Antihypertensive Agents

Antihypertensive Agents E d w a r d L . Engelhardt, EDITOR Merck Sharp & Dohme Research Laboratories A symposium sponsored by the Division of Medicinal Chemistry at the 169th Meeting of the American Chemical Society, Philadelphia, Penn., April 8, 1975 ACS SYMPOSIUM AMERICAN SERIES CHEMICAL SOCIETY WASHINGTON, D. C. 1976 In Antihypertensive Agents; Engelhardt, E.; ACS Symposium Series; American Chemical Society: Washington, DC, 1976. 27 Library of CongressCIPData Antihypertensive agents. (ACS symposium series; 27 ISSN 0097-6156) Includes bibliographical references and index. 1. Hypotensive agents—Congresses. 2. Adrenergic beta receptor blockaders—Congresses. I. Engelhardt, Edward L., 1919. II. American Chemical Society. Division of Medicinal Chemistry. III. Series: American Chemical Society. ACS symposium series; 27. [DNLM: 1. Antihypertensive agents—Congresses. 2. Hypertension—Drug therapy—Congresses. WG340 A629 1975]. RM345.A57 615'.71 76-15416 ISBN 0-8412-0333-4 ACSMC8 27 1-96 Copyright © 1976 American Chemical Society All Rights Reserved. No part of this book may be reproduced or transmitted in any form or by any means—graphic, electronic, including photocopying, recording, taping, or information storage and retrieval systems—without written permission from the American Chemical Society. PRINTED IN THE UNITED STATES OF AMERICA In Antihypertensive Agents; Engelhardt, E.; ACS Symposium Series; American Chemical Society: Washington, DC, 1976. ACS Symposium Series R o b e r t F . G o u l d , Series Editor In Antihypertensive Agents; Engelhardt, E.; ACS Symposium Series; American Chemical Society: Washington, DC, 1976. FOREWORD The ACS SYMPOSIUM SERIES was founded in 1974 to provide a medium for publishin format of the SERIES parallels that of the continuing ADVANCES IN CHEMISTRY SERIES except that in order to save time the papers are not typeset but are reproduced as they are submitted by the authors in camera-ready form. As a further means of saving time, the papers are not edited or reviewed except by the symposium chairman, who becomes editor of the book. Papers published in the ACS SYMPOSIUM SERIES are original contributions not published elsewhere in whole or major part and include reports of research as well as reviews since symposia may embrace both types of presentation. In Antihypertensive Agents; Engelhardt, E.; ACS Symposium Series; American Chemical Society: Washington, DC, 1976. PREFACE ipvuring the quarter of a century that I have been involved in the search for antihypertensive agents, there has been a continuing trend by the clinician to use antihypertensive therapy in patients with less and less severe hypertensive disease. This has led to a need for agents that are effective in milder degrees of hypertension and substantially free from side effects that might reduce compliance of the patient with the therapeutic regimen The four papers tha view of the current status of antihypertensive agents in use or in the later stages of development in 1975. The saluretic diuretics are not described in detail, although G. Onesti discusses their importance as an integral part of the antihypertensive therapeutic armamentarium. The intensive and extensive research in /^-adrenergic blocking agents is critically reviewed by R. Clarkson. W. Hoefke discusses the centrally acting antihypertensive agents as typifi