@mau.ac.in
Assistant Professor
Maharaja Agrasen University
Mr. Arvind Kumar currently works at the Department of Pharmaceutical Chemistry, Maharaja Agrasen school of Pharmacy, Maharaja Agrasen University, Atal Shiksha Kunj, Village kalujhanda, near Barotiwala, Baddi, Himachal Pradesh Mr. Kumar does research in Synthetic Chemistry, Green chemistry and Pharma
M.Pharm. in Medicinal Chemistry
Pharmaceutical Science, Pharmacology (medical), Pharmacology
Scopus Publications
Scholar Citations
Scholar h-index
Scholar i10-index
Rohit Kumar, Arvind Kumar, Adarsh Kumar, Ankit Kumar Singh, and Pradeep Kumar
Bentham Science Publishers Ltd.
Aim: Design, synthesis and molecular docking studies of quinoline/naphthalene containing pyrazoline derivatives as PI3K inhibitors. Background: Phosphatidylinositol 3-kinases (PI3Ks) belong to the family of enzymes, which are associated with various cellular functions such as cell growth, proliferation, differentiation etc. Overexpression or any changes in these functions may result in various abnormalities, which in turn cause cancer. Objectives: To perform synthesis and molecular docking studies of quinoline/naphthalene containing pyrazoline derivatives as PI3K inhibitors. Methods: 2-Chloroquinoline-3-carbaldehyde was synthesized by a reaction of acetanilide and POCl3. The latter was reacted with substituted acetophenones to synthesize chalcones, which were reacted with substituted phenyl hydrazines to yield pyrazoline derivatives (Series I). Similarly, pchloro benzaldehyde was reacted with 2-acetonapthone to yield chalcone with substituted phenyl hydrazines to yield pyrazoline derivatives (Series II). Results: The synthetic compounds were subjected to molecular modelling experiments using Schrodinger 2016 software and evaluated in silico for their PI3K binding affinities. All the compounds had better docking scores than AMG-319 (-4.36 Kcal/mol) and comparable docking scores with PI-103 (-6.83 Kcal/mol). Conclusion: Compounds 5 and 3 had the best docking scores (-7.85 and -7.17 Kcal/mol, respectively). The synthesized compounds have better docking scores than the reference drug AMG-319. As a result, they might be used as lead molecules in investigating PI3K inhibitors.
Raghav Dogra, Mohit Kumar, Arvind Kumar, Marco Roverso, Sara Bogialli, Paolo Pastore, and Uttam Kumar Mandal
Informa UK Limited
One of the most valuable practices for analyzing not-so-analytical-friendly analytes in complex, heterogenous matrices is derivatization. Availability of numerous derivatizing reagents (DRs) makes the modification of analyte more exploitable in terms of an analytical perspective. A wide array of derivatization techniques like pre or post-column, in-situ, enzymatic, ultrasound-assisted, microwave-assisted, photochemical derivatization has added much-needed methodological strength in analyzing intricate analytical matrices (food, water, and soil). In recent years, analytical chemistry has achieved greater heights through the development of new sensitive methods with simple conventional instruments like High-Performance Liquid Chromatography (HPLC) devoid of Mass detectors. The prompt availability of these straightforward instruments also makes it a favorable option for routine analysis in food, environmental, bioanalytical chemistry. Analyzing food, environmental or bioanalytical specimen has some of the most problematic aspects, like the low concentration of the analytes accompanied by not too suitable analytical properties. Even though conventional HPLC lacks the required sensitivity but merger with derivatization can lead to a remarkable increase in sensitivity. In recent years there has been a lot of application of diverse derivatizations to increase the sensitivity and selectivity of the analyte for available instruments, resulting in notable findings. Therefore, this review describes the application of derivatization principles in the analysis of analytes in food and additional matrices using conventional HPLC instruments such as HPLC-UV, HPLC-DAD, and HPLC-FD. In this article, we will briefly review the different modes and multiple types of derivatizing reagents with their mechanisms and importance for encouraging the use of established HPLC instruments.
Deepika Sharma, Swati Sharma, and Preeti Chauhan
Oriental Scientific Publishing Company
Obesity is due to imbalance between energy intake and energy expenditure. Adipose tissues are the main site for the fat storage as well as for dissipation. There are two types of adipose tissues: white adipose tissue, which store fat as triglyceride, brown adipose tissue, which burns the fat into energy through the thermogenesis due to uncoupling protein1 present in inner mitochondrial membrane. Histone acylation causes changes in the chromatin structure without causing any change in the deoxyribonucleic acidsequence and thus regulate gene expression.Histonedeacetylase causes the deacylation of histone and interfere with function of histone. Thus histonedeacetylase inhibitors alter the expression of thermogenic gene encoding uncoupling protein 1, peroxisome proliferator activated receptor γ and also causes browning or beiging of white adipose tissue and increases the energy expenditure.