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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.
- 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.)
- Subjects :
- Humans
Animals
Structure-Activity Relationship
Carbonic Anhydrase II antagonists & inhibitors
Carbonic Anhydrase II metabolism
Intraocular Pressure drug effects
Molecular Structure
Glaucoma drug therapy
Carbonic Anhydrase Inhibitors chemistry
Carbonic Anhydrase Inhibitors pharmacology
Carbonic Anhydrase Inhibitors chemical synthesis
Carbonic Anhydrase Inhibitors therapeutic use
Sulfonamides chemistry
Sulfonamides pharmacology
Sulfonamides chemical synthesis
Sulfonamides therapeutic use
Piperazines pharmacology
Piperazines chemistry
Piperazines chemical synthesis
Subjects
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