The de novo design of molecules from scratch with tailored biological activity is still the major intellectual challenge in chemical biology and drug discovery. Herein we validate natural-product-derived fragments (NPDFs) as excellent molecular seeds for the targeted de novo discovery of lead structures for the modulation of therapeutically relevant proteins. The application of this de novo app...

Some novel 2,3-dioxo-5-(substituted)-arylpyrroles have been synthesized. Among these, pyrrolidine compound 1b was converted to 2,3-dioxo-5-aryl pyrrolidine 2b. Finally a set of hydrazone derivatives was obtained from the reaction of 2b with various hydrazine salts. The structures of all the new synthesized compounds were confirmed by elemental analyses, IR and 1H-NMR spectra.

The adducts produced in the reaction between trialkyl phosphites and acetylenic esters were trapped by hydantoins to produce highly functionalized dialkyl 2-(2,5-dioxo-4,4-diphenylimidazolidin-1-yl) succinate in good yields.

the adducts produced in the reaction between trialkyl phosphites and acetylenic esters were trapped by hydantoins to produce highly functionalized dialkyl 2-(2,5-dioxo-4,4-diphenylimidazolidin-1-yl) succinate in good yields.

an efficient synthesis of 1, 8-dioxo-octahydroxanthens and 1, 8-dioxo-decahydroacridines from the reaction of 5,5-dimethyl-1,3-cyclohexanedione (dimedone) with aromatic aldehydes bearing electron-donating or withdrawing substituents either in the presence or absence of primary amines has been described in a single pot using a catalytic amounts of aluminum tris (dodecyl sulfate) trihydrate [al(d...

Abstract Monofluorinated bis-heterocyclic spirocycles: functionalized ethyl 9-fluoro-8-methyl-1,4-dioxo-2,3,6,10-tetraphenyl-2,3,7-triazaspiro[4.5]dec-7-ene-9-carboxylate derivatives were efficiently synthesized from readily available 1,2-diphenylpyrazolidine-3,5-dione, 2-fluoroacetoacetate, aromatic aldehydes, and ammonium acetate via one-pot four-component reactions in the absence of addition...