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In this article, arylsulfonamides have been highlighted as potential and selective MMP-2 inhibitors through structure-activity relationships study.
The quantitative structure property relationships study of 40 benzoxazines, that seem to be very promising antimycobacterial drugs, allowed proposing and testing of the equations describing effects of substituents on half-wave potentials of these compounds.
Structure activity relationships study showed that monosaccharide substituents, such as glucose, were not necessary and the presence of 4-hydroxy-3,5-dimethoxyphenyl moiety was crucial for inhibitory activity.
Design, synthesis and structure activity relationships study of the HTS-derived hit led to the identification of 5-chloro-2- 3,5-dimethylphenyl -4- 4-methoxyphenoxy pyridazin-3(2H)-one lead molecule with submicromolar antagonist activity at the target receptor and high selectivity against a panel of therapeutically relevant off-target proteins.
The structure-activity relationships study of piperidinylethoxy series demonstrated that the selectivity and physicochemical properties of compounds could be optimized by selection of a proper substituent on the C-7 position of chroman ring, while the high potency of the molecule against AChE was reserved.
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The TMACC interpretation can provide new insight into the structure-activity relationships studied.
Compound 13a shows moderate dual activities and is a promising lead compound for further structure activity relationships studies.
Structure activity relationships studies show that the platinum complex moiety is essential for an optimal cytocidal activity.
This information could help to better understand the relationships studied.
Further structure-function relationships studies must be carried out to verify this hypothesis.
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