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1.
Curr Org Synth ; 20(4): 365-375, 2023.
Article in English | MEDLINE | ID: mdl-35748544

ABSTRACT

BACKGROUND: In this paper, a novel catalyst is synthesized and characterized by immobilizing copper onto imidazopyridine-modified superparamagnetic iron oxide nanoparticles (SPION). METHODS: The catalyst is characterized by several methods, including TEM, SEM, ICP, DLS, and VSM. The catalytic activity of the catalyst is evaluated in the synthesis of thiosolfunamide. The synthesized catalyst showed very good activity in the mentioned reaction and performance for synthesizing the desired products in high isolated yields. RESULTS: For the synthesis of the products, sequential transformations enable the facile synthesis of complex target molecules from simple building blocks in a single preparative step. CONCLUSION: The reaction can be performed with a high yield using water and ethanol as the reaction green solvent using terminal alkynes and sulfonyl azides as starting materials. The reusability of the catalyst was tested, and the results proved high reusability of the catalyst.

2.
Sci Rep ; 12(1): 10569, 2022 06 22.
Article in English | MEDLINE | ID: mdl-35732907

ABSTRACT

In the present work, a new series of 14 novel phthalimide-benzenesulfonamide derivatives 4a-n were synthesized, and their inhibitory activity against yeast α-glucosidase was screened. The obtained results indicated that most of the newly synthesized compounds showed prominent inhibitory activity against α-glucosidase. Among them, 4-phenylpiperazin derivative 4m exhibited the strongest inhibition with the IC50 value of 52.2 ± 0.1 µM. Enzyme kinetic study of compound 4m proved that its inhibition mode was competitive and Ki value of this compound was calculated to be 52.7 µM. In silico induced fit docking and molecular dynamics studies were performed to further investigate the interaction, orientation, and conformation of the target compounds over the active site of α-glucosidase. Obtained date of these studies demonstrated that our new compounds interacted as well with the α-glucosidase active site with the acceptable binding energies. Furthermore, in silico druglikeness/ADME/Toxicity studies of compound 4m were performed and predicted that this compound is druglikeness and has good ADME and toxicity profiles.


Subject(s)
Diabetes Mellitus, Type 2 , alpha-Glucosidases , Catalytic Domain , Diabetes Mellitus, Type 2/drug therapy , Glycoside Hydrolase Inhibitors/chemistry , Humans , Kinetics , Molecular Docking Simulation , Molecular Dynamics Simulation , Molecular Structure , Phthalimides/pharmacology , Structure-Activity Relationship , Sulfonamides , alpha-Glucosidases/metabolism , Benzenesulfonamides
3.
Emerg (Tehran) ; 6(1): e29, 2018.
Article in English | MEDLINE | ID: mdl-30009231

ABSTRACT

Traumatic pulmonary pseudocyst is a rare complication of chest trauma that has been poorly documented and usually resolves without specific treatment. Here, we present a case of pulmonary pseudocyst in a child with chest trauma without obvious symptoms. It is important to consider this diagnosis in patients with chest trauma to avoid unnecessary invasive procedures.

4.
Addict Health ; 4(3-4): 95-101, 2012.
Article in English | MEDLINE | ID: mdl-24494142

ABSTRACT

BACKGROUND: Duration of spinal anesthesia depends on the type of anesthetic agent, dosage and additive materials such as epinephrine, ephedrine and opioid. We compared the duration of spinal anesthesia with lidocaine 5% with or without epinephrine in addict and non-addict patients undergoing inferior limb fracture surgery. METHODS: This single blinded randomized clinical trial was performed on 201 males (height ranged 150-180 cm) who referred to the Shahid Bahonar Hospital of Kerman for the inferior limb fracture. Their physical class was matched to the American association standard class 1 and 2, and they were appropriate candidates for the spinal anesthesia. The addict or non-addict groups were each divided into two subgroups. 75 mg of 5% lidocaine was prescribed for one subgroup, and the other subgroup received 75 mg of 5% lidocaine plus 0.2 mg epinephrine. The level of primary anesthesia was elevated to T6. Duration of returning to the 4 primary sensory levels was measured since baseline. FINDINGS: A significant increase in the duration of anesthesia level in both addict and non-addict patients receiving lidocaine plus epinephrine was observed compared to the subgroups receiving lidocaine alone (P < 0.01). Duration of decrease in sensory level in addict subgroups receiving lidocaine or lidocaine plus epinephrine was lower compared to non-addict patients (P < 0.001). In addict subgroup receiving lidocaine alone, a significant decrease was observed in the time needed for decrease in sensory level (P < 0.01). CONCLUSION: According to the results of this study, regardless of the anesthetic agent being used, duration of spinal anesthesia was shorter in addict patients compared to non-addict ones. Addition of epinephrine to lidocaine 5% increased the duration of spinal anesthesia in both addict and non-addict patients.

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