RESUMO
Novel chiral benzimidazole amine hybrids (4a-4d) were synthesized from commercially available amine [(R)- (+)-phenylethylamine, (-) (S)-(-)-phenylethylamine, (-) (R)-(-)-cyclohexylethylamine, (S)-(+)-cyclohexylethylamine] and 2-(chloromethyl)-N-tosyl-1H-benzimidazole. The synthesized compounds (4a-4d) were characterized by IR, NMR, and LC/MS analysis. The inhibitory effect of 4a-4d on human erythrocytes carbonic anhydrase I (hCA-I), II (hCA-II), and acetylcholinesterase (AChE) activity was investigated. For hCA-I, the IC50 values of 4a-4d were found to be 4.895â µM, 1.750â µM, 0.173â µM, and 0.620â µM, respectively, and for hCA-II, the IC50 values of 4a-4d were found to be 0.469â µM, 0.380â µM, 0.233â µM, 0.635â µM, respectively. Furthermore, IC50 values of 4a-4d on AChE were found as 87.5â nM, 100â nM, 26.92â nM, and 100â nM, respectively. In addition, molecular docking analysis was performed to evaluate the affinity of 4a-4d against hCA-I, hCA-II, and AChE and explain their binding interactions.
Assuntos
Acetilcolinesterase , Inibidores da Anidrase Carbônica , Humanos , Inibidores da Anidrase Carbônica/química , Acetilcolinesterase/metabolismo , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/química , Anidrase Carbônica I , Simulação de Acoplamento Molecular , Anidrase Carbônica II , Eritrócitos/metabolismo , Fenetilaminas , Benzimidazóis/farmacologia , Relação Estrutura-Atividade , Estrutura MolecularRESUMO
Environmental awareness increased the demand for the biomass based materials with superior properties instead of petroleum products. This study aims to prepare starch networks as sorbents for the removal of polycyclic aromatic hydrocarbons (PAHs). Two types of crosslinker, epichlorohydrine (ECH) and glutaraldehyde (GA), were choosed for the preparation of Gel-E and Gel-G networks, respectively. Rheological, swelling and morphological properties of the resulted materials were investigated as a function of various reaction parameters as starch, crosslinker and base concentration and also reaction temperature. The rheological measurements showed that while network formation of Gel-E hydrogels was strongly affected by the NaOH and starch concentration, the strength of the Gel-G hydrogels mainly depends on the crosslinker amount. Starch networks showed high PAH sorption capacities up to 1.42 g per gram sorbent with three model PAH molecules. Although PAH sorption capacities of the Gel-E networks are higher than those of Gel-G gels due to the pore sizes differences of the gel samples, both of them are promising materials as biosorbent for the PAH sorption applications due to the relatively high sorption capacities, low cost and simple preparation methods.