volume 92 pages 103210

Spirocyclic sulfonamides with carbonic anhydrase inhibitory and anti-neuropathic pain activity

Y Kalisha Vali
Rambabu Gundla
Om V. Singh
Yasinalli Tamboli
Lorenzo Di Cesare Manelli
Carla Ghelardini
Abdul-Malek S. Al-Tamimi
Fabrizio Carta
Andrea Angeli
Claudiu T Supuran
Publication typeJournal Article
Publication date2019-11-01
scimago Q1
wos Q1
SJR0.786
CiteScore8.3
Impact factor4.7
ISSN00452068, 10902120
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Abstract
A novel series of 4-oxo-spirochromane bearing primary sulfonamide group were synthetized as Carbonic Anhydrase inhibitors (CAIs) and tested for their management of neuropathic pain. Indeed, CAs have been recently validated as novel therapeutic targets in neuropathic pain. All compounds, here reported, showed strong activity against hCA II and hCA VII with KI values in the low or sub-nanomolar range. Two compounds (6d and 6l) showed good neuropathic pain attenuating effects and longer duration than drug reference acetazolamide in an animal model of oxaliplatin induced neuropathy.
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GOST |
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GOST Copy
Kalisha Vali Y. et al. Spirocyclic sulfonamides with carbonic anhydrase inhibitory and anti-neuropathic pain activity // Bioorganic Chemistry. 2019. Vol. 92. p. 103210.
GOST all authors (up to 50) Copy
Kalisha Vali Y., Gundla R., Singh O. V., Tamboli Y., Di Cesare Manelli L., Ghelardini C., Al-Tamimi A. S., Carta F., Angeli A., Supuran C. T. Spirocyclic sulfonamides with carbonic anhydrase inhibitory and anti-neuropathic pain activity // Bioorganic Chemistry. 2019. Vol. 92. p. 103210.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/j.bioorg.2019.103210
UR - https://doi.org/10.1016/j.bioorg.2019.103210
TI - Spirocyclic sulfonamides with carbonic anhydrase inhibitory and anti-neuropathic pain activity
T2 - Bioorganic Chemistry
AU - Kalisha Vali, Y
AU - Gundla, Rambabu
AU - Singh, Om V.
AU - Tamboli, Yasinalli
AU - Di Cesare Manelli, Lorenzo
AU - Ghelardini, Carla
AU - Al-Tamimi, Abdul-Malek S.
AU - Carta, Fabrizio
AU - Angeli, Andrea
AU - Supuran, Claudiu T
PY - 2019
DA - 2019/11/01
PB - Elsevier
SP - 103210
VL - 92
PMID - 31473472
SN - 0045-2068
SN - 1090-2120
ER -
BibTex
Cite this
BibTex (up to 50 authors) Copy
@article{2019_Kalisha Vali,
author = {Y Kalisha Vali and Rambabu Gundla and Om V. Singh and Yasinalli Tamboli and Lorenzo Di Cesare Manelli and Carla Ghelardini and Abdul-Malek S. Al-Tamimi and Fabrizio Carta and Andrea Angeli and Claudiu T Supuran},
title = {Spirocyclic sulfonamides with carbonic anhydrase inhibitory and anti-neuropathic pain activity},
journal = {Bioorganic Chemistry},
year = {2019},
volume = {92},
publisher = {Elsevier},
month = {nov},
url = {https://doi.org/10.1016/j.bioorg.2019.103210},
pages = {103210},
doi = {10.1016/j.bioorg.2019.103210}
}