Design, synthesis and in vitro evaluation of benzothiazole-based ureas as potential ABAD/17β-HSD10 modulators for Alzheimer’s disease treatment

In Vitro Assay Development and HTS of Small-Molecule Human ABAD/17β-HSD10 Inhibitors as Therapeutics in Alzheimer’s Disease

“…Previously determined conditions 10 were used with a fixed concentration of 700 µM NADH and a starting concentration of up to 200 µM acetoacetyl-CoA.…”

6-Benzothiazolyl Ureas, Thioureas and Guanidines are Potent Inhibitors of ABAD/17β-HSD10 and Potential Drugs for Alzheimer"s Disease Treatment: Design, Synthesis and in vitro Evaluation

“…3). The ability of the synthesised compounds to modulate ABAD/17β-HSD10 activity was assessed by a spectrophotometric assay that was formerly outlined by Hroch et al [24]. An initial compound screen was performed using each compound at 100 μM concentration.…”

Synthesis and evaluation of frentizole-based indolyl thiourea analogues as MAO/ABAD inhibitors for Alzheimer’s disease treatment

“…On the other hand, the introduction of a second phenyl ring connected via an ether (9) or a carbonyl moiety (12) Additionally, a second chlorine present in the C-5 position (21) further increased the inhibitory effect, which is in agreement with recently reported findings. 41 Functional groups other than chlorine (20 and 23) were not beneficial. Comparing the discussed compounds with the previously published urea/thiourea/phosphonate series, it shows that the inhibition ability doesn't vary significantly with the linker changes.…”

“…In this case, the introduction of indole moiety seems to be rather unfavourable for ABAD inhibitory ability if compared to previously used benzothiazoles. [38][39][40][41] This fact might be related to either its flipped position and/or missing substitution of the indolyl scaffold, which will be the matter of further investigation.…”

“…39,40 Recently, low micromolar scale ABAD inhibitors were reported. 41 Furthermore, a fused bicyclic system comprised of 5-and 6-membered rings (i.e. indane) represents core scaffold of several MAO inhibitors (e.g.…”