Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors

Manojit Pal; Venugopal Rao Veeramaneni; Murali Nagabelli; Srinivas Rao Kalleda; Parimal Misra; Seshagiri Rao Casturi; Koteswar Rao Yeleswarapu

doi:10.1016/s0960-894x(03)00282-8

Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors

Bioorg Med Chem Lett. 2003 May 19;13(10):1639-43. doi: 10.1016/s0960-894x(03)00282-8.

Authors

Manojit Pal¹, Venugopal Rao Veeramaneni, Murali Nagabelli, Srinivas Rao Kalleda, Parimal Misra, Seshagiri Rao Casturi, Koteswar Rao Yeleswarapu

Affiliation

¹ Department of Chemistry, Discovery Research, Dr. Reddy's Laboratories Ltd., Bollaram Road, Miyapur, Hyderabad 500050, India. manojitpal@drreddys.com

PMID: 12729631
DOI: 10.1016/s0960-894x(03)00282-8

Abstract

A number of naphthofuranones were synthesized and tested for COX-1 and COX-2 inhibition. Few of them were identified as selective COX-2 inhibitors. Structure-activity relationship studies within the series are discussed.

MeSH terms

Cyclooxygenase 1
Cyclooxygenase 2
Cyclooxygenase 2 Inhibitors
Cyclooxygenase Inhibitors / chemical synthesis*
Cyclooxygenase Inhibitors / chemistry
Cyclooxygenase Inhibitors / pharmacology
Furans / chemical synthesis
Furans / chemistry
Furans / pharmacology*
Heterocyclic Compounds, 4 or More Rings / chemical synthesis
Heterocyclic Compounds, 4 or More Rings / chemistry
Heterocyclic Compounds, 4 or More Rings / pharmacology
Humans
Inhibitory Concentration 50
Isoenzymes / chemistry
Membrane Proteins
Molecular Conformation
Prostaglandin-Endoperoxide Synthases / chemistry
Structure-Activity Relationship

Substances

Cyclooxygenase 2 Inhibitors
Cyclooxygenase Inhibitors
Furans
Heterocyclic Compounds, 4 or More Rings
Isoenzymes
Membrane Proteins
Cyclooxygenase 1
Cyclooxygenase 2
PTGS1 protein, human
PTGS2 protein, human
Prostaglandin-Endoperoxide Synthases