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Journal ArticleDOI

Synthesis of novel acridine and bis acridine sulfonamides with effective inhibitory activity against the cytosolic carbonic anhydrase isoforms II and VII

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TLDR
The structure-activity relationships for the inhibition of these isoforms with the acridine-sulfonamides reported here were elucidated and more precisely the cytosolic isoforms hCA I, II and VII.
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This article is published in Bioorganic & Medicinal Chemistry.The article was published on 2013-09-15. It has received 33 citations till now. The article focuses on the topics: Acridine & Carbonic anhydrase.

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Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review.

TL;DR: A comprehensive review highlights the recent developments of sulfonyl or sulfonamides based compounds in huge range of therapeutic applications such as antimicrobial, anti-inflammatory, antiviral, anticonvulsant, antitubercular, antidiabetic, antileishmanial, carbonic anhydrase, antimalarial, anticancer and other medicinal agents.
Journal ArticleDOI

Recent developments in the synthesis and biological activity of acridine/acridone analogues

TL;DR: This survey describes acridine and acridone derivatives reported since 2013, methods of their synthesis and their potential clinical applications, as well as investigating their clinical application in Alzheimer's disease and other diseases.
Journal ArticleDOI

Oxidation of cyanobenzocycloheptatrienes: Synthesis, photooxygenation reaction and carbonic anhydrase isoenzymes inhibition properties of some new benzotropone derivatives.

TL;DR: The oxidation of some cyanocycloheptatrienes with CrO3 and pyridine was investigated and a few new nitrile functionalised benzotropone derivatives were obtained and the structures of the formed products were determined on the basis of NMR spectroscopy.
Journal ArticleDOI

One-pot, efficient and green synthesis of acridinedione derivatives using highly monodisperse platinum nanoparticles supported with reduced graphene oxide

TL;DR: In this paper, an efficient, high yielding, quick method has been developed for the synthesis of acridinedione derivatives via a one-pot, multi-component condensation of dimedone (1), various aromatic aldehydes (2), and various aromatic amines (3a,b) using highly monodisperse platinum nanoparticles supported with reduced graphene oxide (Pt NPs@rGO) as a recyclable heterogeneous catalyst.
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Pt NPs@GO as a highly efficient and reusable catalyst for one-pot synthesis of acridinedione derivatives

TL;DR: Graphene oxide decorated with platinum nanoparticles (Pt NPs@GO) has been used for the first time as a highly stable, exceptionally reusable, isolable, bottleable, long-lived and highly efficient catalyst for the synthesis of acridinedione derivatives from dimedone, aromatic aldehydes and various amines with great catalytic performance.
References
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Journal ArticleDOI

Carbonic anhydrases: novel therapeutic applications for inhibitors and activators

TL;DR: The biological rationale for the novel uses of inhibitors or activators of CA activity in multiple diseases is discussed, and progress in the development of specific modulators of the relevant CA isoforms is highlighted, some of which are now being evaluated in clinical trials.
Journal ArticleDOI

The Carbon Dioxide Hydration Activity of Carbonic Anhydrase I. STOP-FLOW KINETIC STUDIES ON THE NATIVE HUMAN ISOENZYMES B AND C

TL;DR: The present kinetic results are interpreted as representing a great specificity of carbonic anhydrase for the binding of its substrate CO2, and it is proposed that the enzyme-catalyzed hydration of CO2 requires, not only water activation by a basic group, but also charge neutralization in the transition state by an electron acceptor function.
Journal ArticleDOI

Interfering with pH regulation in tumours as a therapeutic strategy

TL;DR: Key pH regulators in tumour cells include: isoforms 2, 9 and 12 of carbonic anhydrase, isoforms of anion exchangers, Na+/HCO3− co-transporters, Na+./H+ exchanger, monocarboxylate transporters and the vacuolar ATPase.
PatentDOI

Carbonic anhydrase inhibitors

TL;DR: A carbonic anhydrase IX (CA IX) inhibitor is a compound of general formula: R-NH-CX-NH-(CH 2 ) n -Ar-Q-SO 2 -NH 2 or a pharmaceutically acceptable salt, derivative or prodrug thereof.
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