The total syntheses of the Lythracea alkaloids (+)-vertine and (+)-lythrine are described. Enantioenriched pelletierine is used as a chiral building block and engaged into a two step pelletierine condensation leading to two quinolizidin-2-one diastereomers in a 8 : 1 ratio. The major product is used in the synthesis of (+)-vertine via aryl-aryl coupling and ring closing metathesis to provide a ...

Five new 1-hydroxy-2-(1-alkyloxymethyl)-9,10-Anthraquinones (9a-e) have been prepared. Selective nitration of 2-methyl-9,10-anthraquinone, reduction to the corresponding amine, diazotization and treatment by sulfuric acid solution afforded the 1-hydroxy-2-methyl-9,10-anthraquinone in good yield as the key intermediate. Reaction with dimethylsulphate/K2CO3 and subsequen...

Tankyrases-1 and -2 (TNKS-1 and TNKS-2) have three cellular roles which make them important targets in cancer. Using NAD(+) as a substrate, they poly(ADP-ribosyl)ate TRF1 (regulating lengths of telomeres), NuMA (facilitating mitosis) and axin (in wnt/β-catenin signalling). Using molecular modelling and the structure of the weak inhibitor 5-aminoiso quinolin-1-one, 3-aryl-5-substituted-isoquinol...

The aryl-functionalized pyridylamine 2-(i)PrC(6)H(4)N(H)py (1) and bis(2-pyridyl)amines of the type ArN(py)(2) for Ar = Mes (2), 2,6-Et(2)C(6)H(3) (3), 2-(i)PrC(6)H(4) (4), 2,6-(i)Pr(2)C(6)H(3) (5), and 1-naph (6), have been prepared by the palladium-catalyzed cross-coupling of substituted anilines with 2-bromopyridine, and have been characterized by (1)H and (13)C NMR NMR, FTIR, MS, and TGA. C...

synthesis of 4-(n,n- dimethylamino)-3-aryl-3-butene-2-one, ethyl-5-aryl-4-oxo-4h-pyran-2-carboxylate, ethyl-5-aryl-4-pyridones-2-carboxylate and 5-aryl-3-cyano-5-methyl-2-pyridones (aryl=3-thienyl, 2-furyl) are described.

The synthesis and characterisation of axially chiral atropisomeric 1,5-disubstituted 1,2,3-triazoles is reported. Molecules designed to display restricted rotation about 1,2,3-triazole N-1-aryl or C-5-aryl bonds were investigated by physical computational techniques. barrier was found be higher than that for rotation, confirming axial chirality stemming from an bond in a the most suitable devel...

Imidazolones are potent for their intense antimicrobial and mitigating exercises wherein, an assortment of imidazolone analogs 4-aryl-1-(4-chloro-3-fluorophenyl)-2-phenyl-1H-imidazol-5(4H)-ones (2a-o) 4-aryl-2-phenyl-1-(4-(trifluoromethyl) phenyl)-1H-imidazol-5(4H)-ones (3a-o) were studied amalgamating them by using oxazolones various aryl amines. Newly synthesized compounds screened in vitro a...

A series of new 1,2/1,3-bis[o-(N-methylidenamino-3-aryl-5-phenyl-4H-1,2,4-triazole-4-yl)phenoxy]ethane/propane derivatives 4 were prepared in good yields by treatment of 4-amino-3-aryl-5-phenyl-4H-1,2,4-triazoles 2 with certain bis-aldehydes 1.Compounds 4 were reduced with NaBH(4) to afford the corresponding 1,2/1,3-bis[o-(N-methylamino-3-aryl-5-phenyl-4H-1,2,4-triazole-4-yl)phenoxy]ethane/prop...

Several new 2-(2-(4-chlorophenyl)acetyl)-N-arylhydrazinecarbothioamides 1, 5-(4-chlorobenzyl)-4-aryl-4H-1,2,4triazole-3-thiols 2, 5-(4-chlorobenzyl)-N-aryl-1,3,4-thiadiazol-2-amines 3 and 5-(4-chlorobenzyl)-N-aryl-1,3,4-oxadiazol-2amines 4 have been synthesized and screened for their antibacterial activity against gram +ve and gram –ve bacteria i.e S.aureus and E. coli. The QSAR studies of thes...