SEARCH FOR NOVEL ANTI-FERTILITY AGENT BY MONITORING IN VITRO METABOLIC INHIBITION, CELL MOTILITY AND CELLULAR INTERACTIONS OF NIFEDIPINE ANALOGUES

摘要

Current family planning measures predominantly target a female clientele, with relatively few significant developments in male fertility regulation. At present, only effective methods for contraception in men are those that prevent sperm transport, such as condoms and vasectomy. Thus, in an attempt to synthesize non-hormonal, safe, reversible and oral male contraceptive, we have used nifedipine as a prototype molecule. Nifedipine is a calcium channel blocker and popular anti-hypertensive drug. Its reversible anti-fertility effect is a well-known side effect. In order to develop male oral contraceptive, we have synthesized four analogues; m-hydroxy (D5), m-chloro (D6), p-nitro (D7), p-methoxy (D8) aryl 1, 4-dihydropyridine derivative of nifedipine and monitored their effect on sperm motility and metabolic activity. To highlight their mechanism of action on sperm function through membrane interaction, we have studied their molecular level interactions with model membrane using NMR and DSC technique. One of the synthesized analogues (D5) showed promising results.