Intermolecular amination of allylic and benzylic alcohols leads to effective inhibitions of acetylcholinesterase enzyme and carbonic anhydrase I and II isoenzymes

2018 ◽  
Vol 32 (8) ◽  
pp. e22173 ◽  
Author(s):  
Ufuk Atmaca ◽  
Alper Yıldırım ◽  
Parham Taslimi ◽  
Seda Tuncel Çelik ◽  
İlhami Gülçin ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Benzylic Alcohols ◽  
Carbonic Anhydrase I ◽  
Acetylcholinesterase Enzyme

scholarly journals Synthesis and Human Carbonic Anhydrase I, II, IX, and XII Inhibition Studies of Sulphonamides Incorporating Mono-, Bi- and Tricyclic Imide Moieties

2021 ◽  
Vol 14 (7) ◽  
pp. 693
Author(s):  
Kalyan K. Sethi ◽  
KM Abha Mishra ◽  
Saurabh M. Verma ◽  
Daniela Vullo ◽  
Fabrizio Carta ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Carbonic Anhydrase ◽  
Docking Studies ◽  
Carbonic Anhydrases ◽  
Molecular Docking Studies ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Carbonic Anhydrase I ◽  
Human Carbonic Anhydrase ◽  
Inhibition Studies

New derivatives were synthesised by reaction of amino-containing aromatic sulphonamides with mono-, bi-, and tricyclic anhydrides. These sulphonamides were investigated as human carbonic anhydrases (hCAs, EC 4.2.1.1) I, II, IX, and XII inhibitors. hCA I was inhibited with inhibition constants (Kis) ranging from 49 to >10,000 nM. The physiologically dominant hCA II was significantly inhibited by most of the sulphonamide with the Kis ranging between 2.4 and 4515 nM. hCA IX and hCA XII were inhibited by these sulphonamides in the range of 9.7 to 7766 nM and 14 to 316 nM, respectively. The structure–activity relationships (SAR) are rationalised with the help of molecular docking studies.

Crystal analysis of aromatic sulfonamide binding to native and (Zn)2 adduct of human carbonic anhydrase I Michigan 1

2002 ◽  
Vol 339 ◽  
pp. 135-144 ◽  
Author(s):  
Marta Ferraroni ◽  
Fabrizio Briganti ◽  
W.Richard Chegwidden ◽  
Claudiu T. Supuran ◽  
Andrea Scozzafava
Keyword(s):  
Carbonic Anhydrase ◽  
Carbonic Anhydrase I ◽  
Human Carbonic Anhydrase ◽  
Aromatic Sulfonamide

scholarly journals Synthesis and carbonic anhydrase I, II, IX and XII inhibitory activity of sulfamates incorporating piperazinyl-ureido moieties

2015 ◽  
Vol 23 (17) ◽  
pp. 5619-5625 ◽  
Author(s):  
Cenzo Congiu ◽  
Valentina Onnis ◽  
Alessandro Deplano ◽  
Gianfranco Balboni ◽  
Mariangela Ceruso ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Inhibitory Activity ◽  
Carbonic Anhydrase I

Carbonic anhydrase I and II activation with mono- and dihalogenated histamine derivatives

2011 ◽  
Vol 21 (16) ◽  
pp. 4884-4887 ◽  
Author(s):  
Mohamed-Chiheb Saada ◽  
Daniela Vullo ◽  
Jean-Louis Montero ◽  
Andrea Scozzafava ◽  
Jean-Yves Winum ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Carbonic Anhydrase I

A simple enzyme-linked immunoassay of human carbonic anhydrase I for the study of developing erythroid cells

1990 ◽  
Vol 191 (3) ◽  
pp. 169-174 ◽  
Author(s):  
Takahito Kondo ◽  
Kazuhiro Murakami ◽  
Hiroshi Isobe ◽  
Naoyuki Taniguchi ◽  
Yoshikazu Kawakami
Keyword(s):  
Carbonic Anhydrase ◽  
Erythroid Cells ◽  
Carbonic Anhydrase I ◽  
Human Carbonic Anhydrase

scholarly journals Carbonic Anhydrase I as a New Plasma Biomarker for Prostate Cancer

ISRN Oncology ◽  
2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Michiko Takakura ◽  
Akira Yokomizo ◽  
Yoshinori Tanaka ◽  
Michimoto Kobayashi ◽  
Giman Jung ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Carbonic Anhydrase ◽  
Cancer Patients ◽  
Plasma Proteins ◽  
Specific Antigen ◽  
Healthy Controls ◽  
Gray Zone ◽  
Plasma Biomarker ◽  
Carbonic Anhydrase I ◽  
Discrimination Rate

Serum prostate-specific antigen (PSA) levels ranging from 4 to 10 ng/mL is considered a diagnostic gray zone for detecting prostate cancer because biopsies reveal no evidence of cancer in 75% of these subjects. Our goal was to discover a new highly specific biomarker for prostate cancer by analyzing plasma proteins using a proteomic technique. Enriched plasma proteins from 25 prostate cancer patients and 15 healthy controls were analyzed using a label-free quantitative shotgun proteomics platform called 2DICAL (2-dimensional image converted analysis of liquid chromatography and mass spectrometry) and candidate biomarkers were searched. Among the 40,678 identified mass spectrum (MS) peaks, 117 peaks significantly differed between prostate cancer patients and healthy controls. Ten peaks matched carbonic anhydrase I (CAI) by tandem MS. Independent immunological assays revealed that plasma CAI levels in 54 prostate cancer patients were significantly higher than those in 60 healthy controls (, Mann-Whitney test). In the PSA gray-zone group, the discrimination rate of prostate cancer patients increased by considering plasma CAI levels. CAI can potentially serve as a valuable plasma biomarker and the combination of PSA and CAI may have great advantages for diagnosing prostate cancer in patients with gray-zone PSA level.

scholarly journals New Histamine-Related Five-Membered N-Heterocycle Derivatives as Carbonic Anhydrase I Activators

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 545
Author(s):  
Niccolò Chiaramonte ◽  
Alessio Gabellini ◽  
Andrea Angeli ◽  
Gianluca Bartolucci ◽  
Laura Braconi ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Imidazole Ring ◽  
Aliphatic Chain ◽  
Amino Group ◽  
Carbonic Anhydrase I ◽  
Terminal Amino ◽  
Human Carbonic Anhydrase ◽  
New Compounds ◽  
Related Compounds ◽  
Micromolar Range

A series of histamine (HST)-related compounds were synthesized and tested for their activating properties on five physiologically relevant human Carbonic Anhydrase (hCA) isoforms (I, II, Va, VII and XIII). The imidazole ring of HST was replaced with different 5-membered heterocycles and the length of the aliphatic chain was varied. For the most interesting compounds some modifications on the terminal amino group were also performed. The most sensitive isoform to activation was hCA I (KA values in the low micromolar range), but surprisingly none of the new compounds displayed activity on hCA II. Some derivatives (1, 3a and 22) displayed an interesting selectivity for activating hCA I over hCA II, Va, VII and XIII.

scholarly journals Synthesis of Novel Selenides Bearing Benzenesulfonamide Moieties as Carbonic Anhydrase I, II, IV, VII, and IX Inhibitors

2017 ◽  
Vol 8 (12) ◽  
pp. 1213-1217 ◽  
Author(s):  
Andrea Angeli ◽  
Damiano Tanini ◽  
Antonella Capperucci ◽  
Claudiu T. Supuran
Keyword(s):  
Carbonic Anhydrase ◽  
Carbonic Anhydrase I
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