Synthesis and biological evaluation of bicyclic and tricyclic substituted nortropane derivatives: discovery of a novel selective α1D-adrenergic receptor ligand

Microwave Assisted Medicinal Chemistry

“…As part of a program pursuing the development of structurally novel and selective alpha-1 ( 1 )-adrenergic receptor ligands for therapeutic use in cardiovascular diseases, McGinty et al disclosed the potential application of nortropane derivatives as selective 1D -adrenergic ligands [8]. In this report a novel microwave reaction helped in the optimization of the synthesis as desilylation and ketone protection took place in one step, providing a more efficient route to the key cyclic ketal intermediate required for the preparation of target compounds 16-19 (Scheme 4).…”

“…The low level of (8)(9)(10)(11)(12)(13)(14) a Cells were exposed under optimal culture conditions in 96-well plates to four concentrations of the compounds (10, 100, 200, 500 M for the new compounds and 1, 10, 100, 200 for actinomycin D, respectively) or control medium for 20 h before determining cellular metabolic activity by a MTS tetrazolium compound bioreduction assay. The low level of (8)(9)(10)(11)(12)(13)(14) a Cells were exposed under optimal culture conditions in 96-well plates to four concentrations of the compounds (10, 100, 200, 500 M for the new compounds and 1, 10, 100, 200 for actinomycin D, respectively) or control medium for 20 h before determining cellular metabolic activity by a MTS tetrazolium compound bioreduction assay.…”