Back to Search Start Over

Lasamide Containing Sulfonylpiperazines as Effective Agents for the Management of Glaucoma Associated Symptoms.

Lasamide Containing Sulfonylpiperazines as Effective Agents for the Management of Glaucoma Associated Symptoms.

Authors :
Kilbile JT
Sapkal SB
Renzi G
D'Agostino I
Boudjelal M
Tamboli Y
Cutarella L
Mori M
Sgambellone S
Villano S
Marri S
Lucarini L
Carradori S
Carta F
Supuran CT
Source :
ChemMedChem [ChemMedChem] 2024 Dec 16; Vol. 19 (24), pp. e202400601. Date of Electronic Publication: 2024 Nov 08.
Publication Year :
2024

Abstract

A series of 2,4-dichloro-5-{[4-(phenylsulfonyl)piperazin-1-yl]carbonyl}benzenesulfonamides were designed and synthesized through amidation of Lasamide 1 with substituted piperazines. The newly obtained compounds demonstrated remarkable inhibition potency and selectivity for the human (h) expressed Carbonic Anhydrase (CA; EC 4.2.1.1) II isoform. Selected compounds 7 and 9 were investigated in an in vivo model of glaucoma and showed relevant performances, with the latter being able to last the effect up to 4 hours. The results herein reported are in sustainment of Lasamide derivatives as a new class of compounds potentially exploitable for the management of uncontrolled intra ocular pressure (IOP).<br /> (© 2024 The Authors. ChemMedChem published by Wiley-VCH GmbH.)

Details

Language :
English
ISSN :
1860-7187
Volume :
19
Issue :
24
Database :
MEDLINE
Journal :
ChemMedChem
Publication Type :
Academic Journal
Accession number :
39319579
Full Text :
https://doi.org/10.1002/cmdc.202400601