rather specific interactions rather than a nonspecific interaction at hydrophobic regions. This is consistent with the inability of the 1,g-dideoxy derivative to antagonize forskolin's activation of adenylate cyclase.One of the aims of this study was to determine if the potency of forskolin in activating adenylate cyclase could be increased by appropriate derivatization. Although a number of derivatives of forskolin were active, there were none with greater potency than the native molecule. The results of this study do, however, allow characterization of the binding site in terms of the rank order of potency of the partially active species. This could be used to establish a correlation between the initiation of a physiological process induced by forskolin and its derivatives with the activation of adenylate cyclase. Furthermore, a number of inactive derivatives of forskolin are identified that are not grossly different in structure from forskolin, and these can be used as controls in assessing nonspecific effects due to the diterpenoid structure. The similarity of the data on the activity of forskolin derivatives with brain and heart adenylate cyclase, while limited, suggests that the forskolin site may be relatively invariant in different tissues and species (rat, rabbit and guinea pig); Two catechoyl derivatives of desferrioxamine B have been synthesized. The more soluble N-(2,3-dihydroxy-4 carboxybenzoyl)desferrioxamine B derivative was found to remove iron from the human iron transport protein transferrin with a pseudo-first-order rate constant of 8.2 X mid (0.2 mM ligand concentration). These results indicate that, unlike desferrioxamine B (Desferal) itself, the synthetic monocatechoyl derivative is kinetically able to remove transferrin-bound iron. The possible use of these derivatives in the treatment of transfusion-induced iron overload is discussed; The preparation, determination of isomeric configuration, and antifungal properties of (E)-l-(5-chlorothien-2 yl)-2-(1H-imidazol-l-yl)ethanone 2,6-dichlorophenylhydrazone hydrochloride (1) are described. In vitro, compound 1 has been shown to have activity against Candida albicans comparable with miconazole. When administered orally to animals with experimentally induced vaginal candidiasis or systemic candidiasis, compound 1 produced results approaching those produced by ketoconazole. In addition, topical administration of compound 1 to rats with vaginal candidiasis produced results comparable with those produced by similar administration of clotrimazole. Unlike ketoconazole, which is active by a mechanism that is essentially fungistatic, compound 1 shares with miconazole a mode of action that is fungicidal. However, unlike miconazole, compound 1 exhibits activity following oral administration. Compound 1 has been found to be negative in the Ames test