Structure−Activity Relationship and Molecular Mechanisms of Ethyl 2-Amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4H-chromene-3-carboxylate (sHA 14-1) and Its Analogues

2009 ◽  
Vol 52 (19) ◽  
pp. 5937-5949 ◽  
Author(s):  
Sonia G. Das ◽  
Jignesh M. Doshi ◽  
Defeng Tian ◽  
Sadiya N. Addo ◽  
Balasubramanian Srinivasan ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity

Structure–Activity Relationship and Molecular Mechanisms of Ethyl 2-Amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and Its Analogues

2011 ◽  
Vol 54 (16) ◽  
pp. 5937-5948 ◽  
Author(s):  
Sonia G. Das ◽  
Balasubramanian Srinivasan ◽  
David L. Hermanson ◽  
Nicholas P. Bleeker ◽  
Jignesh M. Doshi ◽  
...  
Keyword(s):  
Molecular Mechanisms ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity

Research Progress on the Natural Product Aloperine and Its Derivatives

2021 ◽  
Vol 21 ◽  
Author(s):  
Yu Cheng ◽  
Abdur Rauf ◽  
Xiandao Pan
Keyword(s):  
Natural Product ◽  
Recent Progress ◽  
Molecular Mechanisms ◽  
Structure Activity Relationship ◽  
Research Progress ◽  
Activity Relationship ◽  
Pharmacological Effects ◽  
Structure Activity ◽  
Relationship Of

: In this review, an effort towards the presentation of an all-around account of the recent progress on the natural product, aloperine is made, and the antivirus structure-activity relationship of its derivatives is also summarized comprehensively. In addition, the principal pharmacological effects and corresponding molecular mechanisms of aloperine are discussed. Some new modification directions of aloperine are given in the end, which might be brief guidance for further investigations on the natural product aloperine.

scholarly journals A unique small molecule pair controls the plant circadian clock

2020 ◽  
Author(s):  
Takahiro N Uehara ◽  
Saori Takao ◽  
Hiromi Matsuo ◽  
Ami N. Saito ◽  
Eisuke Ota ◽  
...  
Keyword(s):  
Circadian Clock ◽  
Small Molecule ◽  
Molecular Mechanisms ◽  
Response Regulator ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Genetic Redundancy ◽  
Chemical Library ◽  
Structure Activity ◽  
Relationship Study

SummaryCircadian clocks are the biological time keeping systems that coordinate genetic, metabolic, and physiological behaviors with the external day-night cycle. Previous studies have suggested possible molecular mechanisms for the circadian clock in Arabidopsis thaliana (Arabidopsis), but there might be additional mechanisms that have been hidden due to genetic redundancy.A clock reporter line of Arabidopsis was screened against the 10,000 chemicals in the Maybridge Hitfinder10K chemical library, and a structure-activity relationship study of hit compounds was conducted. Clock mutants were treated with two of the small molecules to gain insight into their mode of action.The screening identified 5-(3,4-dichlorophenyl)-1-phenyl-1,7-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4,6(5H)-dione (TU-892) as a period lengthening molecule. From a structure-activity relationship study, we found that a molecule possessing 2,4-dichlorophenyl instead of a 3,4-dichlorophenyl group (TU-923) had period shortening activity. The period shortening activity of TU-923 was reversed to a lengthening activity in double mutants lacking PSEUDO-RESPONSE REGULATOR 9 (PRR9) and PRR7 (prr9-10 prr7-11).Our study provides a unique small molecule pair that regulates the pace of the clock in opposite ways, likely by targeting unknown factors. Small differences at the atomic level can reverse the period tuning activities. PRR9 and PRR7 are essential for the activity of TU-923 in period shortening.

Structure-activity relationship of (-) mammea A/BB derivatives against Leishmania amazonensis

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
MA Brenzan ◽  
CV Nakamura ◽  
BPD Filho ◽  
T Ueda-Nakamura ◽  
MCM Young ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Leishmania Amazonensis ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of
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