Search

The secondary sulfonamide derivatives containing benzothiazole scaffold (1–10) were synthesized to determine their inhibition properties on two physiologically essential human carbonic anhydrases isoforms (hCAs, EC, 4.2.1.1), hCA I, and hCA II. The inhibitory effects of the compounds on hCA I and hCA II isoenzymes were investigated by comparing their IC50 and Ki values. The Ki values of compounds (1–10) against hCA I and hCA II are in the range of 0.052 ± 0.022–0.971 ± 0.280 and 0.025 ± 0.010–0.682 ± 0.335, respectively. Some of these inhibited the enzyme more effectively than the standard drug, acetazolamide. In particular, compounds 5 and 4 were found to be most effective on hCA I and hCA II. [ABSTRACT FROM AUTHOR]

Quinazoline and quinazolinone derivatives display an extensive application in organic and pharmaceutical chemistry, and they have been used as natural and synthetic materials for medicinal chemistry purposes. Here I reported an investigation of a new series of quinazolinone ring derivatives. In this context, starting from the methyl anthranilate, six quinazolinone derivatives (4a-f) with various aminomethyl moieties at position 2 were synthesized (89-80%). The structures of compounds 4a-f were identified using FTIR and NMR Spectroscopy (¹H NMR - 13C NMR). The data obtained from the all spectra clearly identify the structures of the compounds. [ABSTRACT FROM AUTHOR]