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1.
Int J Biol Macromol ; 211: 653-668, 2022 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-35568155

RESUMO

Variety of 2-aryl quinoxaline derivatives 1-23 were synthesized in good yields, by reacting 1,2-phenylenediamine with varyingly substituted phenacyl bromides in the presence of pyridine catalyst. All molecules 1-23 were characterized by spectroscopic techniques and evaluated for their diverse biological potential against α-amylase (α-AMY), α-glucosidase (α-GLU), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzymes. Synthetic derivatives possess enhanced inhibitory potential against all enzymes at nanomolar concentrations. In particular, compound 14 was found much superior with IC50 = 294.35, 198.21, 17.04, and 21.46 nM against α-AMY, α-GLU, AChE, and BChE, respectively, as compared to standard inhibitors. Furthermore, selected potent compounds, including 3, 4, 8, 14, 15, 17, and 18, were subjected to molecular docking studies to decipher the binding energies and interactions of ligands (synthetic molecules) with all four target enzymes.


Assuntos
Acetilcolinesterase , Butirilcolinesterase , Acetilcolinesterase/metabolismo , Butirilcolinesterase/química , Inibidores da Colinesterase/química , Simulação de Acoplamento Molecular , Quinoxalinas/farmacologia , Relação Estrutura-Atividade , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo
2.
Surg Res Pract ; 2016: 9319147, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27123469

RESUMO

Background. Laparoscopic cholecystectomy is considered to be gold standard for symptomatic gall stones. As a routine every specimen is sent for histopathological examination postoperatively. Incidentally finding gall bladder cancers in those specimens is around 0.5-1.1%. The aim of this study is to identify those preoperative and intraoperative factors in patients with incidental gall bladder cancer to reduce unnecessary work load on pathologist and cost of investigation particularly in a developing world. Methods. Retrospective records were analyzed from January 2005 to February 2015 in a surgical unit. Demographic data, preoperative imaging, peroperative findings, macroscopic appearance, and histopathological findings were noted. Gall bladder wall was considered to be thickened if ≥3 mm on preoperative imaging or surgeons comment (on operative findings) and histopathology report. AJCC TNM system was used to stage gall bladder cancer. Results. 973 patients underwent cholecystectomy for symptomatic gallstone disease. Gallbladder carcinoma was incidentally found in 11 cases. Macroscopic abnormalities of the gallbladder were found in all those 11 patients. In patients with a macroscopically normal gallbladder, there were no cases of gallbladder carcinoma. Conclusion. Preoperative and operative findings play a pivotal role in determining incidental chances of gall bladder malignancy.

3.
Scientifica (Cairo) ; 2016: 1562153, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27034894

RESUMO

Background. There has been argument between clinical practitioners about clamping catheter or not prior to its removal after transurethral resection of prostate (TURP). We conducted a clinical trial to assess whether clamping has any role in early bladder tone recovery particularly in patients who undergo TURP. Methods. Randomized clinical trial was conducted at a tertiary care hospital, Karachi from January 2014 to July 2015. Eighty-six study participants who underwent TURP were randomly allocated into two groups of 43 participants each. In Group I, patient's Foley catheter was not clamped prior to its removal and in Group II Foley catheter was clamped. Data of all subjects were analyzed using SPSS version 20. Results. There was no significant difference in age and weight of resected tissues between two groups. Among 4 patients in Group I who required recatheterization, 1 patient was discharged with catheter as compared to Group II in which 2 patients were discharged with catheter (P = 0.99). Only 1 patient (2.3%) in Group II had bleeding which required recatheterization. Length of stay was significantly affected by early and free removal of Foley catheter (P < 0.001). Conclusion. The results of current study identified that clamping whether done or not had no significant impact on urinary retention.

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