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Hydroxyurea Derivatives: Oxamyl Hydroxamic Acid

Veterans Administration Hospital, and Department of Pharmacology, Medical College of South Carolina, Charleston, South Carolina

Oxamyl hydroxamic acid (OHA), a derivative of hydroxyurea, was shown to inhibit the growth of Gram-negative bacteria; inhibition was accompanied by marked elongation of individual cells as well as by metabolic alterations. No effects were observed on Gram-positive bacteria or fungi. DNA, RNA, soluble ribonucleotide (RNT), and protein analyses of Escherichia coli grown in the presence of 0.002 M OHA revealed a decrease in total protein and decreased DNA/protein, DNA/RNA, and RNT/RNA ratios as compared with the control values, and an increased RNA/protein ratio. Structural changes as observed by electron microscopy included marked elongation of individual cells and a diminution of the bacterial nucleoid. OHA induced a pronounced and immediate inhibition of DNA synthesis in Ehrlich ascites tumor cells, which was followed by a decreased rate of protein synthesis, but to a lesser degree. No effect on RNA synthesis was demonstrated. Other pharmacologic actions of OHA consisted of inhibition of urease, alteration of the ultraviolet absorption spectrum of pyridoxal phosphate, and oxidation of hemoglobin. Significant biotransformation of OHA by rat liver slices or homogenates, or by ascites tumor cells, could not be demonstrated.

¹ Aided by Grant GM-13958 from NIH, USPHS.

Received 3/25/66. Accepted 6/ 8/66.