Identification and characterization of potential impurities in raloxifene hydrochloride.

During the synthesis of the bulk drug Raloxifene hydrochloride, eight impurities were observed, four of which were found to be new. All of the impurities were detected using the gradient high performance liquid chromatographic (HPLC) method, whose area percentages ranged from 0.05 to 0.

Inhibitors interacting with the magnesium binding site of reverse transcriptase: synthesis and biological activity studies of 3'-(omega-amino-acyl) amino-3'-deoxy-thymidine.

Active site of reverse transcriptase contains carboxylate groups involved in the magnesium binding. We prepared some nucleoside analogs which could bind to these carboxylates preventing the binding of nucleotides. To the 3'-amino-3'-deoxy-thymidine, different N-protected omega-amino-acids were bound, the protection removed to give the 3'-(omega-amino-acyl-) amino-3'-deoxy-thymidines in good yield.

Anti-HIV active petrosins from the marine sponge Petrosia similis.

A marine sponge Petrosia similis afforded two compounds which belongs to bis-quinolizidine alkaloids namely, petrosin (1) and petrosin-A (2), respectively. Petrosin (1) and petrosin-A (2) showed anti-HIV inhibition with IC(50) values of 41.3 and 52.

Two new macrocyclic diaryl ether heptanoids from Boswellia ovalifoliolata.

The stems of Boswellia ovalifoliolata BAL. & HENRY (Burseraceae) afforded two new macrocyclic diaryl ether heptanoids, ovalifoliolatin A (1) and B (2) together with three known compounds; acerogenin C (3), 3 alpha-hydroxyurs-12-ene (4), and sitost-4-en-3-one (5). The structures were established by means of spectroscopic analysis and compounds 1, 3-5 were evaluated for their antibacterial activity.

Two new bromotyrosine-derived metabolites from the sponge Psammaplysilla purpurea.

Two new bromotyrosine-derived metabolites (1, 2) have been isolated along with the known compounds 3,5-dibromo-4-methoxyphenylacetonitrile, 3-bromo-4-methoxyphenylacetonitrile, 3-bromo-4-hydroxyphenylacetonitrile, 1-hydroxyuracil, 1-methoxyhemibastadin 2, purpuramine H and a steroid 5alpha,8alpha-epidioxycholest-6-en-3beta-ol from the sponge Psammaplysilla purpurea. Compounds 1 and 2 were characterized by interpretation of their spectral data. The antibacterial activity of these compounds is summarized.