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

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.

scholarly journals Bicyclic Basic Merbarone Analogues as Antiproliferative Agents

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 557
Author(s):  
Andrea Spallarossa ◽  
Matteo Lusardi ◽  
Chiara Caneva ◽  
Aldo Profumo ◽  
Camillo Rosano ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Side Chain ◽  
The Novel ◽  
Bioactive Conformation ◽  
Pyrimidine Derivatives ◽  
Topoisomerase Iiα ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Step Procedure ◽  
Pyrimidine Moiety

Pyrimido-pyrimidine derivatives have been developed as rigid merbarone analogues. In a previous study, these compounds showed potent antiproliferative activity and efficiently inhibited topoisomerase IIα. To further extend the structure–activity relationships on pyrimido-pyrimidines, a novel series of analogues was synthesized by a two-step procedure. Analogues 3–6 bear small alky groups at positions 1 and 3 of the pyrimido-pyrimidine scaffold whereas at position 6a (4-chloro)phenyl substituent was inserted. The basic side chains introduced at position 7 were selected on the basis of the previously developed structure–activity relationships. The antiproliferative activity of the novel compounds proved to be affected by both the nature of the basic side chain and the substituents on the pyrimido-pyrimidine moiety. Derivatives 5d and 5e were identified as the most promising molecules still showing reduced antiproliferative activity in comparison with the previously prepared pyrimido-pyrimidine analogues. In topoisomerase IIα-5d docking complex, the ligand would poorly interact with the enzyme and assume a different orientation in comparison with 1d bioactive conformation.

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

Synthesis and Structure-Activity Relationships of the Novel Homopropargylamine Antimycotics

1994 ◽  
Vol 37 (5) ◽  
pp. 610-615 ◽  
Author(s):  
Peter Nussbaumer ◽  
Ingrid Leitner ◽  
Anton Stuetz
Keyword(s):  
The Novel ◽  
Structure Activity Relationships ◽  
Structure Activity
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