Subject biological properties

The antitumor activity displayed by the mitosanes and many synthetic aziridines stems from their ability to act as alkylating agents which chemically modify (crosslink) DNA. For this reason, a large number have been screened for antitumor activity, the mechanism of which has been the subject of considerable research effort <75CJC289l). An excellent account of the broad spectrum of biological properties of a multitude of compounds containing the aziridinyl moiety has been published [Pg.93]

Other applications of the previously described optimization techniques are beginning to appear regularly in the pharmaceutical literature. A literature search in Chemical Abstracts on process optimization in pharmaceuticals yielded 17 articles in the 1990-1993 time-frame. An additional 18 articles were found between 1985 and 1990 for the same narrow subject. This simple literature search indicates a resurgence in the use of optimization techniques in the pharmaceutical industry. In addition, these same techniques have been applied not only to the physical properties of a tablet formulation, but also to the biological properties and the in-vivo performance of the product [30,31]. In addition to the usual tablet properties the authors studied the following pharmacokinetic parameters (a) time of the peak plasma concentration, (b) lag time, (c) absorption rate constant, and (d) elimination rate constant. The graphs in Fig. 15 show that for the drug hydrochlorothiazide, the time of the plasma peak and the absorption rate constant could, indeed, be... 

Aldonolactones are useful starting materials for the synthesis of modified sugars. They have also been used as chiral templates in synthesis of natural products. Some of them are inexpensive, commercially available products or they may be obtained readily from the respective monosaccharides. The purpose of this chapter is to survey the main reactions of aldonolactones. Previous reviews on the subject include articles on gulono-1,4-lactones (1) and D-ribonolactone (2). Methods of synthesis, conformational analysis, and biological properties are not discussed in this chapter. 

Although N-nitrosamines (l) have been known since the nineteenth century, it was not until quite recently that they became the subject of intensive investigations. This renewed interest was spurred in large part by the report of Magee and Barnes ( ) on the carcinogenicity of these compounds. Since then, research into the chemistry and biological properties of N-nitrosamines has accelerated. This brief survey is intended to serve both as a summary of some of the frontiers in this area and as an introduction to the chemistry of N-nitrosamines discussed in the remaining chapters of this Volume. 

Pyrido[l,2-a]pyrimidines are being increasingly subjected to study, primarily because of their valuable biological properties. 

The structure of a chemical is responsible for the presence and magnitude of its properties. The properties can be energy levels and their derivatives, as well as physicochemical, or biological, properties. To avoid discrimination between the different properties (which are the subject of detailed consideration in Chapters 3, 4, and 6) in the context of quantitative relationships between structural descriptors (i.e., topological indices [TIs]) and various properties, we will use the broader abbreviation QSPR (Quantitative Structure-Property Relationship). 

The biological properties associated with the polysaccharides are those relating to serological specificity, and, at least to some extent, they serve as bacteriophage receptors. The somatic antigens are also referred to as Endotoxins, but their toxic properties and manifold physiological effects are due to the lipide component, and this subject has been adequately reviewed. ... 

Manzamine alkaloids have been the subject of numerous synthetic studies owing to their novel molecular structure coupled with promising biological properties. Most of the synthetic studies on manzamine alkaloids focused on the construction of the ABCDE pentacyclic lower half of the manzamine structure. 

The biological properties of narco tine have been reviewed (1). The antitussive activity of narcotine once more was a subject of many papers (259-271) and the question of this property, when compared with that of codeine, still remains unclear. Codeine is said to be superior in this respect to narcotine (272) but, according to other authors (273, 274), narcotine has some advantage over codeine. The antitussive activity of different stereoisomers of narcotine have also been studied (271). Narcotine-V-oxide showed an increased antitussive activity (271, 275, 276) and narcotine resinate was recommended as a long-acting antitussive (277, 278), as were the esters of 6-hydroxymethylnarcotine (279). The phar-... 

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