- Aldolase-catalyzed synthesis of conformationally constrained iminocyclitols: Preparation of polyhydroxylated benzopyrrolizidines and cyclohexapyrrolizidines
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A straightforward chemo-enzymatic synthesis of new polyhydroxylated benzopyrrolizidines and cyclohexapyrrolizidines is developed. The two-step strategy consists of l-fuculose-1-phosphate aldolase variant F131A-catalyzed aldol addition of dihydroxyacetone phosphate to rac-N-benzyloxycarbonylindoline- 2-carbaldehyde as well as (2S*,3aS*,7aS*)- and (2S*,3aR*,7aR*)-N-benzyloxycarbonyloctahydroindole-2- carbaldehydes and a subsequent one-step catalytic deprotection-reductive amination.
- Laborda, Pedro,Sayago, Francisco J.,Cativiela, Carlos,Parella, Teodor,Joglar, Jesus,Clapes, Pere
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supporting information
p. 1422 - 1425
(2014/04/03)
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- BICYCLIC UNSATURATED TERTIARY AMINE COMPOUND
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The present invention provides a bicyclic unsaturated tertiary amine compound capable of inhibiting the production of inflammatory cytokines.A compound of the following formula (1): (wherein, A represents pyrrole or pyrazole, R1 represents an aryl group or a heteroaryl group which may be substituted, R2 represents a heteroaryl group which may be substituted, and R3 represents an indolizine group), or a pharmacologically acceptable salt thereof, a pharmacologically acceptable ester thereof or other pharmacologically acceptable derivative thereof.
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Page/Page column 81
(2010/02/11)
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- Heteroaryl-substituted pyrrole derivatives, their preparation and their therapeutic uses
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Compounds having activity against production of an inflammatory cytokine of formula (I)′: 1A′ is pyrrole; R1′ is phenyl or naphthyl; R2′ is pyridyl or pyrimidinyl; R3′ is (IIa)′, (IIb)′ or (IIc)′: 2m′ is 1; E′ is nitrogen; D′ is >C(R5′)—, R5′ is hydrogen, Substituent α′ or Substituent β′; B′ is nitrogen-containing 5-membered heterocyclic; R4′ is 1 to 3 substituents from Substituent α′, Substituent β′ and Substituent γ′; R1′ and R3′ are bonded to two atoms of the pyrrole adjacent to the pyrrole atom bonded to R2′; Substituent α′ is hydroxyl, nitro, cyano, halogen, alkoxy, halogeno alkoxy, alkylthio, halogeno alkylthio or —NRa′Rb′; Ra′ and Rb′ are hydrogen, alkyl, alkenyl, alkynyl, aralkyl or alkylsulfonyl, or Ra′ and Rb′ with the nitrogen atom form a heterocyclyl; Substituent β′ is alkyl, alkenyl, alkynyl, aralkyl or cycloalkyl; Substituent γ′ is oxo, hydroxyimino, alkoxyimino, alkylene, alkylenedioxy, alkylsulfinyl, alkylsulfonyl, aryl, aryloxy, alkylidenyl or aralkylidenyl.
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- Heterocycle carboxamides as antiviral agents
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The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
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- Tricyclic [6.5.51]-fused oxazolidinone antibacterial agents
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The present invention involves tricyclic-fused 6-member ring oxazolidinones STR1 and tricyclic-fused 5-member ring oxazolidinones STR2 which are useful as antibacterial agents.
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