Over expression of nucleotide pyrophosphatase (NPPs) activity is associated with chondrocalcinosis, osteoarthritis, type 2 diabetes, neurodegenerative diseases, allergies and cancer metastasis.
Benzothiazoloquinazolines are known to possess several interesting biological properties. Various arylated benzothiazoloquinazolines were synthesized from readily available 2‐bromo‐12H‐benzothiazolo[2,3‐b]quinazolin‐12‐one by palladium catalysed Suzuki‐Miyaura reactions in 43 – 85% yield. Synthesized derivatives were analysed regarding their in vitro inhibition activity towards monoamine oxidases A and B and showed significant inhibitory values in the micromolar range. Molecular modelling as well as PAINS studies on the binding interaction of most potent inhibitors with both isoforms were studied to verify the experimental results.
Abstract. Electrochemical properties of intergel system polyacrylic acid (gPAA) and poly-4-vinylpyridine hydrogels (gP4VP) and conformational properties of initial hydrogels were studied depending on hydrogels initial state. Maximum activation area is: for dry hydrogelsgPAA:gP4VP ratios 5:1 and 1:5, for swollen -ratios 5:1, 2:4 and 1:5.
Abstract.1 Sorption ability of intergel system polymethacrylic acid hydrogel (gPMAA) -poly-4-vinylpyridine hydrogel (gP4VP) in relation to lanthanum ions is studied. Hydrogels mutual activation in an aqueous medium, particularly dependencies of swelling coefficient, specific electric conductivity and pH of water solutions are studied. Maximum activation of hydrogels occurs at gPMAA:gP4VP molar ratio 3:3. Maximum total binding degree of polymer chain in the intergel system is observed at the ratio gPMAA:gP4VP = 1:5. It has the value of 73.13 %, which is much higher than at initial hydrogels: gPMAA binding degree is 55.17 %, gP4VP -55.00 %. The obtained results point to the fact that at this ratio there are significant changes of electrochemical, conformational and sorption degrees of initial macromolecules in intergel system.
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