Please use this identifier to cite or link to this item: https://scholarbank.nus.edu.sg/handle/10635/106210
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dc.titlePharmacological activity and structure-activity relationship of (±)- erythro-mefloquine and related compounds on the isolated mouse phrenic nerve diaphragm preparation
dc.contributor.authorGo, M.-L.
dc.contributor.authorLee, H.-S.
dc.contributor.authorNgiam, T.-L.
dc.date.accessioned2014-10-29T01:56:44Z
dc.date.available2014-10-29T01:56:44Z
dc.date.issued1993
dc.identifier.citationGo, M.-L.,Lee, H.-S.,Ngiam, T.-L. (1993). Pharmacological activity and structure-activity relationship of (±)- erythro-mefloquine and related compounds on the isolated mouse phrenic nerve diaphragm preparation. Biological and Pharmaceutical Bulletin 16 (7) : 668-674. ScholarBank@NUS Repository.
dc.identifier.issn09186158
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/106210
dc.description.abstractThe effects of the antimalarial agent, (±)-erythro-mefloquine and related compounds [(±)-threo-mefloquine, (±)-erythro-N-methylmelloquine and its N- oxide, quinine, WR 184806 and halofanthrine] on the isolated mouse phrenic nerve diaphragm preparation were investigated. Based on their pharmacological effects, these compounds may be divided into two groups. The group I compounds, comprising (±)-erythro-mefloquine, (±)-threo-mefloquine and WR 184806, were found to exert a contractile effect on the muscle and also to inhibit the indirectly (nerve) stimulated and directly (muscle) stimulated (after α-bungarotoxin) twitch responses. The group II compounds, comprising the other compounds except halofanthrine, lacked a contractile effect on muscle but potentiated the directly stimulated twitch responses (after α- bungarotoxin). Halofanthrine did not elicit any response from the preparation. The minimum energy conformations of these compounds were determined using an interactive molecular modelling program which incorporates MMX force field for molecular mechanics calculations. Conformational analyses of the erythro and threo isomers of mefloquine hydrochloride were also undertaken using 1H-NMR. The 1H-NMR data supported the proposal made on the basis of MMX calculations that the erythro isomer exists in solution as one predominant conformer whereas the threo isomer is present in solution as a mixed population of two stable conformers. The structure-activity relationship of the compounds is discussed.
dc.sourceScopus
dc.typeArticle
dc.contributor.departmentPHARMACY
dc.description.sourcetitleBiological and Pharmaceutical Bulletin
dc.description.volume16
dc.description.issue7
dc.description.page668-674
dc.description.codenBPBLE
dc.identifier.isiutNOT_IN_WOS
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