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Research Article

Synthesis and evaluation of new thiadiazole derivatives as potential inhibitors of human carbonic anhydrase isozymes (hCA-I and hCA-II)

Mehlika Dilek AltintopFaculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, Eskisehir, Turkey,

Ahmet OzdemirFaculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, Eskisehir, Turkey,

Kaan KucukogluFaculty of Pharmacy, Department of Pharmaceutical Chemistry, Ataturk University, Erzurum, Turkey,

Gulhan Turan-ZitouniFaculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, Eskisehir, Turkey,

Hayrunnisa NadarogluErzurum Vocational Training School, Department of Food Technology, Ataturk University, Erzurum, Turkey, and

Zafer Asim KaplancikliFaculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, Eskisehir, Turkey, ;Graduate School of Health Sciences, Department of Pharmaceutical Chemistry, Anadolu University, Eskisehir, TurkeyCorrespondence[email protected]

Figures & data

Figure 1. Chemical structure of the clinically used sulfonamide acetazolamide (AAZ).

Scheme 1. The synthetic route for the preparation of the thiadiazole derivatives (3a–s). Reagents and conditions: (i) NH₂NH₂ ċ H₂O, ethanol, rt, 5 h; (ii) (1) CS₂/NaOH, ethanol, reflux, 10 h; (2) HCl, pH 4–5; (iii) PhCOCH₂Br, K₂CO₃, acetone, rt, 8 h.

Scheme 1. The synthetic route for the preparation of the thiadiazole derivatives (3a–s). Reagents and conditions: (i) NH2NH2 ċ H2O, ethanol, rt, 5 h; (ii) (1) CS2/NaOH, ethanol, reflux, 10 h; (2) HCl, pH 4–5; (iii) PhCOCH2Br, K2CO3, acetone, rt, 8 h.

Table 1. Physicochemical properties of the compounds (3a–s).

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Table 2. Summary of purification for hCA-I and hCA-II from human erythrocyte.

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**Table 3. IC₅₀ values for the in vitro inhibition of hCA-I and hCA-II with compounds 3a–s.**

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Synthesis and evaluation of new thiadiazole derivatives as potential inhibitors of human carbonic anhydrase isozymes (hCA-I and hCA-II)

Table 1. Physicochemical properties of the compounds (3a–s).

Table 2. Summary of purification for hCA-I and hCA-II from human erythrocyte.

**Table 3. IC₅₀ values for the in vitro inhibition of hCA-I and hCA-II with compounds 3a–s.**

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Synthesis and evaluation of new thiadiazole derivatives as potential inhibitors of human carbonic anhydrase isozymes (hCA-I and hCA-II)

Figures & data

Table 1. Physicochemical properties of the compounds (3a–s).

Table 2. Summary of purification for hCA-I and hCA-II from human erythrocyte.

Table 3. IC50 values for the in vitro inhibition of hCA-I and hCA-II with compounds 3a–s.

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**Table 3. IC₅₀ values for the in vitro inhibition of hCA-I and hCA-II with compounds 3a–s.**