- Identifying new lead structures to enhance tolerance towards drought stress via high-throughput screening giving crops a quantum of solace
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Novel synthetic lead structures interacting with RCAR/(PYR/PYL) receptor proteins were identified based on the results of a high-throughput screening campaign of a large compound library followed by focused SAR studies of the three most promising hit clusters. Whilst indolinylmethyl sulfonamides 8y,z and phenylsulfonyl ethylenediamines 9y,z showed strong affinities for RCAR/ (PYR/PYL) receptor proteins in wheat, thiotriazolyl acetamides 7f,s exhibited promising efficacy against drought stress in vivo (wheat, corn and canola) combined with confirmed target interaction in wheat and arabidopsis thaliana. Remarkably, binding affinities of several representatives of 8 and 9 were on the same level or even better than the essential plant hormone abscisic acid (ABA).
- Frackenpohl, Jens,Schneider, Linn,Decker, Luka J.B.,Dittgen, Jan,Fenkl, Franz,Fischer, Christian,Franke, Jana,Freigang, Joerg,Getachew, Rahel,Gonzalez Fernandez-Nino, Susana M.,Helmke, Hendrik,Hills, Martin J.,Hohmann, Sabine,Kleemann, Jochen,Kurowski, Karoline,Lange, Gudrun,Luemmen, Peter,Meyering, Nicole,Poree, Fabien,Schmutzler, Dirk,Wrede, Sebastian
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- Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors
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A novel sulfanyltriazole was discovered as an HIV-1 non-nucleoside reverse transcriptase inhibitor via HTS using a cell-based assay. Chemical modifications and molecular modeling studies were carried out to establish its SAR and understand its interactions with the enzyme. These modifications led to the identification of sulfanyltriazoles with low nanomolar potency for inhibiting HIV-1 replication and promising activities against selected NNRTI resistant mutants. These novel and potent sulfanyltriazoles could serve as advanced leads for further optimization.
- Wang, Zhiwei,Wu, Baogen,Kuhen, Kelli L.,Bursulaya, Badry,Nguyen, Truc N.,Nguyen, Deborah G.,He, Yun
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p. 4174 - 4177
(2007/10/03)
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