61946-89-2Relevant articles and documents
Dibenzazepine-linked isoxazoles: New and potent class of α-glucosidase inhibitors
Umm-E-Farwa,Ullah, Saeed,Khan, Maria Aqeel,Zafar, Humaira,Atia-tul-Wahab,Younus, Munisaa,Choudhary, M. Iqbal,Basha, Fatima Z.
, (2021/05/10)
α-Glucosidase inhibition is a valid approach for controlling hyperglycemia in diabetes. In the current study, new molecules as a hybrid of isoxazole and dibenzazepine scaffolds were designed, based on their literature as antidiabetic agents. For this, a series of dibenzazepine-linked isoxazoles (33–54) was prepared using Nitrile oxide-Alkyne cycloaddition (NOAC) reaction, and evaluated for their α-glucosidase inhibitory activities to explore new hits for treatment of diabetes. Most of the compounds showed potent inhibitory potency against α-glucosidase (EC 3.2.1.20) enzyme (IC50 = 35.62 ± 1.48 to 333.30 ± 1.67 μM) using acarbose as a reference drug (IC50 = 875.75 ± 2.08 μM). Structure-activity relationship, kinetics and molecular docking studies of active isoxazoles were also determined to study enzyme-inhibitor interactions. Compounds 33, 40, 41, 46, 48–50, and 54 showed binding interactions with critical amino acid residues of α-glucosidase enzyme, such as Lys156, Ser157, Asp242, and Gln353.
N -Oxide-Controlled Chemoselective Reduction of Nitrofuroxans
Fershtat, Leonid L.,Bystrov, Dmitry M.,Zhilin, Egor S.,Makhova, Nina N.
, p. 747 - 756 (2019/01/23)
A facile and chemoselective SnCl 2 -mediated mild reduction of regioisomeric 3- and 4-nitrofuroxans for the synthesis of aminofurazans and aminofuroxans in good yields is developed. Reduction of 4-nitrofuroxans results in the selective formation of 4-aminofuroxans, while analogous reduction of 3-nitrofuroxans affords 3-aminofurazans as a result of simultaneous reduction of the nitro group and exocyclic N-O bond.
N-(sulfonyloxy) benzimidoyl halides as bactericidal or fungicidal agents
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, (2008/06/13)
Agricultural fungicidal compositions based on N-(sulfonyloxy)benzimidoyl halides exhibit a broad spectrum of antifungal activity, particularly against late blight, bean rust and rice blast. The synthesis of representative compounds is described, and the utility of antifungal compositions is exemplified.