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Synthesis of benzensulfonamides linked to quinazoline scaffolds as novel carbonic anhydrase inhibitors.
Carbonic anhydrase (CA) inhibitory activities of newly synthesized quinazoline-linked benzensulfonamides 10-29, 31, 32, 35, 36, and 45-51 against human CA (hCA) isoforms I, II, IX, and XII wereExpand
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Benzoxaborole compounds for therapeutic uses: a patent review (2010- 2018)
ABSTRACT Introduction: Benzoxaborole is a versatile boron-heterocyclic scaffold which has found in the last 10 years a broad spectrum of applications in medicinal chemistry, due to itsExpand
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Continued exploration of 1,2,4-oxadiazole periphery for carbonic anhydrase-targeting primary arene sulfonamides: Discovery of subnanomolar inhibitors of membrane-bound hCA IX isoform that selectively
An expanded set of diversely substituted 1,2,4-oxadiazole-containing primary aromatic sulfonamides was synthesized and tested for inhibition of human carbonic anhydrase I, II, IX and XII isoforms.Expand
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Novel synthesized SLC-0111 thiazole and thiadiazole analogues: Determination of their carbonic anhydrase inhibitory activity and molecular modeling studies.
In the presented work, we report the design and synthesis of novel SLC-0111 thiazole and thiadiazole analogues (11a-d, 12a-d, 16a-c and 17a-d). A bioisosteric replacement approach was adopted toExpand
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A New Kid on the Block? Carbonic Anhydrases as Possible New Targets in Alzheimer’s Disease
The increase in the incidence of neurodegenerative diseases, in particular Alzheimer’s Disease (AD), is a consequence of the world′s population aging but unfortunately, existing treatments are onlyExpand
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The role of carbonic anhydrases in extinction of contextual fear memory
Significance Disruption of memories of stressful events may trigger maladaptive responses that are distinctive features of obsessive-compulsive disorders, phobias, posttraumatic stress disorderExpand
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Novel 2-substituted-benzimidazole-6-sulfonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IX and XII and molecular docking studies
Abstract Inhibition of Carbonic Anhydrases (CAs) has been clinically exploited for many decades for a variety of therapeutic applications. Within a research project aimed at developing novel classesExpand
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Novel 4/3-((4-oxo-5-(2-oxoindolin-3-ylidene)thiazolidin-2-ylidene)amino) benzenesulfonamides: Synthesis, carbonic anhydrase inhibitory activity, anticancer activity and molecular modelling studies.
Herein we report the synthesis of two series of novel 4/3-((4-oxo-5-(2-oxoindolin-3-ylidene)thiazolidin-2-ylidene)amino)benzenesulfonamides (4a-m and 7a-g). All the newly prepared sulfonamides wereExpand
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Carbonic anhydrase inhibitors as antitumor/antimetastatic agents: a patent review (2008–2018)
ABSTRACT Introduction: Human carbonic anhydrases (CA, EC 4.2.1.1) IX and XII are tumor-associated proteins, being part of the molecular machinery that tumor cells build as adaptive responses toExpand
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Benzenesulfonamides Incorporating Flexible Triazole Moieties Are Highly Effective Carbonic Anhydrase Inhibitors: Synthesis and Kinetic, Crystallographic, Computational, and Intraocular Pressure
Herein we report the synthesis of two series of benzenesulfonamide containing compounds that incorporate the phenyl-1,2,3-triazole moieties. We explored the insertion of appropriate linkers, such asExpand
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