17894-25-6Relevant articles and documents
Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
Rahim, Fazal,Malik, Fazal,Ullah, Hayat,Wadood, Abdul,Khan, Fahad,Javid, Muhammad Tariq,Taha, Muhammad,Rehman, Wajid,Ur Rehman, Ashfaq,Khan, Khalid Mohammed
, p. 42 - 48 (2015/05/13)
Isatin base Schiff bases (1-20) were synthesized, characterized by 1H NMR and EI/MS and evaluated for α-glucosidase inhibitory potential. Out of these twenty (20) compounds only six analogs showed potent α-glucosidase inhibitory potential with IC50 value ranging in between 2.2 ± 0.25 and 83.5 ± 1.0 μM when compared with the standard acarbose (IC50 = 840 ± 1.73 μM). Among the series compound 2 having IC50 value (18.3 ± 0.56 μM), 9 (83.5 ± 1.0 μM), 11 (3.3 ± 0.25 μM), 12 (2.2 ± 0.25 μM), 14 (11.8 ± 0.15 μM), and 20 (3.0 ± 0.15 μM) showed excellent inhibitory potential many fold better than the standard acarbose. The binding interactions of these active analogs were confirmed through molecular docking.
PHOSPHODIESTERASE INHIBITORS
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Page/Page column 38, (2009/09/04)
The invention relates to compounds of formula I useful for inhibiting phosphodiesterase-4
Identification of a potent new chemotype for the selective inhibition of PDE4
Skoumbourdis, Amanda P.,Huang, Ruili,Southall, Noel,Leister, William,Guo, Vicky,Cho, Ming-Hsuang,Inglese, James,Nirenberg, Marshall,Austin, Christopher P.,Xia, Menghang,Thomas, Craig J.
, p. 1297 - 1303 (2008/09/20)
A series of substituted 3,6-diphenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines were prepared and analyzed as inhibitors of phosphodiesterase 4 (PDE4). Synthesis, structure-activity relationships, and the selectivity of a highly potent analogue against related phosphodiesterase isoforms are presented.