Antiviral Agents

In the treatment of infections caused by rapidly mutating viruses like human immunodeficiency virus (HIV), combination therapy with multiple drugs act ing by different mechanisms offers several advantages over monotherapy. It may provide: synergistic effect, possible reduction of dosages and side-effects, and reduction of the chance of drug resistance. In the past few years, hun dreds of HIV protease inhibitors have been synthesized and tested in order to overcome the limitations of reverse transcriptase inhibitors like zidovudine and others. In this review, emphasis is placed on the development of HIV pro tease inhibitors as antiviral agents against HIY, and structure-activity rela tionship analysis of saquinavir and related compounds. Limitations of some protease inhibitors and ways to overcome the shortcomings are presented. Among these many protease inhibitors five have been marketed during 1995-1999. They are saquinavir, ritonavir, indinavir, nelfinavir and ampre navir. Their different structural features, important physicochemical, phar macokinetic and clinical profiles are presented in a table form for easy com parison. It is hoped that in the future new drugs based on additional mech anisms can be developed for the treatment of AIDS. Contents 4 1 Introduction .................................................................... . HIV protease as a target for chemotherapy ................................... . 2 5 Design of protease inhibitors .................................................. . 3 5 Basis of rational design of HIV protease inhibitors ........................... . 3.1 5 New development of HIV protease inhibitors ................................ . 6 3.2 HIV protease inhibitors on the market ........................................ . 20 4 20 4.1 SAR of saquinavir and related compounds .................................... .

Klappentext

20 4 20 4.1 SAR of saquinavir and related compounds .................................... .

Zusammenfassung
The unfortunate appearance of AIDS, the manifold problems with herpesviruses and other viruses attacking humans have led to an enormous dynamism of worldwide research and to an immense increase in the corresponding literature. With this first Special Topic of the monograph series Progress in Drug Research, the editor and the publishers undertake an effort to supply concise reviews on virus research, especially on the development of new and future antiviral agents in some important and widespread viral diseases. Latest Progress in Drug Research articles dealing with new chemotherapeutics for the treatment of the most threatening viral diseases are presented. These very well received articles were upgraded and supplemented with new chapters to form this actual overview of the achievements in the respective fields of virus research. This special volume contains six review articles covering the latest studies on the HIV and hepatitis C and B viruses...

Inhalt
Development of HIV protease inhibitors: A survey.- Anti-influenza drugs and neuraminidase inhibitors.- Recent advances in prevention and treatment of hepatitis C virus infections.- Drug discovery and development of antiviral agents for the treatment of chronic hepatitis B virus infection.- Current and potential therapies for the treatment of herpesvirus infections.- Protease inhibitors as potential antiviral agents for the treatment of picornaviral infections.