A series of new aromatic esters based on 4,16-pregnadiene-6,20-dione skeleton, namely 3β-benzoyloxy-4,16-pregnadiene-6,20-dione and 3β-furoyloxy-4,16-pregnadiene- 6,20-dione, which may be good inhibitors for the 5α-reductase enzyme and show high antiandrogenic activity, were synthesized starting from diosgenin. The structures of the steroids were characterized by elemental analysis, 1H NMR, 13C...

Mycobacterium smegmatis PTCC 1307 (CIP 73.26) was used as a microbial agent to produce androsta-1,4-diene-3,17-dione (ADD) and androst-4-ene-3,17-dione, two useful precursors in the synthesis of steroid drugs. The side chain of cholesterol, as the substrate, was selectively cleaved in the presence of five enzyme inhibitors. An intermediate structure with intact side chain, cholest-4-ene-3-one, ...

2-Substituted derivatives of indane-1,3-dione 3a–f , 5a–g, 6a–g were synthesized and investigated as anticoagulant agents. 2-Arylindane-1,3-diones (3) were obtained in the reaction of phthalide with appropriate arylaldehydes. 2-Arylmethyleneindane-1,3-diones (5) were prepared by condensation of indane-1,3-dione with the corresponding arylaldehydes. The compounds 5 were converted into their meth...

The synthesis and evaluation of the anticancer activity of 3'-aryl-5'-arylidene-spiro[3H-indole-3,2'-thiazolidine]-2,4'(1H)-diones and spiro[3H-indole-3,2'-thi-azolidine]-2,4'(1H)-dione-3'-alkanoic acid esters were described. The structure of the compounds was determined by (1)H and (13)C NMR and their in vitro anticancer activity was tested in the National Cancer Institute. Among the tested co...

In the title compound, C21H23N3O7, the pyrimidine-dione ring adopts a screw-boat conformation, whereas the cyclo-hexenone ring adopts an envelope conformation, with the C atom bearing the methyl groups as the flap atom. The dihedral angle between the mean planes of the pyrimidine-dione and cyclo-hexenone rings is 58.78 (2)°. The pyrimidine-dione and cyclo-hexenone rings form dihedral angles of ...

Four new purine alkaloids, namely, 6-(1'-purine-6',8'-dionyl)suberosanone ( 1), 3,9-(2-imino-1-methyl-4-imidazolidinone-5-yl)isopropenylpurine-6,8-dione ( 2), 1-(3'-carbonylbutyl)purine-6,8-dione ( 3), and 9-(3'-carbonylbutyl)purine-6,8-dione ( 4), together with three known compounds, guanosine ( 5), thymidine ( 6), and adenosine ( 7), were isolated from the EtOH/CH 2Cl 2 extracts of the South ...

New 7-thio derivatives of 6,7-dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione have been synthesized by the reaction of 3-cyclohexyl-7-thio-6,7-dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione with alkylhalogenides. The synthesized compounds were tested for antioxidant activity on the model of Fe(2+)-dependent oxidation of adrenaline in vitro. It was found that the antiradical activity of...

The chromatographic parameters of arylpiperazinylpropyl derivatives of imidazolidine-2,4-dione and imidazo[2,1-f]purine-2,4-dione were investigated using reversed-phase thin layer chromatography method. The results revealed that R(M0) of investigated compounds depended on substituent in arylpiperazinyl fragment as well as on a nature of (cycloalkyl)aromatic ring at 5 position of imidazolidine-2...