Novel small molecule inhibitors targeting the "switch region" of bacterial RNAP: Structure-based optimization of a virtual screening hit
Rising resistance against current antibiotics necessitates the development of antibacterial agents with alternative targets. The "switch region" of RNA polymerase (RNAP), addressed by the myxopyronins, could be such a novel target site. Based on a hit can
Sahner, J. Henning,Groh, Matthias,Negri, Matthias,Haupenthal, J?rg,Hartmann, Rolf W.
supporting information
p. 223 - 231
(2013/10/01)
Synthesis and combinatorial approach of the reactivity of 6- and 7-arylthieno[3,2-d][1,3]oxazine-2,4-diones
This paper describes a general procedure for the synthesis of new substituted thiaisatoic anhydrides or 6- or 7-aryl-1H-thiéno[3,2-d][1,3] oxazine-2,4-diones 3a-j and 4a-f. They were synthesized in large scale under microwave heating conditions with high yields. The reactivity vs nucleophilic reagents of these compounds was studied and permitted to develop a simple combinatorial procedure to synthesize a library of new thiophene ureidoacids 7a-j and 8a-j.
Le Foulon, Fran?ois-Xavier,Braud, Emmanuelle,Fabis, Frédéric,Lancelot, Jean-Charles,Rault, Sylvain
p. 10051 - 10057
(2007/10/03)
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