Assessing the issue of instability due to Michael adduct formation in novel chemical entities possessing a carbon-carbon double bond during early drug development--applicability of common laboratory analytical protocols.

Akshanth R. Polepally; V. Kumar; Ravikanth Bhamidipati; J. Kota; S. A. Naveed; K. H. Reddy; R. Mamidi; N. Selvakumar; R. Mullangi; N. Srinivas

DOI:10.1002/bmc.1015

Corpus ID: 7031156

Assessing the issue of instability due to Michael adduct formation in novel chemical entities possessing a carbon-carbon double bond during early drug development--applicability of common laboratory analytical protocols.

@article{Polepally2008AssessingTI,
  title={Assessing the issue of instability due to Michael adduct formation in novel chemical entities possessing a carbon-carbon double bond during early drug development--applicability of common laboratory analytical protocols.},
  author={Akshanth R. Polepally and V. Kumar and Ravikanth Bhamidipati and J. Kota and S. A. Naveed and K. H. Reddy and R. Mamidi and N. Selvakumar and R. Mullangi and N. Srinivas},
  journal={Biomedical chromatography : BMC},
  year={2008},
  volume={22 9},
  pages={
          960-76
        }
}

Akshanth R. Polepally, V. Kumar, +7 authors N. Srinivas
Published 2008
Chemistry, Medicine
Biomedical chromatography : BMC

The discovery of small-molecule novel chemical entities (NCEs) is often a complex play between appropriate structural requirements and optimization of the desired efficacy, safety and pharmacokinetic properties. One of the typical structural variants such as having an active carbon-carbon double bond (alpha, beta-unsaturated carbonyl group) in xenobiotics may lead to stability issues. Such functionalities are extremely reactive, paving way to nucleophilic attack by endogenously occurring and… Expand

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