Synthesis of Dinaphtho-dioxaphosphocin-8-oxides, Epoxides and Bisphosphonates

Preparation of 8-substituted-16H-dinaphtho [2,1-d:1’,2’-g] [1,3,2] dioxaphosphocin 8-oxides (5a–g) with an eight-membered phosphorus heterocyclic system (2) and their epoxides and bisphosphonates was accomplished by reacting 8-bromo-dinaphthophosphocin (2) with different mono and bis Grignard reagents (3a–g and 6) followed by oxidation with H2O2. Their structures were confirmed by elemental and spectral (1H, 13C and 31P NMR) data analysis. Some of these compounds are found to possess moderate antimicrobial activity.KEYWORDS: Dioxaphosphocin 8-oxides, dioxaphosphocin bisphosphonates, antimicrobial activity

Synthesis of phosphorus, nitrogen, oxygen and sulphur macrocycles

Phosphorus macromolecules containing oxygen, nitrogen and sulphur were synthesised by the addition of phosphoric acid diallyl esters to 1,2-ethandithiol or various amines in dry dichloromethane. All compounds were characterised by IR, NMR ( 1 H, 13 C and 31 P) and mass spectral studies and elemental analysis. Their antimicrobial activity has also been evaluated

Synthesis and bioactivity of some new 2-substituted-3,4-dihydro-3-(3'-chloro-4'-fluorophenyl)-2<i style="">H</i>-[1,3,2]benzoxaza­phosphorin 2-oxides

2171-2177Synthesis, spectral analysis and bioactivity of the title compounds have been described. The structures of these compounds are confirmed by analytical and spectral (IR, 1H, 13C, 31P NMR and mass) data. They show significant antimicrobial and insecticidal activity. They promote growth of the phosphate solubilizing bacteria in the soil without any toxic effect on the host tissue

Basic Quinolinonyl Diketo Acid Derivatives as Inhibitors of HIV Integrase and their Activity against RNase H Function of Reverse Transcriptase

A series of antiviral basic quinolinonyl diketo acid derivatives were developed as inhibitors of HIV-1 IN. Compounds 12d,f,i inhibited HIV-1 IN with IC50 values below 100 nM for strand transfer and showed a 2 order of magnitude selectivity over 3′-processing. These strand transfer selective inhibitors also inhibited HIV-1 RNase H with low micromolar potencies. Molecular modeling studies based on both the HIV- 1 IN and RNase H catalytic core domains provided new structural insights for the future development of these compounds as dual HIV-1 IN and RNase H inhibitors

Activities, crystal structures, and molecular dynamics of dihydro-1H-isoindole derivatives, inhibitors of HIV-1 integrase

Based on a series of lactam and phthalimide derivatives that inhibit HIV-1 integrase, we developed a new derivative, XZ-259, with biochemical and antiviral activities comparable to raltegravir. We determined the crystal structures of XZ-259 and four other derivatives in complex with the prototype foamy virus intasome. The compounds bind at the integrase-Mg(2+)-DNA interface of the integrase active site. In biochemical and antiviral assays, XZ-259 inhibits raltegravir-resistant HIV-1 integrases harboring the Y143R mutation. Molecular modeling is also presented suggesting that XZ-259 can bind in the HIV-1 intasome with its dimethyl sulfonamide group adopting two opposite orientations. Molecular dynamics analyses of the HIV-1 intasome highlight the importance of the viral DNA in drug potency