Advances in the structural annotation of human carbonic anhydrases and impact on future drug discovery

A Nocentini, CT Supuran - Expert Opinion on Drug Discovery, 2019 - Taylor & Francis
Introduction: Of the 15 human carbonic anhydrase (CA, EC 4.2. 1.1) isoforms known to date,
for 11 the crystal structure is known. Many different classes of CA inhibitors (CAIs) were …

Activation of α-, β-, γ-δ-, ζ-and η-class of carbonic anhydrases with amines and amino acids: A review

S Akocak, CT Supuran - Journal of enzyme inhibition and …, 2019 - Taylor & Francis
Eight genetically distinct carbonic anhydrase (EC 4.2. 1.1) enzyme families (α-, β-, γ-δ-, ζ-, η-
, θ-and ι-CAs) were described to date. On the other hand, 16 mammalian α-CA isoforms are …

3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and …

MF Abo-Ashour, WM Eldehna, A Nocentini… - European Journal of …, 2019 - Elsevier
Herein we describe the design and synthesis of two series of sulfonamides featuring N-
unsubstituted (4a-c) or N-substituted (7a-o) isatin moieties (as tails) connected to …

Continued exploration and tail approach synthesis of benzenesulfonamides containing triazole and dual triazole moieties as carbonic anhydrase I, II, IV and IX …

L Vats, R Kumar, S Bua, A Nocentini, P Gratteri… - European Journal of …, 2019 - Elsevier
A library of twenty two novel 1, 2, 3-triazole benzenesulfonamides incorporating
thiosemicarbazide, 5 (4 H)-thione-1, 2, 4-triazole and variously substituted phenacyl …

Bioisosteric development of multitarget nonsteroidal anti-inflammatory drug–carbonic anhydrases inhibitor hybrids for the management of rheumatoid arthritis

S Bua, L Lucarini, L Micheli, M Menicatti… - Journal of Medicinal …, 2019 - ACS Publications
Multitarget nonsteroidal anti-inflammatory drug (NSAID)–carbonic anhydrase inhibitor (CAI)
agents for the management of rheumatoid arthritis are reported. The evidence of the plasma …

Carbonic anhydrases: An overview

A Nocentini, CT Supuran - Carbonic Anhydrases, 2019 - Elsevier
Abstract Carbonic anhydrases (CAs, EC 4.2. 1.1) catalyze the interconversion between CO 2
and bicarbonate as well as other hydrolytic reactions. Seven genetic families of CAs have …

Synthesis, biological evaluation and in silico studies with 4-benzylidene-2-phenyl-5 (4H)-imidazolone-based benzenesulfonamides as novel selective carbonic …

WM Eldehna, MA Abdelrahman, A Nocentini, S Bua… - Bioorganic …, 2019 - Elsevier
In the presented work, we report the synthesis of a series of 4-benzylidene-2-phenyl-5 (4H)-
imidazolone-based benzenesulfonamides 7a-f via the Erlenmeyer–Plöchl reaction. All the …

Synthesis and comparative carbonic anhydrase inhibition of new Schiff's bases incorporating benzenesulfonamide, methanesulfonamide, and methylsulfonylbenzene …

AS El-Azab, AM Alaa, S Bua, A Nocentini… - Bioorganic …, 2019 - Elsevier
Herein, we report the synthesis, characterization, and carbonic anhydrase (CA) inhibition of
the newly synthesized Schiff's bases 4–18 with benzenesulfonamide, methanesulfonamide …

Novel diamide-based benzenesulfonamides as selective carbonic anhydrase IX inhibitors endowed with antitumor activity: synthesis, biological evaluation and in …

MA Abdelrahman, WM Eldehna, A Nocentini… - International Journal of …, 2019 - mdpi.com
In this work, we present the synthesis and biological evaluation of novel series of diamide-
based benzenesulfonamides 5a–h as inhibitors of the metalloenzyme carbonic anhydrase …

Synthesis and biological evaluation of novel 3-(quinolin-4-ylamino) benzenesulfonamides as carbonic anhydrase isoforms I and II inhibitors

MM Al-Sanea, A Elkamhawy, S Paik, S Bua… - Journal of enzyme …, 2019 - Taylor & Francis
Abstract Carbonic anhydrases (CAs, EC 4.2. 1.1) are crucial metalloenzymes that are
involved in diverse bioprocesses. We report the synthesis and biological evaluation of novel …