307539-90-8Relevant articles and documents
Lead derivatization of ethyl 6-bromo-2-((dimethylamino)methyl)-5-hydroxy-1-phenyl-1H-indole-3-carboxylate and 5-bromo-2-(thiophene-2-carboxamido) benzoic acid as FabG inhibitors targeting ESKAPE pathogens
Varakala, Saiprasad Dasugari,Reshma, Rudraraju Srilakshmi,Schnell, Robert,Dharmarajan, Sriram
, (2021/11/26)
Our previous studies on FabG have identified two compounds 5-bromo-2-(thiophene-2-carboxamido) benzoic acid (A) and ethyl 6-bromo-2-((dimethylamino)methyl)-5-hydroxy-1-phenyl-1H-indole-3-carboxylate(B) as best hits with allosteric mode of inhibition. FabG is an integral part of bacterial fatty acid biosynthetic system FAS II shown to be an essential gene in most ESKAPE Pathogens. The current work is focussed on lead expansion of these two hit molecules which ended up with forty-three analogues (twenty-nine analogues from lead compound A and fourteen compounds from lead compound B). The enzyme inhibition studies revealed that compound 15 (effective against EcFabG, AbFabG, StFabG, MtFabG1) and 19 (inhibiting EcFabG and StFabG) had potency of broad-spectrum inhibition on FabG panel.
The first synthesis of 2-amino-1,4-dihydroquinolines
Viault, Guillaume,Grée, Danielle,Roisnel, Thierry,Chandrasekhar, Srivari,Grée, René
experimental part, p. 10149 - 10154 (2010/02/27)
A versatile strategy is described for the synthesis of new 2-amino-1,4-dihydroquinolines. It involved a Knoevenagel condensation of N-protected-2-amino-5-bromobenzaldehyde with ethylcyanoacetate, followed by a cyclization and protection of the NH group to
An intramolecular cycloaddition approach to pyrrolo[3,2-c]quinolones
He, Yong,Mahmud, Hossen,Wayland, Brian R,Dias, H.V.Rasika,Lovely, Carl J
, p. 1171 - 1174 (2007/10/03)
An approach to pyrrolo[3,2-c]quinolones is described which relies on an intramolecular azomethine ylide alkene cycloaddition reaction. Critical to the success of this reaction was the requirement for alkylation of the aniline nitrogen, in the absence of t
