This article sheds light on the various scaffolds that can be used in the designing and development of novel synthetic compounds to create DPP-4 inhibitors for the treatment of type 2 diabetes mellitus (T2DM). This review highlights a variety of scaffolds with high DPP-4 inhibition activity, such as pyrazolopyrimidine, tetrahydro pyridopyrimidine, uracil-based benzoic acid and esters, triazole-based, fluorophenyl-based, glycinamide, glycolamide, β-carbonyl 1,2,4-triazole, and quinazoline motifs. The article further explains that the potential of the compounds can be increased by substituting atoms such as fluorine, chlorine, and bromine. Docking of existing drugs like sitagliptin, saxagliptin, and vildagliptin was done using Maestro 12.5, and the interaction with specific residues was studied to gain a better understanding of the active sites of DPP-4. The structural activities of the various scaffolds against DPP-4 were further illustrated by their inhibitory concentration (IC50) values. Additionally, various synthesis schemes were developed to make several commercially available DPP4 inhibitors such as vildagliptin, sitagliptin and omarigliptin. In conclusion, the use of halogenated scaffolds for the development of DPP-4 inhibitors is likely to be an area of increasing interest in the future.
The heavy oil belt of North Cambay Basin comprising of Santhal, Lanwa and Balol oil fields poses great problems in floatation of these heavy oils due to high viscosity (10,000–16,000 cps) of the emulsion. Oil-in-water emulsions provide a cost effective alternative to the heated pipelines or diluents for their transportation. Emulsions in different phase ratios and application doses of 2000–5000 ppm of non-ionic surfactants have been found to be effective in phase reversal of emulsions with drastic reduction in viscosities which are in 100–400 cps range at pipeline operating conditions. Non-ionic surfactants have the advantage of relative insensitivity to the salt content of the aqeous phase. The non-ionic family of surfactants has been used successfully for the formation of stable emulsions that resist inversion to a wide operating temperature range. Resulting reverse emulsions are heat sensitive and resolve themselves at elevated temperatures without addition of dehydration chemicals. Suggested surfactant treatment has the potential to successfully transport heavy/viscous emulsions of Lanwa oilfield resulting in tremendous savings in transportation costs.
P. 301
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.