5-arylaminouracil derivatives as potential dual-action agents

Several 5-aminouracil derivatives that have previously been shown to inhibit Mycobacterium tuberculosis growth at concentrations of 5-40 μg/mL are demonstrated to act also as noncompetitive non-nucleoside inhibitors of HIV-1 reverse transcriptase without causing toxicity in vitro (McyrillicT-4 cells) and ex vivo (human tonsillar tissue)

2-(2,4-Dioxy-1,2,3,4-tetrahydropyrimidin-1-yl)-N-(4-phenoxyphenyl)-acetamides as a novel class of cytomegalovirus replication inhibitors

A series of novel uracil derivatives, bearing N-(4-phenoxyphenyl)acetamide moiety at N3 of a pyrimidine ring, has been synthesized. Their antiviral activity has been evaluated. It has been found that the novel compounds possess high inhibitory activity against replication of human cytomegalovirus (AD-169 and Davis strains) in HEL cell cultures. In addition, some of the derivatives proved to be inhibitory against varicella zoster virus.status: publishe

An efficient route to novel uracil-based drug-like molecules

In order to identify new antiretroviral agents, a series of novel uracil derivatives have been synthesized. Optimized conditions for coupling of Weinreb amides with aromatic Grignard reagents allow the convenient preparation of key benzophenone intermediates in high yields and purities. The use of a modified silyl Hilbert–Johnson reaction affords the target compounds under mild conditions

Synthesis and anti-HIV-1 activity of 1-[omega-(phenoxy)alkyl and -alkenyl]Uracil derivatives

1-[ω-(Phenoxy)alkyl and -alkenyl]uracil derivatives were synthesized via condensation of equimolar amounts of 2,4-bis(trimethylsilyloxy)pyrimidine and 1-halo-ω-(phenoxy)alkane or -alkene in order to discover new non-nucleoside inhibitors of HIV-1 reverse transcriptase. Their anti-HIV-1 activity was studied in CEM-cell culture and against HIV-1 reverse transcriptase. It was found that several compounds exhibited marked activity. © 2013 Springer Science+Business Media New York.status: publishe

Clay-mineral and grain-size distributions in surface sediments of the White Sea (Arctic Ocean): indicators of sediment sources and transport processes

In this study, the grain-size and clay-mineral compositions of 73 surface sediment samples collected in a variety of environmental settings in the White Sea are presented to characterize recent sedimentation processes, reconstruct transport pathways, and identify potential source areas of the terrigenous components. Areas >100 m deep are invariably characterized by silty clay, whereas areas <100 m deep exhibit more heterogeneous grain-size compositions plausibly explained by coastal erosion and (re-)distribution mechanisms, particularly tidal currents. The dominance of sand in the estuarine areas of the Onega and Dvina rivers as well as toward Gorlo Strait connecting the White Sea with the Barents Sea, is attributed to increased current speeds. Illite and smectite are the dominant clay minerals in recent sediments of the southwestern and eastern White Sea sectors, respectively. Their distribution patterns largely depend on the geology of the source areas and mirror surface circulation patterns, especially in Dvina Bay. Smectite is a key clay mineral in White Sea surface sediments as it reveals the dominating influence of the Northern Dvina's runoff on sedimentation and water circulation throughout the basin of the sea. In comparison to other Eurasian shelf seas, the White Sea is characterized by a greater diversity of clay-mineral assemblages, which range from illite- to smectite-dominated sectors containing variable amounts of chlorite and kaolinite