Tetrahydro-1H-benzo[b]azonin-2,7-dione (2a) has been used as a precursor in the synthesis of dibenzo[b,f ][1,5]diazacyclododecene and dibenzo[b,g][1,6]diazacyclododecene ring systems 4 and 5, respectively, via periodate oxidation of the appropriate indolo-benzo[b]azonines 3 and 7. The synthesis of hexahydro-benzo[b][1,4]diazecin-2,7-dione (10) has been achieved by the Schmidt reaction of 2a. Th...

A series of 2-substituted 6-hydroxy-1,2,4-triazine-3,5(2H,4H)-dione derivatives were synthesized as inhibitors of D-amino acid oxidase (DAAO). Many compounds in this series were found to be potent DAAO inhibitors, with IC50 values in the double-digit nanomolar range. The 6-hydroxy-1,2,4-triazine-3,5(2H,4H)-dione pharmacophore appears metabolically resistant to O-glucuronidation unlike other str...

The microbial degradation of cholic acid by Pseudomonas sp. N.C.I.B. 10590 was studied, and two major products were isolated and identified as 7 alpha, 12 beta-dihydroxyandrosta-1,4-diene-3,17-dione and 7 alpha, 12 alpha-dihydroxy-3-oxopregna-1,4-diene-20-carboxylic acid. Four minor products were isolated and evidence is given for the following structures: 7 alpha, 12 alpha-dihydroxyandrosta-1,...

Transposon mutant strains which were affected in bile acid catabolism were isolated from four Pseudomonas spp. Two of the mutant groups isolated were found to accumulate 12 alpha-hydroxyandrosta-1,4-diene-3,17-dione as the major product from deoxycholic acid. Strains in one of these two groups were able to grow on steroids such as chenodeoxycholic acid, which lacks a 12 alpha-hydroxy function, ...

Two series of N-(4-methylpiperazin-1-yl)- and N-[3-(4-methylpiperazin-1-yl)-propyl]-3-aryl- and 3-spirocycloalkyl-pyrrolidine-2,5-dione derivatives were synthesized and tested for anticonvulsant activity in the maximum electroshock (MES) seizure and pentetrazole (sc PTZ) seizure threshold tests. Compounds with an aromatic ring at position-3 of pyrrolidine-2,5-dione exhibited anticonvulsant acti...

the reaction of bis[4-hydroxy-3-methoxyphenyl]-1,6-heptadiene-3,5-dione (curcumin) and two novel ligands of bis[4-tetrabenzylglucose-3-methoxyphenyl]-1,6-heptadiene-3,5-dione (bis(tetrabenzylglucose)curcumin) (btbgc) and bis[4-tetraacetylglucose-3-methoxyphenyl]-1,6-heptadiene-3,5-dione (bis(tetraacetylglucose)curcumin) (btagc) with vanadium in methanol, in a 2:1 molar ratio, which yield the co...