Syntheses and bioevaluation of substituted dihydropyridines for pregnancy-interceptive activity in hamsters

Abstract

A number of 2,6-dimethyl-3,5-bis(methoxycarbonyl)-4-substituted-1,4- dihydropyridines were synthesized and evaluated for pregnancy-interceptive activity in mated hamsters. Out of 24 compounds, 12, 15, 21, 22, 28, and 34 caused a marked reduction in the number of implantations when administered on days 3-8 postcoitum. In an in vitro competition assay, none of the compounds exhibited noticeable binding affinity for uterine progesterone receptors. The results reported here have helped to identify new leads for developing pregnancy-interceptive agents and the active compounds do not seem to elicit their interceptive effect through receptor-mediated inhibition of progesterone action in hamster uterus.

Chemoenzymatic synthesis and biological evaluation of enantiomerically enriched 1-(β-hydroxypropyl)imidazolium- and triazolium-based ionic liquids

“…Imidazole rings are also frequently present in antibacterial [6–8], antifungal [9–13], antiparasitic [14–15], anticancer [16–17] and antiaggregatory [18] preparations.…”

Chemotherapy of Filariasis -On the Search of New Agents Effective on the Reproductive System of Female Adult Worms

“…All the com pounds showed molecular ion peaks at their respective m /z values as given in Table II. The syntheses of l,2-dim ethyl-3-methoxycarbonylpyrroles (17)(18)(19) were carried out [13] by reacting methyl-N-m ethylam inocrotonates with substitut ed nitrostyrenes. All the pyrrole esters exhibited IR absorption at 1720-1750 cm -1 showing the presence of an ester function.…”

“…O ther characteriza tion data are recorded in Table III. 1,3,5-Tricyano-3-phenylpentane (20) was prepared by method reported by K addah and coworkers [14,15] while the representative candidates (21-24) from other heterocycles designed to explore newer avenues in filarial chemotherapy, were prepared by the methods reported by us earlier [16][17][18][19]. The physical constants of com pounds 2 0 -2 4 are recorded in Table IV.…”

An efficient one-pot synthesis and in vitro antimicrobial activity of new pyridine derivatives bearing the tetrazoloquinoline nucleus

“…We wish to report herein this heterocyclic aldehyde which is biologically active [8][9][10] with a view to obtaining more active heterocyclic system containing two biologically active moieties quinoline [11][12][13] and pyridine 14,15 together. The most suitable protocol for the synthesis of functionalized organic compounds would be a one-pot reaction due to the fact that the synthesis can be performed without the Hence, in the present investigation, we report an efficient one-pot multicomponent synthesis of 2-amino-3-cyanopyridine derivatives having tetrazoloquinoline nucleus which have also been recognized as promising new scaffold to endow good biological properties 17,18 such as antiinflammatory and antimicrobial activity.…”