Bioorganometallic derivatives of 4-hydrazino-benzenesulphonamide as carbonic anhydrase inhibitors: synthesis, characterisation and biological evaluation
A series of bio-organometallic-hydrazones of the general formula [{(η5-C5H4)-C(R)=N-N(H)-C6H4-4-SO2NH2}]MLn(MLn = Re(CO)3, Mn(CO)3, FeCp; R=H, CH3) were prepared by reaction of formyl/acetyl organometallic precursors with 4-hydrazino-benzenesulphonamide. All compounds were characterized by conventio...
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Taylor & Francis Group,
2020-01-01T00:00:00Z.
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|---|---|---|---|
| 001 | doaj_e4e17d4a27ad4436a3ad8d4f759a898b | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Jeremie Brichet |e author |
| 700 | 1 | 0 | |a Rodrigo Arancibia |e author |
| 700 | 1 | 0 | |a Emanuela Berrino |e author |
| 700 | 1 | 0 | |a Claudiu T. Supuran |e author |
| 245 | 0 | 0 | |a Bioorganometallic derivatives of 4-hydrazino-benzenesulphonamide as carbonic anhydrase inhibitors: synthesis, characterisation and biological evaluation |
| 260 | |b Taylor & Francis Group, |c 2020-01-01T00:00:00Z. | ||
| 500 | |a 1475-6366 | ||
| 500 | |a 1475-6374 | ||
| 500 | |a 10.1080/14756366.2020.1724995 | ||
| 520 | |a A series of bio-organometallic-hydrazones of the general formula [{(η5-C5H4)-C(R)=N-N(H)-C6H4-4-SO2NH2}]MLn(MLn = Re(CO)3, Mn(CO)3, FeCp; R=H, CH3) were prepared by reaction of formyl/acetyl organometallic precursors with 4-hydrazino-benzenesulphonamide. All compounds were characterized by conventional spectroscopic techniques (infra-red, 1H and 13C NMR, mass spectrometry and elemental analysis). Biological evaluation as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors agents was carried out using four human/h) isoforms, hCA I, II, IX and XII. The cytosolic isoforms hCA I and II were effectively inhibited by almost all derivatives with inhibition constants of 1.7-22.4 nM. Similar effects were observed for the tumour-associated transmembrane isoform hCA XII (KIs of 1.9-24.4 nM). hCA IX was less sensitive to inhibition with these compounds. The presence of bio-organometallic or metallo-carbonyl moieties in the molecules of these CAIs makes them amenable for interesting pharmacologic applications, for example for compounds with CO donating properties. | ||
| 546 | |a EN | ||
| 690 | |a bioorganometallic-hydrazones | ||
| 690 | |a sulphanilamide | ||
| 690 | |a carbonic anhydrase | ||
| 690 | |a inhibitors | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 622-628 (2020) | |
| 787 | 0 | |n http://dx.doi.org/10.1080/14756366.2020.1724995 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6366 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6374 | |
| 856 | 4 | 1 | |u https://doaj.org/article/e4e17d4a27ad4436a3ad8d4f759a898b |z Connect to this object online. |