Morpholine-2,5-dione derivatives having substituents with benzyl-protected carboxylic acid, benzyloxycarbonyl-protected amine and p-methoxy-protected thiol groups, respectively, were prepared in 2958% yield by cyclization of the corresponding N-[(2RS)-bromopropionyl]L-amino acids. Polyesteramides with protected pendant functional groups were obtained by ringopening copolymerization of either &-...

2-Chloro-, 2-bromo- and 2-azido-1,4,6-androstatriene-3,17-diones were synthesized from 1alpha,2alpha-epoxy-4,6-androstadiene-3,17-dione (2) using HCl, HBr and NaN(3), respectively. Compound 2 was also reacted with NaCN to give 2-cyano-1,4,6-androstatriene-3,17-dione (5) and 2beta-cyano-1alpha-hydroxy-4,6-androstadiene-3,17-dione (6). 6Alpha,7alpha-epoxy-1,4-androstadiene-3,17-dione (8) was reac...

Abstract: Introduction: Diabetes Mellitus is a disorder of metabolism described by high glucose levels. The kills larger number individuals consistently than malignant growth and AIDS combined. Presently available drugs have several drawbacks forcing to withdraw from treatment. potent side effect i.e., hepatotoxicity cardiovascular toxicity limits the use thiazolidine-2,4-dione derivative as sa...

The asymmetric unit of the title compound, C16H13N3O3·0.5C2H6OS, is composed of two independent pyrazolidine-3,5-dione mol-ecules and one dimethyl sulfoxide solvent mol-ecule. In each pyrazolidine-3,5-dione mol-ecule, an intra-molecular N-H⋯O hydrogen bond forms an S(5)S(6) motif. In the crystal, pairs of each independent pyrazolidine-3,5-dione mol-ecule are linked by N-H⋯O hydrogen bonds, form...

Comamonas testosteroni metabolizes testosterone as the sole carbon source via a meta-cleavage reaction. A meta-cleavage enzyme gene, tesB, was cloned from C. testosteroni TA441. The deduced N-terminal amino acid sequence of tesB matched that of the purified meta-cleavage enzyme which is induced in TA441 during growth on testosterone as the sole carbon source. The tesB-disrupted mutant did not s...

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...