Summary
The new compounds of 1,2,4-triazole derivatives were synthesized. The chemical structures of the synthesized compounds S1-S11 were determined by some spectroscopy techniques such as FTIR,1HNMR. The reactions were followed by thin layer chromatography (TLC) to ensure that the synthesized of these compounds is complete and their purity , some physical properties of synthesized compounds were recorded such as melting points and colours.
The current study included some steps:
- The Compounds (S1-S5) were synthesized through the reaction of substituted benzoic acid [glycine, 4-chlorobenzoic acid, 4-aminobenzoic acid, 4- hydroxybenzoic acid, 3,4-diaminobenzoic acid] with thiocarbohydrazide.
- The Compounds (S1,S2,S4,S5) underwent condensation reaction with Chloroactylchloride to produce (S6-S9).
- The terephthalic acid was reacted with thiocarbohydrazide in the ratio (1:2) to produce (S10).
- The Compounds (S10) was reacted with Chloroactyl chloride in the ratio (1:2) to produce (S11).
In addition, the study included (150) sample from serum of T2DM patients and(75) sample from serum sanples from people without diabetes were used as a control and determine level of biochemical parameters such as Glycated Hemoglobin,Glucose ,kidney function (urea creatinine, uric acid) and liver function; Alanine transaminase (ALT) Aspartate aminotransferase (AST), Alkaline phosphatase (ALP). There was also an aspect of the research that included partial purification of the ALP enzyme from serum of T2DM patients people, and estimated the kinetics properties of the enzyme also this study was intended to determine .
Alkaline phosphatase Also this study included the effectiveness of the new synthesized compounds prepared (S1, S2, and S6) on the activity of alkaline phosphatase enzyme (partly purified) in vitro and studied also the type of inhibition results of this study.
The Results showed that:
- About age and BMI for the Studied Groups : The age among groups for patient and control shows no significant difference (p>0.05). The body mass index results were measurement showed no significant different (p>0.05) between the studied groups patients and control healthy group. When compare patient groups between themself showed the age among groups (good glycemic control, moderate glycemic control, and poor glycemic control) was found increase but no significant (p>0.05). The body mass index results showed no significant different (p>0.05) between the studied groups patients (good glycemic control, moderate glycemic control, and poor glycemic control).
- The present study showed statistically significant differences (p˂0.001) for Glucose, Glycated Hemoglobin,Urea and Uric acid in the T2DM patients groups when compared with control group. Creatinine showed statistically significant differences between study groups (p< 0.05). Whilst, when we studied difference between T2DM patients groups [Good Glycemic Control , Moderate Glycemic Control and Poor Glycemic Control ]showed statistically significant differences (p˂0.001) for Glucose and Glycated Hemoglobin in the T2DM patients groups, whilst Urea, Creatinine and Uric acid showed nonsignificant differences between study groups (p<0.001).
- The present study showed statistically significant differences (p˂0.001) for GPT, GOT and ALP in the T2DM patients groups when compared with control group. Whilst, when we were studied difference between T2DM patients groups [Good Glycemic Control , Moderate Glycemic Control and Poor Glycemic Control ] showed nonsignificant differences (p˂0.001) for GPT, GOT and ALP.
- This study included partially purification ALP enzyme from serum of T2DM patients using Sephadex G 100. The activity of purified ALP enzyme reached (0.067 IU/L), and the specific activity of ALP enzyme was enhanced to (0.0055 IU/mg) by (1.57) folds and enzyme yields (12.41%) . Kinetics studies were carried out which values of Km and Vmax of ALP were (10 mM) for a substrate, optimum temperature was (27°C), optimum pH was (10.4) and optimum time was (1 min).
- When examining the effect of these compounds with a different concentration on Purified enzyme (ALP) in serum of T2DM patients, it was found that the compounds (S1,S2,S6) acts as an inhibitor for enzyme, and this was demonstrated by the decrease in readings resulting from the addition of this compounds and increased inhibition with increased concentration of the compounds. The all compounds acts as an inhibitor of ALP . The results shown in the model indicated that the type of inhibition of compounds (S1,S2, and S6),, was non-competitive