Medicinal and Pharmaceutical Chemistry Commons^™

Synthesis Of Mesoionic Nucleosides As Potential Antineoplastic Agents, Shanaz Mohammedali Tejani

Theses and Dissertations

During the past few decades, analogs of purine nucleosides have been described that are modified either in the heterocyclic base, sugar moiety or both, and many of these modified nucleosides display antiviral and/or antineoplastic activity. The Class II mesoionic purinones are isosteric with their non~mesoionic purinone counterparts. It is conceivable that the mesoionic purinone nucleosides might constitute an entirely novel class of modified nucleosides with potential chemotherapeutic activity. That the mesoionic heterobases are bioisosteric as well as isosteric with non-mesoionic purinones was realized by demonstrating that certain mesoionic xanthine derivatives, such as Anhydro-8-ethylw-5-hydroxy-7-oxo-l,3,4-thiadiazolo[3,2-a]pyrimidinium hydroxide and Anhydro-6-p-chlorobenzyl-8-ethyl-5-hydroxy-7-oxo—l,3,4—thiadiazolo [3,2-a]pyrimidinium hydroxide were comparable …

Meal Interference With Antibiotics Administered Orally In Kentucky Hospitals, Shirley Harper

Masters Theses & Specialist Projects

Hospitals within the State of Kentucky were surveyed to determine if the size of the hospitals influence the frequency of potential meal interference with the administration of oral antibiotics where the "empty stomach" concept must be fulfilled. One hundred and ten hospitals responded to the mailed survey. Of the responding hospitals 103 were short-term and 7 were long-term hospitals. The frequency of conflict was greater for nourishments than with meal interference. Ninety-three and six tenths percent or 103 answered yes when asked if all patients received nourishments on request. The conflicts of potential meal interference ranged from 15 to 40 …

Synthesis And Biological Evaluation Of Sparsomycin Analogues, Scherer Preston Sanders

Theses and Dissertations

In 1962, Owen, Dietz, and Camiener reported the isolation of a new antitumor antibiotic from the culture filtrate of Streptomyces sparsogenes. The structure of the crystalline antibiotic, named sparsomycin, remained elusive until 1970, when Wiley and MacKellar reported results of spectroscopic and degradation studies which elucidated the structure. In addition to the molecular structure, investigators have examined the mechanism of action, toxicity, and related analogues, striving to establish sparsomycin or a synthetic analogue's usefulness as an effective chemotherapeutic agent.

The initial pharmacological evaluation of sparsomycin revealed it possessed activity against KB human epidermoid carcinoma cells, a variety of gram-negative and …

Toxicology And Pharmacology Of N¹-Acetylspermidine And N⁸-Acetylspermidine, Othman A. Alshabanah

University of the Pacific Theses and Dissertations

The polyamines are a group of natural compounds which have been found in almost all living tissues. N¹- and N⁸- acetylspermidine have been known for a considerable time as normal constituents in human urine, but their physiological role is unknown. Recent studies have indicated the presence of enzymes in the tissues capable of converting spermidine into N¹-acetylspermidine and N⁸-acetylspermidine and other enzyme activities which catalyze deacetylation and interconversion reactions.

One approach for determining physiologic activity of an endogenous compound is to observe their pharmacologic and toxicologic effects. In the present study, the …

Synthesis And Evaluation Of Some Arylalkenyl And Arylepoxyalkyl Hydrogen Succinates And Hydrogen Glutarates As Inhibitors Of Rat Liver Β-Hydroxy-Β-Methylglutaryl Coenzyme A Reductase, Paul Emil Marecki

Theses and Dissertations

Atherosclerotic disease is an almost universal phenomenon and increases in severity and frequency with increasing age. Atherosclerosis may contribute to several disorders including bursting of an artery, blockage of an artery, or induction of arterial clotting. The culmination of these diseases is usually premature since at the time of death the unaffected organs are in reasonably satisfactory condition and could have operated for several more years. Among the many factors which act in concert to produce the disease, serum cholesterol levels play a central role. It has been suggested that the lowering of cholesterol levels will provide an effective means …

The Pharmacology Of Rodenticides, S. A. Peoples

Vertebrate Pest Conference Proceedings: 4th (1970)

The compounds used as rodenticides are tremendously varied in their chemical structure and mechanism of action. With a few exceptions, these agents are generally poisonous to all animals, including man, and a great deal of study has been directed to their toxicity in animals other than rodents. However, the development of new compounds as Norbormide and certain antifertility drugs which are highly selective in their action may justify the hope that the ideal rodenticide free of secondary toxic hazards will soon be available. Until this happy announcement is made, a review of the pharmacology of the older compounds is in …

Syntheses And Antimicrobial Activities Of Some 4-Aza-Sitostane Derivatives, Hassan Y. Aboul-Enein

Electronic Theses and Dissertations

Research into the chemical and pharmacological properties of aza­steroids has become of interest because of their potential value as pharmacodynamic and chemotherapeutic agents. A nitrogen atom, for example, would be able to interact, unlike carbon, with a variety of sites in enzymes by means of ionic-ionic, ionic-dipole, dipole-dipole and hydrogen.bonds. Azasteroids having a nitrogen, atom might be adsorbed more strongly or in a different orientation to a given enzyme, and also may produce.a different biologic effect with a new spectrum of biological activities. The pharmacological.activities of a number of synthetic azasteroids, have been reported.

This investigation is concerned with the …

The Alkaloids, Felix F. Barre

Electronic Theses and Dissertations

This thesis, presented for the degree of Bachelor of Science, provides a systematic chemical study of the alkaloids, a class of complex nitrogenous plant substances possessing basic properties. Barre opens by defining the alkaloids and surveying the various systems used to classify them, whether by natural versus artificial origin, chemical nucleus (pyridine, quinoline, or isoquinoline), volatility, or botanical family of origin, and outlines their general physical and chemical properties, including solubility, optical activity, and characteristic reactions with precipitating and color-test reagents.

The thesis details standard laboratory methods for the extraction and separation of alkaloids from plant material, including a step-by-step …