Inhibitory Binding of Angiotensin Converting Enzyme Inhibitors with Carbonic Anhydrase III

Daoud, Nour El-Huda; Alzweiri, Muhammed

doi:10.1007/s10337-020-03973-1

Cited by 4 publications

(3 citation statements)

References 35 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The fluctuation in the amount of the volatile chemical reflects the tested drug's action against CAs [17]. Captopril was employed as a positive control because, as previously documented by our research, it has strong action against CA [4]. (17.49%).…”

Section: Inhibition Of Enzyme Activitymentioning

confidence: 89%

“…CAs catalyze the reaction involving the conversion of carbon dioxide to bicarbonate and protons, which is essential for pH regulation, electrolytes, gases, and anion balance [1,3]. Furthermore, CAs exhibit weak esterase activity [4].…”

Section: Introductionmentioning

confidence: 99%

“…Sulfonamides, dithiocarbamates, and thiols were reported to show activity on fungi such as candida albican [9]. α-CA isoform is expressed in human cells and has a significant role in human pathology [4]. Human CA inhibitors such as sulfonamides have been in clinical use for decades as diuretics, anti-obesity, antiglaucoma, antiepileptic, and even anti-cancer [1,10], [11][12][13].…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Synthesis and Biological Evaluation of Carbonic Anhydrase III and IX Inhibitors using Gas Chromatography with Modified pH Sensitive Pellets

Hussein,

Bourghli,

Alzweiri

et al. 2023

Jordan j. pharm. sci.

View full text Add to dashboard Cite

Fifteen compounds were synthesized and tested as potential carbonic anhydrase III (CAIII) and carbonic anhydrase IX (CAIX) inhibitors, six of which are novel. Amides (a1-4), hydroxamic acids (b1-2), and imines (c1-9) derivatives were evaluated for their inhibitory activity against CAII and CAIX using gas chromatography with modified pH-sensitive pellets. The derivatives showed inhibition percentages between 12-56% for CAIII and 44-59% for CAIX, compared to 49% and 63% for captopril (the positive control), respectively. Imines showed the best inhibition of CAIII, while all derivatives showed comparable activity against CAIX. It is hypothesized that the nitrogen atom in imine, amide, or hydroxamic acid moieties in the vicinity of an ionizable group is in coordination with the zinc ion in the active site. Furthermore, the candidates were tested for their antimicrobial and antifungal activity. Generally, they showed low to zero activity against some gram-positive and negative bacteria. This supports the theory of their ability to bind to human carbonic anhydrase but not to bacterial one. These compounds could serve as useful scaffolds to develop more potent and selective carbonic anhydrase inhibitors as anti-obesity and anticancer candidates.

show abstract

Section: Inhibition Of Enzyme Activitymentioning

confidence: 89%