Epoxyeicosatrienoic acids (EETs) are endothelium-derived eicosanoids that activate potassium channels, hyperpolarize the membrane, and cause relaxation. We tested 19 analogs of 14,15-EET on vascular tone to determine the structural features required for activity. 14,15-EET relaxed bovine coronary arterial rings in a concentration-related manner (ED(50) = 10(-6) M). Changing the carboxyl to an alcohol eliminated dilator activity, whereas 14,15-EET-methyl ester and 14,15-EET-methylsulfonimide retained full activity. Shortening the distance between the carboxyl and epoxy groups reduced the agonist potency and activity. Removal of all three double bonds decreased potency. An analog with a Delta8 double bond had full activity and potency. However, the analogs with only a Delta5 or Delta11 double bond had reduced potency. Conversion of the epoxy oxygen to a sulfur or nitrogen resulted in loss of activity. 14(S),15(R)-EET was more potent than 14(R),15(S)-EET, and 14,15-(cis)-EET was more potent than 14,15-(trans)-EET. These studies indicate that the structural features of 14,15-EET required for relaxation of the bovine coronary artery include a carbon-1 acidic group, a Delta8 double bond, and a 14(S),15(R)-(cis)-epoxy group.
This review accentuates the recent developments in the Wacker oxidation from its conventional form to the more efficient, economical and greener method established in last five years (2015-2020). The Wacker...
A theory of a helical wiggler free-electron laser with ion-channel guiding is presented. Electron motion has been analyzed using single particle dynamics and regimes of orbit stability have been discussed. With the help of these trajectories, source currents have been obtained and the linear dispersion equation showing coupling of electromagnetic and space-charge waves by the wiggler field has been set up for a monoenergetic electron beam. Growth rates have been obtained for different ion-channel frequencies. The variation of resonant frequencies and peak growth rates with ion-channel frequency has been illustrated. Substantial enhancement in peak growth rate is obtained as the ion-channel frequency approaches the wiggler frequency.
The defensive cyclic hydroxamates 7-methoxy-2,4-dihydroxy-1,4(2H)-benzoxazin-3-one (DIMBOA) and 7,8-dimethoxy-2,4-dihydroxy-1,4(2H)-benzoxazin-3-one (DIM2BOA) of wheat and corn are transformed in nonsterile soil, via 6-methoxy-2(3H)-benzoxazolone (MBOA) and 6,7-dimethoxy-2(3H)-benzoxazolone (M2BOA) respectively, into 2-amino-7-methoxy-3H-phenoxazin-3-one and 2-amino-4,6,7-trimethoxy-3H-phenoxazin-3-one. The soil transformation is similar of that undergone by the rye metabolite 2(3H)-benzoxazolone (BOA) into 2-amino-3H-phenoxazin-3-one. The transformations to phenoxazinones are not observed in sterile soil. The 2-amino-3H-phenoxazin-3-one inhibits barnyard grass radicle elongation, but the methoxylated aminophenoxazinones are not significantly inhibitory.
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