Benzopyrazines: Synthesis, Characterization and Evaluation as Aldose Reductase Inhibitors
Huma Aslam Bhatti,
Qurat-Ul-Ain Zaheer,
Yildiz Tehseen,
Zahid Shaiq,
Khalid Mohammed Khan,
Abdul Hameed,
Jamshed Iqbal
Issue:
Volume 7, Issue 5, October 2019
Pages:
90-97
Received:
14 September 2019
Accepted:
15 October 2019
Published:
24 October 2019
Abstract: Role of aldose reductase (ALR2) in diabetic complications such as retinopathy, nephropathy, neuropathy, and cataract etc. is well-evident. ALR2 in the first step of polyol pathway reduces glucose to sorbitol whose elevated level leads to diabetic cataract, characterize by clouding of the lens in the eye that affects vision. Inhibition of ALR2 enzyme with small molecules as inhibitor is a rapid approach for diabetic management. In the present study the synthetic route to synthesize desired benzopyrazines and a library of sixteen (16) methyl benzopyrazines were screened against aldose reductase. From the bioactivity results, the 3'-hydroxyphenyl benzopyrazine 6l was found most active (IC50 = 1.34 ± 0.07 µM) while 3'-bromophenyl analogue 6i showed comparable activity for ALR2 (IC50 = 3.48 ± 0.66 µM) as compared to standard sorbinil (IC50 = 3.14 ± 0.02 µM). Both compounds (6l and 6i) showed excellent selectivity for ALR2 over aldehyde reductase (ALR1) which has important role in detoxification of toxic aldehydes. The structure of two regio-isomers were fully characterize by 1H and 13C NMR two dimensional NMR techniques including COSY, NOESY, HSQC, and HMBC. Regio-isomers separation was proved to be difficult in different solvent systems. Only an isomer of 3'-bromo benzopyrazine 6i' was isolated that help to assign the structure of regioisomers from NMR data. All the benzopyrazines were fully characterized by using different spectral techniques including 1H, 13C NMR, IR spectroscopy, and mass spectrometry.
Abstract: Role of aldose reductase (ALR2) in diabetic complications such as retinopathy, nephropathy, neuropathy, and cataract etc. is well-evident. ALR2 in the first step of polyol pathway reduces glucose to sorbitol whose elevated level leads to diabetic cataract, characterize by clouding of the lens in the eye that affects vision. Inhibition of ALR2 enzym...
Show More
Significance of Plant Growth Regulators (PGR’s) on the Growth and Yield of Wheat Crop
Muhammad Nasir,
Muhammad Ameen Ahmad,
Shabbir Hussain,
Muhammad Ismaeel
Issue:
Volume 7, Issue 5, October 2019
Pages:
98-104
Received:
18 March 2019
Accepted:
16 May 2019
Published:
21 November 2019
Abstract: The current studies reveal the effect of a plant growth regulator (PGRs) on growth and yield performance of wheat crop. It was demonstrated that plant morphology, physiology, biochemistry and yield of wheat crop is highly effected/ stimulated by the use of low/ different concentration of growth regulators. Various filed experiments were conducted to investigate the effect of concentrations and formulations of three PGR salts (ortho-nitrophenolate, para-nitrophenolate and Sodium-5-Nitroguaiacolate). Various compositions of PGRs were applied as foliar application during different stages of plant growth. Control measurements were also carried out simultaneously using water only. A significant increase in plant height, stem growth, leaf development, chlorophyll contents and other biochemical contents of plant has been observed by the use of PGR. The results indicate that the PGR concentrations of 100 ppm and 150 ppm were found to give the best results. From the current study, it was suggested that dose concentration ranging from100ppm to 150ppm has momentous potential on plant growth and yield of wheat crop. Also it enhances the nutritional value of crop and reduces the economic cost of former.
Abstract: The current studies reveal the effect of a plant growth regulator (PGRs) on growth and yield performance of wheat crop. It was demonstrated that plant morphology, physiology, biochemistry and yield of wheat crop is highly effected/ stimulated by the use of low/ different concentration of growth regulators. Various filed experiments were conducted t...
Show More
