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A series of prenylated flavones ( 1 – 8 ) were isolated and evaluated for their BACE-1 inhibitory activities. The inhibition and structural reliability of these analogs are described.
The exploration of heterocyclic carboxamidines as iNOS inhibitors led to the identification of (2 R )-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.
A new unusual sterol, named lobophytosterol ( 1 ), and five known metabolites ( 2 – 6 ) were isolated from the methanol extract of the soft coral Lobophytum laevigatum . Compounds 1 – 3 showed cytotoxic activity against selected human cancer cell lines. Treatment of these cells with compound...
We report the design of novel, potent cPLA 2 α inhibitors that possess an α-methyl-2-ketothiazole that acts as a serine-reactive moiety. We describe the optimization of the series for potency and metabolic stability towards ketone reduction. This was achieved by attenuating the reactivity of...
Two new monoterpene glycosides, distyloside A–B ( 1 – 2 ), and a new megastigmane glucoside, iso -dihydrodendranthemoside A ( 3 ) were isolated from twigs and leaves of Distylium racemosum Siebold & Zucc. (Hamamelidaceae).
Described herein is the initial optimization of the screening hit (+/−) N -benzyl-4-heteroaryl-1-(phenylsulfonyl)-piperazine-2-carboxamide ( 1 ) that led to the discovery of the potent NS5B inhibitor ( S )- N - sec -butyl-6-(( R...
Solamargine has been synthesized in 13 steps and 10.5% overall yield from the natural abundant diosgenin.
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