Chlorinated Sugars: A Biochemical Approach to the Control of Male Fertility

6‐Chloro‐6‐deoxyglucose (120 μmol; 24 mg kg b.wt.), 6‐chloro‐6‐deoxyfructose (< 240 μ 48 mg/kg b.wt.), 6‐chloro‐6‐deoxysucrose (240 μmol; 85 mg/kg b.wt.), ′6‐chloro‐′6‐deoxysucrose (< 240 μmol; 85 mg/kg b.wt.) and 6.′6‐dichloro‐6,′6‐dideoxysucrose (240 μmol; 89 mg/kg b.wt.) administered to male rats daily, by oral gavage, render them infertile after 7 days treatment. The effect is sustained through at least 4 weeks of treatment and is reversed 3 to 6 weeks after treatment is withdrawn. Spermatozoa from the cauda epididymidis of treated rats oxidize only 10% as much glucose as spermatozoa from controls and their ATP and total adenine nucleotide content fall more rapidly during incubation with 2 mM [U14C]D‐glucose. These biochemical effects are associated with a more rapid decline in cell motility. The LD50 for 6‐chloro‐6‐deoxyglucose in the rat is > 16 g/kg b.wt. Administration of [36Cl] ′6‐chloro‐′6‐deoxysucrose has shown this compound to be extensively dechlorinated in vivo. Chlorodeoxy sugars are discussed as potential male antifertility agents worthy of further investigation.