to an elevated blood pressure. The increase of blood pressure in the human body can cause destructive health problems and even death. Hypertension is not easily diagnosed and is highly spread in our modernized societies, due to the diet style and stressful life.

Several aspects of hypertension have been covered in this issue. The majority of the articles cover Medicinal Chemistry Aspects of Hypertension and the major Renin Angiotensin System. Two important drug classes that interfere with this system are Angiotensin Converting Enzyme (ACE inhibitors) and AT1 antagonists. These two drug classes have important similarities as they act on the same system but it is shown also to have certain differences of clinical importance. In one of the articles, RAS inactivation was shown to confer susceptibility to the hematocrit-lowering effects of angiotensin-converting enzyme inhibitors or angiotensin receptor blocker.

Information on the conformational analysis and receptor binding for these two classes of molecules are provided in this issue. It is stated that comprehension of the relationship between the conformation and bioactivity may lead both to decipher of the molecular basis of hypertension and to design of novel molecules with better pharmacological profile. This explains the tremendous efforts to reveal the key stereo electronic features that determine bioactivity of hormone Angiotensin II, which is known to be the vasoconstrictor of the RAS system.

The physicochemical parameters that govern drug:membrane interactions are described. The stereoelectronic properties of the drug molecules in membrane bilayers may in turn affect the bioactivity of the drugs. The use of in silico technology to simulate the drug circulation to its active site is described in another article. The development of powerful computers and programming will undoubtedly contribute in the augmentation of up-to-present knowledge concerning the pharmacokinetics and the drug mode of action.

Furthermore, the identification of genetic polymorphisms in the effectors involved in the pathophysiology of hypertension or in the responsed to anti-hypertensive drugs, such as the p22phox subunit of NADPH oxidase, β- adducin or adrenergic receptors, has promoted the prospective of better understanding of hypertension and individualized strategies for its treatment.

It would be an omission not to include in this issue some clinical aspects of the disease and some comparisons of clinical profiles of different drug classes against hypertension. By including these articles we clearly emphasize the necessity of a broad collaboration between the scientists involved in the hypertension. It is undoubted today that in order to regulate the blood pressure and control hypertension's serious health consequences, a collaboration of many disciplines is necessary. Theoretical chemists, biologists, medicinal chemists, doctors, pharmacists specified in pharmacokinetics and drug capsulation, must develop collaborative human networks in order to succeed in controlling hypertension.

We would like to thank all authors for contributing in the publication of this issue and especially the graduate students P. Zoumpoulakis, I. Kyrikou and E. Matzourani for aiding in the editing.
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Document Type: Book Review

Affiliations: Institute of Organic and Pharmaceutical Chemistry National Hellenic Research Foundation Athens, Greece

Publication date: February 1, 2004

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