Studies on the Novel α-Glucosidase Inhibitory Activity and Structure—Activity Relationships for Andrographolide Analogues.

ChemInform ◽  
2006 ◽  
Vol 37 (33) ◽  
Author(s):  
Gui-Fu Dai ◽  
Hai-Wei Xu ◽  
Jun-Feng Wang ◽  
Feng-Wu Liu ◽  
Hong-Min Liu
Keyword(s):  
Inhibitory Activity ◽  
The Novel ◽  
Structure Activity Relationships ◽  
Structure Activity

scholarly journals Synthesis and structure-activity relationships of the novel isothiobarbamine analogues with lowered basicity

2020 ◽  
Author(s):  
I. A. Novakov ◽  
L. L. Brunilina ◽  
V. V. Chapurkin ◽  
M. B. Nawrozkij ◽  
D. S. Sheikin ◽  
...  
Keyword(s):  
The Novel ◽  
Structure Activity Relationships ◽  
Structure Activity

ChemInform Abstract: Structure-Activity Relationships of Biflavonoids for β-Secretase (BACE-1) Inhibitory Activity.

ChemInform ◽  
2013 ◽  
Vol 44 (11) ◽  
pp. no-no
Author(s):  
Hiroaki Sasaki ◽  
Yuki Kitoh ◽  
Kazuhiko Miki ◽  
Kaoru Kinoshita ◽  
Kiyotaka Koyama ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Abstract Structure ◽  
Bace 1

Structure-activity relationships in the Hill inhibitory activity of substituted phenylureas

1987 ◽  
Vol 35 (4) ◽  
pp. 479-483 ◽  
Author(s):  
Patrick Camilleri ◽  
John R. Bowyer ◽  
Terence Gilkerson ◽  
Barbara Odell ◽  
Roger C. Weaver
Keyword(s):  
Inhibitory Activity ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
The Hill

scholarly journals Characterization of platinum(II) complexes exhibiting inhibitory activity against the 20S proteasome

2020 ◽  
Vol 7 (8) ◽  
pp. 200545
Author(s):  
Tatsuto Kiwada ◽  
Hiromu Katakasu ◽  
Serina Okumura ◽  
Akira Odani
Keyword(s):  
Inhibitory Activity ◽  
Chemical Structure ◽  
Competitive Inhibition ◽  
Proteasome Inhibitors ◽  
Platinum Complex ◽  
Platinum Complexes ◽  
Binding Mode ◽  
Structure Activity Relationships ◽  
Structure Activity

Proteasome inhibitors are useful for biochemical research and clinical treatment. In our previous study, we reported that the 4N-coordinated platinum complexes with anthracenyl ring and heterocycle exhibited proteasome-inhibitory activity. In the present study, the structure–activity relationships and characterization of these complexes were determined for the elucidation of the role of aromatic ligands. Lineweaver–Burk analysis revealed that the chemical structure of heterocycles affects the binding mode of platinum complexes. Platinum complexes with anthracenyl ring and pyridine showed competitive inhibition, although platinum complexes with anthracenyl ring and phenanthroline showed non-competitive inhibition. The structure–activity relationships demonstrated that anthracenyl moiety plays a crucial role in proteasome-inhibitory activity. The platinum complexes with naphthyl or phenyl rings exhibited lower inhibitory activities than the platinum complex with anthracenyl ring. The reactivity with N-acetylcysteine varied according to the chemical structure of complexes.

scholarly journals UFLC-MS-IT-TOF and Bioassay Guided Isolation of Flavonoids as Xanthine Oxidase Inhibitors from Diospyros dumetorum

2017 ◽  
Vol 12 (11) ◽  
pp. 1934578X1701201
Author(s):  
Zhen-Tao Deng ◽  
Tong-Hua Yang ◽  
Xiao-Yan Huang ◽  
Xing-Long Chen ◽  
Jian-Gang Zhang ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Folk Medicine ◽  
Hydroxyl Groups ◽  
Active Constituents ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Pulmonary Abscess ◽  
Xanthine Oxidase Inhibitors

Diospyros dumetorum is an important folk medicine for treating pulmonary abscess and inflammation. The leaves of D. dumetorum revealed xanthine oxidase (XOD) inhibitory activity. With the guidance of UFLC-MS-IT-TOF analyses combined with bioassay in vitro, 15 flavonoids were isolated from the active parts of D. dumetorum. Except for 11 (IC50 > 200μM), all compounds showed obvious XOD inhibitory activity with IC50 values of 32.5 ± 0.7 ~ 145.0 ± 3.3 μM. The preliminary structure-activity relationships study suggested that glycosylation on C-3 was unfavorable for XOD inhibitory activity; hydroxyl groups on ring B were essential for maintaining activity; the activity was closely related with the position of galloylation. This is the first recognition of the XOD inhibitory activity and active constituents of D. dumetorum, and will provide valuable information for this plant as a new resource for treating hyperuricemia and gout.

scholarly journals The Discovery of Novel Selective D1 Dopaminergic Agonists: A-68930, A-77636, A-86929, and ABT-413

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Yvonne Connolly Martin
Keyword(s):  
Medicinal Chemistry ◽  
Partial Agonist ◽  
Skf 38393 ◽  
The Novel ◽  
Bioactive Conformation ◽  
Dopaminergic Agonists ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
A 68930

The novel selective D1 dopaminergic full agonists A-68930, A-77636 were discovered by the synthesis of molecules to probe the bioactive conformation of the partial agonist SKF-38393, by the use of this information to add D1 affinity and selectivity to a screening hit, and by traditional medicinal chemistry exploration of structure-activity relationships. The subsequent design of A-86929 and ABT-413 capitalized on these results, recently disclosed agonists, and traditional medicinal chemistry.

Structure-Activity Relationships of Biflavonoids for β-Secretase (BACE-1) Inhibitory Activity

Heterocycles ◽  
2012 ◽  
Vol 85 (11) ◽  
pp. 2749 ◽  
Author(s):  
Kunio Takahashi ◽  
Hiroaki Sasaki ◽  
Yuki Kitoh ◽  
Kazuhiko Miki ◽  
Kaoru Kinoshita ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Bace 1
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