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1.
Expert Opin Ther Pat ; 34(6): 401-414, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38439633

ABSTRACT

INTRODUCTION: Antibacterial photodynamic therapy presents a promising alternative to antibiotics, with potential against multidrug-resistant bacteria, offering broad-spectrum action, reduced resistance risk, and improved tissue selectivity. AREAS COVERED: This manuscript reviews patent literature in the field of antibacterial photodynamic therapy through the period of 2019-2023. All data are from the US and European patent databases and SciFinder. EXPERT OPINION: Antibacterial photodynamic therapy (PDT) is an appealing approach for treating bacterial infections, especially biofilm-related ones, by releasing reactive oxygen species (ROS) upon light activation. Its success is driven by a growing variety of photosensitizers (PSs) with tailored properties, like water solubility, controllable surface charge, and ROS generation efficiency. Among them, Aggregation Induced Emission (AIE)-type PSs are promising, demonstrating enhanced efficacy when aggregated in biological environments. However, the penetration of pristine PSs into bacterial biofilms within deep tissues or complex anatomical regions is limited, reducing their antibacterial effectiveness. To address this, nanotechnology has been integrated into antibacterial PDT to synthesize various nano-PSs. This adaptability allows seamless integration with other antimicrobial treatments, offering a comprehensive approach to combat localized infections, especially in dentistry and dermatology. By combining PSs with complementary therapies, antibacterial PDT offers a multifaceted strategy for effective microbial control and management.


Subject(s)
Anti-Bacterial Agents , Bacterial Infections , Biofilms , Patents as Topic , Photochemotherapy , Photosensitizing Agents , Reactive Oxygen Species , Humans , Photosensitizing Agents/pharmacology , Anti-Bacterial Agents/pharmacology , Bacterial Infections/drug therapy , Bacterial Infections/microbiology , Biofilms/drug effects , Animals , Reactive Oxygen Species/metabolism , Drug Resistance, Multiple, Bacterial , Nanotechnology
2.
Bioorg Med Chem Lett ; 18(12): 3475-80, 2008 Jun 15.
Article in English | MEDLINE | ID: mdl-18513964

ABSTRACT

A series of spin-labeled sulfonamides incorporating TEMPO moieties were synthesized by a procedure involving the formation of a thiourea functionality between the benzenesulfonamide and free radical fragment of the molecules. The new compounds were tested as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) and showed efficient inhibition of the physiologically relevant isozymes hCA II and hCA IX (hCA IX being predominantly found in tumors) and moderate to weak inhibitory activity against hCA I. Some derivatives were also selective for inhibiting the tumor-associated isoform over the cytosolic one CA II, and presented significant changes in their ESR signals when complexed to the enzyme active site, being interesting candidates for the investigation of hypoxic tumors overexpressing CA IX by ESR techniques, as well as for imaging/treatment purposes.


Subject(s)
Carbonic Anhydrase Inhibitors/chemical synthesis , Carbonic Anhydrase Inhibitors/pharmacology , Carbonic Anhydrases/drug effects , Cyclic N-Oxides/chemistry , Sulfonamides/chemical synthesis , Sulfonamides/pharmacology , Antigens, Neoplasm/chemistry , Antigens, Neoplasm/drug effects , Carbonic Anhydrase II/antagonists & inhibitors , Carbonic Anhydrase II/chemistry , Carbonic Anhydrase IX , Carbonic Anhydrase Inhibitors/chemistry , Carbonic Anhydrases/chemistry , Cell Membrane/drug effects , Cell Membrane/enzymology , Cytosol/drug effects , Cytosol/enzymology , Drug Design , Drug Evaluation, Preclinical , Free Radicals/chemical synthesis , Free Radicals/chemistry , Free Radicals/pharmacology , Humans , Isoenzymes/antagonists & inhibitors , Isoenzymes/chemistry , Molecular Structure , Recombinant Proteins/drug effects , Spin Labels , Stereoisomerism , Structure-Activity Relationship , Sulfonamides/chemistry
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