title: DBU-assisted cyclorelease elimination: combinatorial synthesis and gamma-glutamyl cysteine synthetase and glutathione-S-transeferase modulatory effect of C-nucleoside analogs.
abstract: A combinatorial library of 60C- 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 gamma-glutamyl cysteine synthetase (gamma-GCase) and glutathione-S-transeferases (GSTs). Several compounds were found to be weak inhibitors of filarial gamma-GCase, whereas, most of them stimulated filarial GSTs.
authors.affiliation: Medicinal Chemistry and Central Drug Research Institute, Lucknow-226001, India. rpt_56@yahoo.com
authors.forename: R C
authors.initials: RC
authors.lastname: Mishra
authors.forename: Neetu
authors.initials: N
authors.lastname: Tewari
authors.forename: Kavita
authors.initials: K
authors.lastname: Arora
authors.forename: Rumana
authors.initials: R
authors.lastname: Ahmad
authors.forename: R P
authors.initials: RP
authors.lastname: Tripathi
authors.forename: V K
authors.initials: VK
authors.lastname: Tiwari
authors.forename: R D
authors.initials: RD
authors.lastname: Walter
authors.forename: A K
authors.initials: AK
authors.lastname: Srivastava
mesh_terms: D000447:Aldehydes / Q000737:chemistry; D000818:Animals; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000737:chemistry*; D002417:Cattle; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D005370:Filarioidea / Q000187:drug effects / Q000201:enzymology; D005721:Glutamate-Cysteine Ligase / Q000037:antagonists & inhibitors*; D005982:Glutathione Transferase / Q000037:antagonists & inhibitors*; D017953:Isocyanates / Q000737:chemistry; D009705:Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology*; D012441:Saccharomyces cerevisiae / Q000187:drug effects / Q000201:enzymology; D013329:Structure-Activity Relationship
chemical_list: D000447:Aldehydes; D019086:Bridged Bicyclo Compounds, Heterocyclic; D017953:Isocyanates; D009705:Nucleosides; D005982:Glutathione Transferase; D005721:Glutamate-Cysteine Ligase; C031033:1,8-diazabicyclo(5.4.0)undec-7-ene