title: In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues.
abstract: In search of non-hormonal male contraceptives, analogues of nifedipine, which causes reversible infertility, have been synthesized and their interaction at molecular level with model membrane has been probed. Analogues act differently with respect to their antifertility action. This is achieved by altering the cell metabolism thereby directly affecting the motility which is responsible for fertility. Secondly, these drugs bind differently to the interior of the cell-membrane affecting the membrane fluidity, architecture and dynamics. Sulfasalazine and D(4) interact to a larger extent and alter the lipid bilayer phase to a hexagonal. D(1), D(2) and D(3) do not have considerable effect. D(4) is the most promising candidate as a lead compound for the development of novel non-hormonal male antifertility agents.
authors.affiliation: Prin K M Kundnani College of Pharmacy, Cuffe Parade, Mumbai 400005, India.
authors.forename: Abhijeet
authors.initials: A
authors.lastname: Waghmare
authors.forename: Meena
authors.initials: M
authors.lastname: Kanyalkar
authors.forename: Mamata
authors.initials: M
authors.lastname: Joshi
authors.forename: Sudha
authors.initials: S
authors.lastname: Srivastava
mesh_terms: D002152:Calorimetry, Differential Scanning; D002462:Cell Membrane / Q000187:drug effects; D003272:Contraceptive Agents, Male / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D009543:Nifedipine / Q000031:analogs & derivatives* / Q000494:pharmacology; D013081:Sperm Motility / Q000187:drug effects
chemical_list: D003272:Contraceptive Agents, Male; D009543:Nifedipine