Canavalia ensiformis native starch was succinylated and the functional properties of the succinylated starch evaluated. Reaction conditions investigated included: pH (8.0-8.5 and 9.0-9.5), succinic anhydride concentration (3 and 4%), temperature (20 and 30 °C) and reaction time (1 and 3 h). When starch was succinylated with 4% succinic anhydride, at pH 8.0-8.5, at 30 °C for 1 h, 1.58% succinylation was obtained. Compared to native Canavalia starch, these succinylated products exhibited increasing paste and gel clarity, solubility (36%), swelling power (46.2 g water/g starch), and viscosity (86.5 mPas). Gelatinization temperature range was reduced to 67-73 °C and retrogradation was eliminated. The use of succinylated Canavalia starches as thickening and stabilizing agents in ice creams, fruit jellies, baked products, sauces and frozen foods is suggested.
S i n c e s eve ra l ye a r s a g o, d i ve r s e corticosteroid derivatives have been development; for example, the synthesis 3α-acetoxy-16α
Aim. The present study was designed to investigate the activity of two glibenclamide derivatives on glucose concentration. An additional aim was to identify the biodistribution of glibenclamide derivatives in different organs in a diabetic animal model. Methods. The effects of two glibenclamide derivatives on glucose concentration were evaluated in a diabetic animal model. In addition, glibenclamide derivatives were bound to Tc-99m using radioimmunoassay methods. To evaluate the pharmacokinetics of the glibenclamide derivatives over time (15, 30, 45 and 60 min) the Tc-99m-glibenclamide conjugates were used. Results. The results showed that glibenclamide-pregnenolone had greater hypoglycemic activity than glibenclamide or glibenclamide-OH. The data also showed that the biodistribution of Tc-99m-glibenclamide-OH in all organs was less than that of the Tc-99m-glibenclamide-pregnenolone derivative. Conclusions. The glibenclamide-pregnenolone derivative had greater hypoglycemic effects and its biodistribution was wider than glibenclamide-OH. The data suggest that the steroid nucleus may be important to the hypoglycemic activity of the glibenclamide-pregnenolone derivative and this could be related to the degree of lipophilicity induced by the steroid nucleus in the chemical structure of glibenclamide-pregnenolone.
Two danazol derivatives were synthesized and characterized by spectral analyses. In order to characterize the structural and chemical requirements of danazol derivatives, several parameters such aslogP, π, Rmand Vmwere evaluated. The results showed an increase in the values oflogPfor the compound 6 in comparison with 3. The compound 3 showed an increase in the values of π, R Vmand V Vmwith respect to 6. These data indicate a high degree of lipophilicity and a low steric impediment for compound 6 in comparison with 3.
There are studies which show that several derivatives of brucine have been developed for its use in different biological and analytical methods 1-4. For example, a report shows the synthesis of N-chloromethylbrucine chloride by the reaction of brucine with dichloromethane 5. Other studies have shown the preparation of a brucine derivative (brucidine) by electrolytic reduction of brucine 6. In addition, there are reports of the synthesis of N-(5-carboxypentyl)brucinium bromide via N-alkylation of brucine with 6-bromohexanoic acid 7. Other experimental data showed the preparation of compounds brucinium hydrogen (S)-malate pentahydrate and anhydrous brucinium hydrogen (2R,3R)-tartrate by the reaction between brucine and D-L-malic acid or L-tartaric acid in ethanol:water 8. Additionally, the porphyrin-brucine conjugates was synthetized by the N-alkylation of brucine with alkylbromotetraphenylporphyrin derivatives 9. Recently, a brucine derivative (N 1-(2,3-dimethoxy strychnidin-10-yliden)-ethane-1,2-diamine) was synthetized by the reaction of brucine and ethylenediamine using boric acid as catalyst. Also other brucine derivative (11-[(2-aminoethylamino)-methyl]-2,3-dimethoxystrychnidin-10-ona) was prepared by the reaction of brucine with ethylenediamine in presence of formaldehyde 10. Additionally, other study showed the synthesis of a brucine-dihydropirymidine derivative using the multi-component system (brucine, benzaldehyde and
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