Amidation Bioactive agents

In an earlier investigation by the authors (1) biodegradable poly(ester-amides) were prepared and used as drug delivery devices for internally administered bioactive agents. Unsaturated analogs, (II), were prepared by Chu et al. (2). 

It will be recalled that certain local anesthetic amides, such as procainamide and lidocaine, are active antiarrythmic agents. Annelation of a second aromatic ring is consistent with bioactivity. Bunaftine (21) is such an agent, prepared simply from reaction of the acid chloride of 1-naphthoic acid and... 

The articles contained in this volume include the interaction of alkaloids with neuroreceptors and ion channels, anthracyclines suited for antibody-directed enzyme prodrug therapy and metabolites from soilborne fungi. Several articles are concerned with bioactive natural products from marine sources. The other areas covered include natural products with polyene amide structures, potential hypoglycemic agents, biological activity of essential oils, bioactive saponins and biologically active diterpenoids. 

The carboxylesterase superfamily catalyzes the hydrolysis of ester- and amide-containing compounds. These enzymes are found in both the ER and cytosol of many cell types and are involved in detoxification or metabolic activation of drugs, environmental toxins, and carcinogens. Car-boxylesterases also catalyze the activation of prodrugs to their respective free acids. For example, the prodrug and cancer chemotherapeutic agent irinotecan is bioactivated by plasma and intracellular carboxylesterases to the potent topoisomerase inhibitor SN-38. 

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