Subscribe to the gold package and get unlimited access to Shamra Academy
Register a new userRational Design Based Molecular Modeling for Novel Lumiracoxib Analogues: Enhancing The Affinity Toward Cyclooxygenase Type 2 Over Cyclooxygenase Type 1
التصميم العقلاني المعتمد على النمذجة الجزيئية لمشابهات بنيوية جديدة لمركب لوميراكوكسيب: تحسين الإلفة تجاه إنزيم السيكلوأوكسيجيناز من النمط - 2 زيادة على النمط -1
900
0 58
0
(
0
)
Added by
Aِl-Baath University ورقة بحثية
Publication date
2015
fields
Pharmacy
and research's language is
العربية
Created by
Shamra Editor
Ask ChatGPT about the research
تعتبر المركبات الانتقائية تجاه السيكلواوكسيجيناز-2 عوامل واعدة تسمح بالحد من الآثار الجانبية لمضادات الالتهاب غير الانتقائية. حيث تتمتع مثل هذه الأدوية بتأثيرات جانبية هضمية أقل. تزايد الحديث مؤخرا حول التأثيرات الجانبية للمثبطات الانتقائية على المستوى القلبي الوعائي. لذلك تم العمل على تطوير الجيل الثاني من مثبطات السيكلواوكسيجيماز-2 ذات الانتقائية الأعلىو التي تعد أشد أمانا إذا ما قورنت مع الجيل الأول من المثبطات الانتقائية. من هذه المركبات نجد مركب لوميراكوكسيب. تم من خلال هذه الدراسة تحضير البنية الجزيئية للإنزيم الهدف.
Compounds, showing selectivity towards COX-2, are promising agents as selective non-steroidal anti-inflammatory drugs (NSAIDs) with lower side effects, especially, gastrointestinal ones. However, recent reports reveal the cardiovascular side effects associated with the selective COX-2 inhibitors. Therefore, attempts have been done to develop the second generation of selective COX-2 inheritors. They have safer profile compared to the first generation. Lumiracoxib belongs to this class of compounds. In this study, the molecular structure of the target enzymes were prepared. Library of rationally designed lumiracoxib analogues were docked.
References used
Mysler, E., 2004, Lumiracoxib (Prexige®): a new selective cox-2 inhibitor. International Journal of Clinical Practice. 58(6): p. 606-611
Bombardier, C., et al., 2000, Comparison of Upper Gastrointestinal Toxicity of Rofecoxib and Naproxen in Patients with Rheumatoid Arthritis. New England Journal of Medicine. 343(21): p. 1520-15282
Chan, F.K., et al., 2002, Celecoxib versus diclofenac and omeprazole in reducing the risk of recurrent ulcer bleeding in patients with arthritis. New England Journal of Medicine. 347(26): p. 2104-21102
rate research
Read More
Nowadays, the usage of NSAIDs has been increased dramatically
for relieving pain and the treatment of divers inflammatory
conditions, therefore, it is necessary to develop this class of drug
by increasing their activity and decreasing their side e
ffects. Their
most common side effect is the gastrointestinal disorders,
especially, gastric bleeding resulting from the inhibition of
prostaglandins synthesis.
To study the prevalence of the diabetic hand in a group of type 2 diabetics,
comparing to age- sex matched non-diabetics control group, and to investigate clinical features among
diabetics with or without the diabetic hand.
Blood glucose control reduces the microvascular and macrovascular
complications in patients with diabetes mellitus type II. According to the American Diabetes Association, less than a half of those with diabetes achieve optimal control of blood gluc
ose and target values of HbA1c. Life style modifications is one of the preferences of diabetes management because the potential relationship between diet and diabetic control. So nutrition therapy which given by dietitian and generally lifestyle modifications are considered mainly integrated to traditional medication for disease.
The study included 104 patients with diabetes type II (HbA1c 8% ± 1.07, BMI 26.45 ± 2.69, fasting blood glucose 148.25 ± 33.76) given diabetes self-management education program and divided into two groups. The first group was treated with glibenclamide only and the second was treated with a combination of glibenclamide and metformin. After three months monitoring, 103 patients Completed the study. Therapeutic efficacy was evaluated considering HbA1c ≤ 6.5% as a target value. The necessary statistical study to analyze the data and evaluate the statistical
significance of the results was made.
The results indicate that the treatment supported with life style
modifications was more effective than traditional therapy and patient education at blood glucose control in patients with diabetes mellitus type II and improve their health.
Nowadays, glycogen synthase kinase 3 (GSK-3) inhibitors become
one of the most important drug targets for the development of their
selective inhibitors serving as promising drugs for the treatment of
many diseases, particularly Alzheimer's disease
. Targeting GSK-3
enzyme has a therapeutic importance in many diseases and is one of
the valuable fields for researchers in both academic research centers
and pharmaceutical companies.
Type 2 Diabetes mellitus T2DM has been suggested to be the most common
metabolic disorder associated with magnesium deficiency which has many adverse
outcomes. The aim of this study was to evaluate plasma Mg in 126 T2DM patients
recruited from Dia
betes Centre in Lattakia, compare them to 70 healthy individuals, and
assess the correlation between plasma Mg and HbA1c as a glycemic control biomarker.
Magnesium was measured using xylidyl blue colorimetric method. HbA1c was measured
using ion-exchange resin separation. The SPSS 19.0 software was used for statistical
analysis. Mean plasma Mg concentrations of the diabetics was significantly lower than
controls (P=0.0001). Plasma magnesium was negatively correlated with HbA1c (r=-0.5,
P=0.0002). Plasma magnesium was below the normal reference range (1.9-2.5 mg/dL) in
47.6% of diabetics and 28.6% of controls. In conclusion, it is important to monitor Mg
levels in both T2DM patients and non-diabetics and take procedures to correct
hypomagnesaemia states.
Log in to be able to interact and post comments
comments
Fetching comments
Sign in to be able to follow your search criteria
