Three new aromatic sulfonamide inhibitors of carbonic anhydrases I, II, IV and XII

7-Aryl-triazolyl-substituted sulfocoumarins are potent, selective inhibitors of the tumor-associated carbonic anhydrase IX and XII

“…Since many CA isoforms are involved in diverse physio/pathological conditions such as glaucoma (hCA I, II, IV and XII), edema (hCA II, IV, XIV as the most important), central nervous system (CNS)-related pathologies (hCAVII and XIV are particularly involved in the epilepsy) and tumors (hCA IX and hCA XII are strictly associated with hypoxic tumors), it is not surprising that CAIs are used in the clinic for some applications for almost 70 years [18][19][20][21][22][23][24] . Many synthetic efforts have been made for the development of specific CAIs: in the last 15 years, in addition to the classical ''tail approach'' [10][11][12][13][14][15][16][17][25][26][27][28] which is mainly applied to classical sulfonamide inhibitors and their isosters, novel CAIs scaffolds have been also identified such as the polyamines 29 , phenols [30][31][32] , dithiocarbamates [33][34][35][36] , xanthates 37 , coumarins, thiocoumarins, 2-thioxocoumarins, coumarine oximes 4,38,39 . Sulfocoumarins are the latest CAI class identified and similarly to the coumarins showed the most selective inhibition profiles against the pathologically valuable CA isoforms 1,9,[40][41][42][43][44] .…”

A magnificent enzyme superfamily: carbonic anhydrases, their purification and characterization

“…Apart from the classical applications of the CA inhibitors (CAIs) as diuretics, antiglaucoma and antiepileptic agents [83][84][85][86][87][88][89][90][91] of pharmaceuticals that suppress the activity of carbonic anhydrase, ultimately many such agents were shown to be effective as antiobesity and anticancer agents [91][92][93] . Moreover, the inhibition of CAs from pathogenic organisms (such as bacteria, fungi and protozoa) started to be considered as an interesting approach for designing anti-infective agents with a new mechanism of action [1][2][3]94 .…”

The history and rationale of using carbonic anhydrase inhibitors in the treatment of peptic ulcers. In memoriam Ioan Puşcaş (1932–2015)

“…Only hCA VB and especially hCA II, one of the best catalysts known in nature, show a better activity than HpbCA [38][39][40][41] . Also, it may be observed that the activity of all these enzymes is inhibited by the CA inhibitor (CAI) par excellence, the sulfonamide drug, acetazolamide AAZ [53][54][55][56][57] , which may explain why Ulcosilvanil showed a range of severe side effects, due to inhibition of CA isoforms in other organs than the stomach, or better to say, due to hCAs and not Hpa/bCA inhibition (Table 3).…”