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Article

Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists.

Bioorganic & medicinal chemistry letters - 15 Mar 2009

Kalgutkar Amit S, Bauman Jonathan N, McClure Kim F, Aubrecht Jiri, Cortina Santo R, Paralkar Janvi

Abstract excerpt

The biochemical basis for S9-dependent mutagenic response of the 5-HT(2C) receptor agonist and diazinylpiperazine derivative 1 in the Salmonella Ames assay involves P450-mediated bioactivation to DNA-reactive quinone-methide, aldehyde and nitrone intermediates. Mechanistic information pertaining to the metabolism of 1 was used in the design of diazinylpiperazine 5 to eliminate the safety liability. While 5 was...

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PMID: 19246199
DOI: 10.1016/j.bmcl.2009.02.032

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

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