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Showing papers in "Progress in Medicinal Chemistry in 1969"


Book ChapterDOI
TL;DR: Pyrimidine derivatives have been found to possess fungicidal, antibacterial, antimitotic, antithyroid and surface-anaesthesia activities, with the exception of pyrimidine antibiotics.
Abstract: Publisher Summary The beginning of pyrimidine chemistry may be traced back to the isolation of alloxan, a pyrimidine derivative. The synthesis of barbituric acid from urea and malonic acid perhaps marked the next major event in the development. Since then pyrimidines have occupied a unique and important place in the fields of biological and medicinal chemistry. It is well known that uracil, thymine, and cytosine are essential constituents in nucleic acids; thiamine that possesses antiberiberi activity was the first vitamin discovered in the B series; barbiturates are widely used as sedatives; pyrimethamine is highly potent against erythrocytic parasites in antimalarial study; aminometradine (Mictine) is an orally effective diuretic; and the 5-halogen-substituted uracils and derivatives have recently been reported as antitumour or antiviral agents, or both. Other pyrimidine derivatives have been found to possess fungicidal, antibacterial, antimitotic, antithyroid and surface-anaesthesia activities. With the exception of pyrimidine antibiotics, in this chapter, pyrimidines are classified based on special structural features and functional groups. The chapter discusses the following areas: 2,4- diaminopyrimidines, halogenated pyrimidines, sulphur-substituted pyrimidines, 2-substituted 4-amino-5-hydroxymethylpyrimidines, pyrimidine sulphonamides and pyrimidine antibiotics.

58 citations


Book ChapterDOI
TL;DR: An important section of the pharmacopoeia comprises the appendices in which general methods of test are set out, which provides specifications that apply to the medicines at the time they are delivered to the patient.
Abstract: Publisher Summary The first British Pharmacopoeia was published in 1864. It was compiled by a committee that was composed of members of the council and was divided into three sub-committees working separately in London, Edinburgh, and Dublin. An important section of the pharmacopoeia comprises the appendices in which general methods of test are set out. The revision of this section is mainly undertaken by committees on general analytical methods and biological assays, while a third deals with the reagents and provides specifications for the majority of the substances and materials used in the tests and assays, on which the standards of the pharmacopoeia depend. Advantage is taken of the issue of an addendum to include amendments to monographs already in the pharmacopoeia. In the earlier British pharmacopoeias, the monographs concentrated more on the preparative stages of the medicines described therein, than on the examination of the final product. The identity and quality of the ingredients were specified, the proportions in which they were to be compounded were fixed, and the pharmaceutical procedures carefully described. The commission now aims to provide specifications that apply to the medicines at the time they are delivered to the patient.

53 citations


Book ChapterDOI
TL;DR: This chapter attempts to stress new and neglected aspects of the catecholamine metabolism, including the role of MAO in the inactivation of the sympathomimetic amines.
Abstract: Publisher Summary This chapter attempts to stress new and neglected aspects of the catecholamines. An attempt has also been made to indicate briefly some of the important historical landmarks and key observations that have given such impetus to the subject in recent years. Catecholamine formation in the mammal takes place in structures belonging to, or deriving from, the nervous system, largely occurring in adrenal Medulla, extra-medullary chromaffin tissue, heart, brain, and sympathetic nerves and ganglia. Because of their known difficulty in crossing the blood-brain barrier, the presence and rapid turnover of dopamine and noradrenaline in the brain, is indirect evidence for their synthesis in situ; their common precursor, DOPA, gains easy access to the brain from the circulation. The complexity of catecholamine metabolism had been foreshadowed in the early fifties when it was found that after cleavage of the molecule between the and methyl carbon atoms, adrenaline gives rise to at least five or six urinary catabolite; one possible catabolite, DHMA, was later found in human urine. It is derived from adrenaline by the action of MAO. For many years, it was thought that MAO was the primary mediator in the inactivation of the sympathomimetic amines.

34 citations


Book ChapterDOI
TL;DR: Various substances have an antibacterial action by virtue of their effect on the cytoplasmic membrane, and such substances are discussed in this chapter.
Abstract: Publisher Summary In recent years, remarkable progress has been made in the elucidation and understanding of the metabolic and biosynthetic processes of microorganisms and of the effect thereon of various antimicrobial compounds. This chapter discusses the mode of action of various antibacterial substances. Antibacterial agents are divided into sections, depending on the nature of their effect. The chapter presents a discussion on antibacterial agents and bacterial cell walls. A summary of the main constituents of cell walls of gram-positive and gram-negative bacteria is presented in the chapter. Various substances have an antibacterial action by virtue of their effect on the cytoplasmic membrane, and such substances are discussed in this chapter. Such substances include novobiocin, polymyxin, chlorhexidine, quaternary ammonium compounds and phenols.

22 citations


Book ChapterDOI
TL;DR: This chapter discusses basic physiology of the coronary vascular bed as it is essential before the mode of action of drugs that act upon it can be fully grasped, and some of the possible ways by which a drug can influence the coronary circulation.
Abstract: Publisher Summary Over the past few years, several new coronary vasodilator drugs have been introduced into therapeutics, with varying claims to effectiveness in treating coronary insufficiency. In addition, much new work has been carried out on the mode of action of the group of drugs first introduced for the treatment of angina pectoris over 100 years ago—the nitrites. This chapter discusses the research in this field over the past several years, concentrating particularly on the mode of action of these compounds. The chapter discusses basic physiology of the coronary vascular bed as it is essential before the mode of action of drugs that act upon it can be fully grasped. Some of the possible ways by which a drug can influence the coronary circulation have been summarized. Recent methods and refinements of evaluating the action of drugs on the coronary circulation are described.

20 citations


Book ChapterDOI
TL;DR: This chapter presents contents list that are classified partly on a chemical and part on a biological basis, and most of the main classes are subdivided to reduce the amount of searching.
Abstract: Publisher Summary The explosive rate of growth of the scientific literature in recent years makes a heavy demand on the time of those who seek information on a particular topic. A reasonably broad view of the term “medicinal chemistry” has been taken, partly because it is almost impossible to define the subject and partly because the chapter may be of interest to pharmacologists, biochemists, microbiologists and possibly others. This chapter presents contents list that are classified partly on a chemical and partly on a biological basis. The first half of the chapter lists titles according to a chemical classification, whereas in the second half a medicinal basis is used. Most of the main classes are subdivided to reduce the amount of searching. Within each class or subdivision, the titles are arranged in reversed chronological order. When several titles are available in any one year, they are arranged alphabetically according to the first author's surname.

4 citations