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Combinatorial Chemistry & High Throughput Screening

Author(s): R. C. Mishra, Neetu Tewari, Kavita Arora, Rumana Ahmad, R. P. Tripathi, V. K. Tiwari, R. D. Walter and A. K. Srivastava

DOI: 10.2174/1386207033329887

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DBU-Assisted Cyclorelease Elimination: Combinatorial Synthesis and γ- Glutamyl Cysteine Synthetase and Glutathione-S-Transeferase Modulatory Effect of C-Nucleoside Analogs

Page: [37 - 50] Pages: 14

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Abstract

A combinatorial library of 60 C- nucleoside analogs was synthesized by sequential coupling of building blocks followed by cyclative cleavage with DBU in an efficient manner. Only DMSO soluble compounds were tested for their modulatory effect against filarial γ-glutamyl cysteine synthetase (γ-GCase) and glutathione-S-transeferases (GSTs). Several compounds were found to be weak inhibitors of filarial γ-GCase, whereas, most of them stimulated filarial GSTs.

Keywords: cyclorelease elimination, c- nucleosides, combinatorial synthesis, diazabicyclo (5.4.0) undec-7-ene, glutamyl cysteine synthetase, glutathione-s- transeferase, dihydropyrimidinones