A. R. Schwartz, M. Hahnemann
1974
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Journal
Annual Reports in Medicinal Chemistry
Abstract
Publisher Summary This chapter discusses the development of antiviral agents. The status of ascorbic acid as a clinically available therapeutic substance in relation to viral diseases is analyzed. Tissue, leukocyte, and plasma levels of ascorbic acid are quite variable and tend to fall in a stress situation, with a corresponding fall in urinary excretion of ascorbic acid in the unsupplemented state. Supplementary ascorbic acid given to adults, results in transient increases in plasma levels and increased excretion in the urine, with a degree of augmentation relating to dose, but not uniformly, in these substrates. Derived from the fermentation of Streptomyces mediterranei , this family of ansa-macrolide drugs possesses a very broad spectrum of antimicrobial activity against gram-positive and gram-negative bacteria, mycobacteria, chlamydia, and several viruses. The 3-hydrazonomethyl derivatives of rifamycin SV with bulky side chains are excellent inhibitors of murine sarcoma virus (MSV) polymerase, in 3-formyl rifamycin SV oxime derivatives, good correlation is seen between the length of the alkyl- o -substituent and RNA polymerase inhibitory activity. It is observed that Rifamycin SV-3-substituted derivatives, other than 3-iminomethyl, 3-formylhydrazo, or 3-formyl oxime, are either inactive or on minimally active against RNA polymerases.