a b s t r a c tThe design and synthesis of a small library of pyrrolidine iminocyclitol inhibitors with a structural similarity to 1,4-dideoxy-1,4-imino-D-arabitol (DAB-1) is reported. This library was specifically designed to gain a better insight into the mechanism of inhibition of glycosidases by polyhydroxylated pyrrolidines or iminocyclitols. Pyrrolidine-3,4-diol 15a and pyrrolidine-3,4-diol diacetate 15b had emerged as the most potent a-glucosidase inhibitors in the series. Docking studies performed with an homology model of a-glucosidase disclosed binding poses for compounds 15a, 15b, 16a, and 16a 0 occupying the same region as the NH group of the terminal ring of acarbose and suggest a closer and stronger binding of compound 15a and 15b with the enzyme active site residues. Our studies indicate that 2 or 5-hydroxyl substituents appear to be vital for high inhibitory activity.
Based on the positive bioassay results of the known oxindole hit compound rac‐1‐benzyl‐3‐hydroxy‐3‐phenylindolin‐2‐one which showed significant inhibition of butyrylcholinesterase (BuChE) (IC50=7.41 μM), a library of 31 analogues of 3‐substituted‐3‐hydroxyoxindoles was synthesized and screened for both acetylcholinesterase (AChE) and BuChE activity. Our bioassays revealed that some of the new compounds exhibited moderate inhibition of eel AChE (EeAChE) and very good inhibition of equine serum BuChE (EqBuChE) with a best IC50 of 1.02 μM. On the basis of these results, the lead compound 1‐((1‐benzylpiperidin‐4‐yl)methyl)‐3‐hydroxy‐3‐phenylindolin‐2‐one was designed, which was shown to interact well with the enzymes active sites by molecular docking, was synthesized and upon bioassay gave an IC50 of 6.61 μM for BuChE. Interestingly, when we separated rac‐benzyl‐3‐hydroxy‐3‐phenylindolin‐2‐one into the individual enantiomers (R)‐ and (S)‐benzyl‐3‐hydroxy‐3‐phenylindolin‐2‐one it was the latter enantiomer that gave the best IC50 of 6.19 μM for BuChE.
This paper analyses the economic viability of a power production hybrid system (Photovoltaic -Wind -Fuel) for domestic supply in isolated areas.A correctly designed photovoltaic-wind-diesel hybrid system enlarges considerably both the diesel generator lifecycle as well as the batteries lifecycle, when referring to the most common used technology (off-grid generator systems). Both benefits need to be correctly accounted in the evaluation process, as maintenance costs are reduced significantly in the case of a PVwind-Diesel solution.This paper aims to develop a new method to evaluate the design of a PV-Wind-Diesel Hybrid System for electricity production. The different types of renewable sources are specifically evaluated in the economical performance of the overall equipment. The developed methodology bases the investment decision on the standard Net Present Value analysis, with sound capital cost evaluation.
This paper aims to develop a new method for the economical evaluation of Hybrid Systems for electricity production. The different types of renewable sources are specifically evaluated in the economical performance of the overall equipment. The presented methodology was applied to evaluate the design of a photovoltaic-wind-diesel hybrid system to produce electricity for a community in the neighbourhood of Luanda, Angola.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.