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1.	Saeed, Aamer, et al. (author) Novel N-(benzo[d]oxazol-2-yl)alkanamides : synthesis and carbonic anhydrase II inhibition studies 2020 In: Journal of Heterocyclic Chemistry. - : WILEY. - 0022-152X .- 1943-5193. ; 57:7, s. 2831-2843 Journal article (peer-reviewed)abstract Carbonic anhydrase (CA II) inhibitors are very important therapeutic targets in drug design for treatment of neuropathic pain and in eradication of glaucoma, cancer, epilepsy, ulcer and obesity. In this study, some two2-substituted benzoxazoles (3a-j) were developed as a new family of carbonic anhydrase II inhibitors by employing acyl thiourea chemistry via a simple and expedient protocol and evaluated for CA II inhibitor activity and radical scavenging ability. Compounds 3f and 3j were found to be the most potent inhibitors, with IC50 values of 0.00564 and 0.00596 mu M, respectively which are several times better than that of the standard, acetazolamide (IC50 value 0.997 +/- 0.0586 mu M). Docking experiments were carried out against the carbonic anhydrase II crystal structure to better rationalize the inhibitory activities of these new structures. Moreover, the results of a DPPH radical scavenging assay showed that the antioxidant profile of compound 3i is superior to those of other derivatives. The results have revealed that derivatives 3f and 3j behave as CA-II inhibitors significantly better than standard and 3i has good anti-oxidation potential.

Saeed, Aamer, et al. (author)
Novel N-(benzo[d]oxazol-2-yl)alkanamides : synthesis and carbonic anhydrase II inhibition studies
2020
In: Journal of Heterocyclic Chemistry. - : WILEY. - 0022-152X .- 1943-5193. ; 57:7, s. 2831-2843
Journal article (peer-reviewed)abstract
- Carbonic anhydrase (CA II) inhibitors are very important therapeutic targets in drug design for treatment of neuropathic pain and in eradication of glaucoma, cancer, epilepsy, ulcer and obesity. In this study, some two2-substituted benzoxazoles (3a-j) were developed as a new family of carbonic anhydrase II inhibitors by employing acyl thiourea chemistry via a simple and expedient protocol and evaluated for CA II inhibitor activity and radical scavenging ability. Compounds 3f and 3j were found to be the most potent inhibitors, with IC50 values of 0.00564 and 0.00596 mu M, respectively which are several times better than that of the standard, acetazolamide (IC50 value 0.997 +/- 0.0586 mu M). Docking experiments were carried out against the carbonic anhydrase II crystal structure to better rationalize the inhibitory activities of these new structures. Moreover, the results of a DPPH radical scavenging assay showed that the antioxidant profile of compound 3i is superior to those of other derivatives. The results have revealed that derivatives 3f and 3j behave as CA-II inhibitors significantly better than standard and 3i has good anti-oxidation potential.

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