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Relevant academic research and scientific papers

Pyrazole compounds as well as preparation method and application thereof

The invention provides pyrazole compounds with neuraminidase (NA) inhibitory activity as well as a preparation method and application thereof in pharmacy, and specifically relates to a compound shownin a formula (I), and pharmaceutically acceptable salt, an isomer and a prodrug thereof, and the definition of various groups is as described in the description. The invention further relates to pharmaceutic preparations and pharmaceutical compositions of the compounds and application of the pharmaceutic preparations and the pharmaceutical compositions in treatment of diseases caused by influenzavirus infection. The pyrazole compounds provided by the invention have good inhibitory effects on H1N1 influenza A virus infected cells.

Efficient regio- And stereoselective formation of azocan-2-ones via 8-endo cyclization of α-carbamoyl radicals

The iodine-atom-transfer 8-endo cyclization of α-carbamoyl radicals was investigated experimentally and theoretically. With the aid of Mg(CIO 4)2 and a bis(oxazoline) ligand, N- ethoxycarbonylsubstituted N-(pent-4-enyl)-2-iodoalkanamides underwent 8-endo cyclization leading to the formation of only the corresponding 3,5-trans-substituted azocan-2-ones in excellent yields. Similarly, the BF 3·OEt2/H2O-promoted reactions of N-ethoxycarbonyl-N-(2-allylaryl)-2-iodoalkanamides afforded exclusively the benzazocanone products with a 3,5-cis configuration in high yields. The bidentate chelation of substrate radicals not only significantly improved the efficiency of cyclization but also resulted in the change of stereochemistry of azocanone products from 3,8-iransto 3,8-cis. Theoretical calculations at the UB3LYP/6-31G* level revealed that the cyclization of N-carbonyl- substituted α-carbamoyl radicals occurs via the E-conformational transition states without the presence of a Lewis acid. On the other hand, the cyclization proceeds via the Z-conformational transition states when the substrates form the bidentate chelation with a Lewis acid. In both cases, the 8-endo cyclization is always fundamentally preferred over the corresponding 7-exo cyclization. The complexed radicals having the more rigid conformations also allow the better stereochemical control in the iodine-atom-abstraction step. To further understand the reactivity of a-carbamoyl radicals, the competition between the 8-endo and 5-exo cyclization was also studied. The results demonstrated that the 8-endo cyclization is of comparable rate to the corresponding 5-exo cyclization for a-carbamoyl radicals with fixed Z-conformational transition states. As a comparison, the 8-endo mode is fundamentally preferred over the 5-exo mode in the cyclization of NH-amide substrates because the latter requires the Z-conformational transition states, whereas the former proceeds via the more stable E-conformational transition states.

COMPOUNDS COMPRISING A LACTAM OR A LACTAM DERIVATIVE MOIETY, PROCESSES FOR MAKING THEM, AND THEIR USES

The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.

2-azacycloalkylthiopenem derivatives

Certain 2-azacycloalkylthio-2-penem-3-carboxylic acid compounds are useful as antibacterials for treating mammals and have the formula STR1 or a pharmaceutically acceptable salt thereof, wherein: R is STR2 A is alkylene having 2-4 carbon atoms, alkylene h