A series of helicid analogues were prepared and evaluated in vitro for the cholinesterase (AChE and BuChE) inhibitory activities via UV spectroscopy. The results indicated that compounds 5, 6d and 8 exhibited potent A...

Eight novel heterocyclic Schiff bases derived from the condensation reactions of indole 3-carboxaldehyde with different L-amino acids (histidine, glutamic acid, aspartic acid, leucine, valine) as well as with some ami...

The synthesis and evaluation of 2,5-bis[4-(N-ethoxycarbonyl-N'-isopropyl)amidinophenyl]furan, 2,5-bis[4-(N-2,2,2-trichloroethoxycarbonyl-N'-isopropyl)amidinophenyl]furan and 2,5-bis[4-(N-cyclopentyl-N'-2,2,2-trichloro...

Complexes of cerium(III) with bis(4-hydroxy-2-oxo-2H-chromen-3-yl)-pyridin-2-yl-methane, bis(4-hydroxy-2-oxo-2H-chromen-3-yl)pyridin-3-yl-methane and bis(4-hydroxy-2-oxo-2H-chromen-3-yl)-pyridin-4-yl-methane were synt...

Several diamino quinoxalines were designed, synthesized and evaluated as anti-tumor agents. Two compounds showed the most potent cytotoxic activities against the leukemia CCRF-CEM cell line (GI(50) < 0-01 mu M) and...

3D-QSAR analysis of a set of 37 analogues of SCH 66336 (Sarasar) was performed by most widely used computational tool, molecular field analysis (MFA) to investigate the substitutional requirements for the favorable re...

Monogalactosyl diglycerides. with medium to long fatty acid acyl chains, were prepared and examined for antimicrobial activity against Gram positive, Gram negative bacteria and fungi. The study of their in vitro antim...

A series of 3,5-bis(benzylidene)piperidin-4-ones 1, 1-acryloyl-3,5-bis(benzylidene)piperidin-4-ones 2 and adducts of 2 with sodium 2-mercaptoethanesulfonate (mesna), namely series 3, were prepared as candidate cytotox...

Developing novel anti-inflammatory drugs is increasingly important in modern pharmaceutical industry. In this work, the reactions of both amino acids and their methylesters with 3-(5,5-dimethyl-1,3-dioxane-2-yl)propan...

A series of 2,4-dichloro-5-fluorophenyl containing 1,3,4-oxadiazoles (10 and 11) were synthesized by POCl3 cyclization of 2,4-dichloro-5-fluorobenzoyl hydrazide (4) and 2-(2,4-dichloro-5-fluorophenyl)cinchoninyl hydra...

A series of new pseudopeptidic macrolides 2a-f based on an amino alcohol were synthesized and evaluated for in vitro antibacterial and antifungal activities. The structure-activity relationships of these compounds wer...

The naphthylisoquinoline alkaloids (NIQs) represent a class of natural products with manifold activities against various tropical diseases. They are isolated from rare and difficult-to-cultivate tropical plants. In or...

Classification models of estrogen receptor-beta ligands were proposed using linear and nonlinear models. The data set was divided into active and inactive classes on the basis of their binding affinities. The two-clas...

The synthesis, physicochemical and pharmacological properties of new N-phenylamino derivatives of 2-azaspiro[4.4]nonane-1,3-dione (8-10), 2-azaspiro[4.5]decane-1,3-dione (11-18) and 3-cyclohexyl-pyrrolidine-2,5-dione ...

QSAR studies have been performed on some PPAR-gamma agonists using TATA-BioSuite software to identify the essential structural and physicochemical features for their PPAR-gamma agonistic activity. The 23 compounds wer...

We have synthesized a series of 18 1,5- and 2,5-disubstituted carbamoyl tetrazoles, including LY2183240 (1) and LY2318912 (7), two compounds previously described as potent inhibitors of the cellular uptake of the endo...