In-vitro metabolic inhibition and antifertility effect facilitated by membrane alteration: search for novel antifertility agent using nifedipine analogues
Waghmare, A.; Kanyalkar, M.; Joshi, M.; Srivastava, S.
European Journal of Medicinal Chemistry 46(9): 3581-3589
2011
ISSN/ISBN: 1768-3254 PMID: 21632156 DOI: 10.1016/j.ejmech.2011.05.022Document Number: 226466
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.
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