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Exact(12)
Many compounds showed balanced activity on both the receptors but compound (22) was found to be the most active derivative having higher antagonistic activity on both the receptors.
The most active derivative, 45 demonstrated potent anticonvulsant activity in MES test at the dose of 30 mg/kg (0.5 h) and 100 mg/kg (4 h) and also delivered excellent protection in sc-PTZ test (100 mg/kg) at both time intervals.
However, compound 3b, the most active derivative was subjected to mechanistic studies to understand the underlying mechanism.
Some compounds exhibited better anti-cancer activity against HCT116 compared to positive controls, such as 5-fluorouracil and Albiziabioside A. Compound 8n was the most active derivative.
The target compound 7d was the most active derivative behaving as a pure NPSR antagonist and displaying IC50 value of 2 μM.
Compound 2b bearing a hydrophobic aromatic tie was the most active derivative against all bacteria studied with MIC values ranging from 0.098 to 0.78 μg/mL.
Similar(48)
Compounds 4b and 9b were the most active derivatives, and their activities were 5-fold higher than chloroquine.
Compounds 12a, 12d, and 28 are the most active derivatives in this series, displaying activity comparable to that of retapamulin and BC-3781.
The compounds were evaluated for their in vivo antimalarial activity against Plasmodium berghei infected mice and the most active derivatives were further examined for their in vitro antimalarial activity against chloroquine resistant (RKL9) strain of Plasmodium falciparum.
Structures of the most active derivatives are determined by NMR spectroscopy and X-ray crystallography.
The most active derivatives with substituent R2 = Cl or CH3 at the benzenesulfonamide moiety exhibited the lowest IC50.
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CEO of Professional Science Editing for Scientists @ prosciediting.com