Compounds containing aryl/heteroaryl acetic acid and aryl/heteroaryl ethylamine cores play important roles in the pharmaceutical field. Compounds containing aryl/heteroaryl acetic acid units form a large group of non-steroidal anti-inflammatory drugs such as Indomethacin [1], Diclophenac [2], Sulindac [3], Ketorolac [4], and many others. Also, this subunit appears in a number of antifungal [5],...

Several 2-(4-chlorophenyl)-N-(4-oxo-2-aryl(l,3,thiazolidin-3-yl))acetamides 2, N-[3-chloro-4-(2-aryl)-2-oxo-azetidinyl]-2-(4-chlorophenyl)acetamides 3, N-(4-oxo-2-aryl(1,3,-thiadiazolidin-3-yl){4-[5-oxo-2-phenyl-4-(phenylmethylene) (2imidazolinyl)phenyl}carboxamides 7 and N-(3-chloro-2-oxo-4-arylazetidinyl){4-[5-oxo-2-phenyl-4-(phenylmethylene)(2imidazolinyl)] phenyl}carboxamides 8 have been sy...

Many directing group containing arenes can now be arylated or alkylated under palladium, rhodium, or ruthenium catalysis.1 Even arenes lacking traditional directing groups can be functionalized representing the most atom-efficient method for creation of arylaryl bonds.2 However, in this case, regioselectivity issues often are unsolved. An exception can be found in recent elegant work by Fagnou ...

Novel direct C-H borylations of 7-deazapurines to position 8 by B2pin2 under Ir catalysis were followed by Suzuki cross-couplings with aryl halides and other functional group transformations to give diverse 8-substituted 7-deazaadenines.

2-Amino-5-(2-aryl-2H-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles 2-4 have been synthesized by the reaction of 2-aryl-2H-1,2,3-triazole-4-carboxylic acids 1 with thiosemicarbazide. Their reaction with phenacyl (p-substituted phenacyl) bromides led to formation of the respective 6-aryl-2-(2-aryl-2H-1,2,3-triazol-4-yl)imidazo[2,1-b]-1,3,4-thiadiazoles 5. Reactivity of the latter fused ring towards reac...

(E)-Methyl-4-aryl-4-oxabut-2-enoate (YH-8) is a novel PKnB protein kinase inhibitor with good anti-tuberculosis activity. To evaluate its pharmacokinetics in rats, a sensitive and selective high performance liquid chromatography-tandem mass spectrometric (LC--MS/MS) method has been developed and validated for the quantification of YH-8 in rat plasma for the first time. Samples were pre-treated ...

Chart 1) were reported to inhibit colon and lung tumors in a patent literature. Subsequently, we found that 3-aryl b-carbolin-1-ones (2) inhibit the proliferation of HeLa cells with IC50 values in the low micromolar range and that the aromatic substitution on C3 in 2 proved to be essential for their biological activity. To broaden the scope of previous studies, aryl-substituted 2-pyridone-conta...

The aryl hydrocarbon receptor (AHR) is a ligand-regulated transcription factor that can be activated by structurally diverse chemicals, ranging from environmental carcinogens to dietary metabolites. Evidence supporting a necessary role for the AHR in normal biology has been established; however, identification of key endogenous ligand/activator remains to be established. Here, we report the abi...

An efficient and greener protocol for the synthesis of 12-aryl-8,9,10,12-tetrahydrobenzo[a]xanthen-11-one using tetradecyltrimethylammonium bromide (TTAB) at room temperature in water is described.