2-Substituted 7-trifluoromethyl-thiadiazolopyrimidones as alkaline phosphatase inhibitors. Synthesis, structure activity relationship and molecular docking study
“…These ndings provide new insight into the development of 2-substituted 7-triuoromethylthiadiazolopyrimidones as potential inhibitors of AP for therapeutic applications. 152 Langer et al (2018) reported the synthesis of new pyrazolopyridines and benzofuropyridines through a domino reaction of 3-chlorochromones with aminoheterocycles and demonstrated their inhibitory activity against ecto-5 ′ -nucleotidase, making them potential lead compounds for further drug development. The pyrazolo [3,4-b]pyridines showed intriguing results in their interaction with h-e5 ′ NT.…”
“…These findings provide new insight into the development of 2-substituted 7-trifluoromethyl-thiadiazolopyrimidones as potential inhibitors of AP for therapeutic applications. 152 …”
Heterocycles, powerful inhibitors of alkaline phosphatase (AP), are compounds that hinder an enzyme crucial for vital physiological functions including bone metabolism, cell growth, and differentiation.
“…These ndings provide new insight into the development of 2-substituted 7-triuoromethylthiadiazolopyrimidones as potential inhibitors of AP for therapeutic applications. 152 Langer et al (2018) reported the synthesis of new pyrazolopyridines and benzofuropyridines through a domino reaction of 3-chlorochromones with aminoheterocycles and demonstrated their inhibitory activity against ecto-5 ′ -nucleotidase, making them potential lead compounds for further drug development. The pyrazolo [3,4-b]pyridines showed intriguing results in their interaction with h-e5 ′ NT.…”
“…These findings provide new insight into the development of 2-substituted 7-trifluoromethyl-thiadiazolopyrimidones as potential inhibitors of AP for therapeutic applications. 152 …”
Heterocycles, powerful inhibitors of alkaline phosphatase (AP), are compounds that hinder an enzyme crucial for vital physiological functions including bone metabolism, cell growth, and differentiation.
Alkaline phosphatases are found in different living species and play crucial roles in various significant functions, such as hydrolyzing a variable spectrum of phosphatecontaining physiological compounds, contributing to DNA synthesis, bone calcification, and attenuation of inflammation. They are homodimeric enzymes; each subunit contains one magnesium ion and two zinc ions crucial for the catalytic activity of the enzyme. Alkaline phosphatases exist in four distinct isoenzymes (placental, intestinal, germ cell, and tissue nonspecific alkaline phosphatases), which are expressed by four different genes; each one of them has distinguished functions. Any disturbance in the gene expression of alkaline phosphatase eventually induces serious disease conditions. Thus, the need to explore new lead inhibitors has increased recently. In this literature review, we aim to investigate the role of alkaline phosphatase in different diseases and physiological conditions and to study the structure-activity relationships of recently reported inhibitors. We focused on the lead compounds reported in the last 5 years (between 2015 and 2019). K E Y W O R D S alkaline phosphatase, inhibitors, isoenzymes, structure-activity relationship
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.
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