V.V.P.C. Narayana’s research while affiliated with Sri Venkateswara University and other places

About Abstract A series of thiazole-piperazine sulfonamide hybrids (8a-k) were synthesized, characterized and subsequently tested on Alzheimer's disease (AD) targets, including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and the ABTS radical, to assess their effectiveness. Three of the target analogues 8c, 8e and 8g exhibited augmented inhibition on AChE with IC50 values of 2.52±0.92, 2.99±0.01 and 2.14±0.02 µM, respectively. These analogues also showed strong inhibition selectivity against AChE over BChE. Furthermore, the congeners 8d, 8f, 8h and 8i had remarkable ABTS radical scavenging properties as their IC50 values were in the range of 0.05±0.07 to 0.99±0.12 µM. A study of the kinetics of inhibition of AChE for active analogue 8g revealed a mixed type of inhibition. From the molecular docking experiments, it was clear that the compounds 8c, 8e and 8g were placed optimally within the active site of AChE. Molecular dynamics (MD) simulations of these docked complexes indicated that the root mean square deviation (RMSD) of the complexes stabilized below 4 Å. Furthermore, in silico ADMET prediction studies revealed that the targeted analogs satisfied all the characteristics of CNS acting drugs. Finally, these active compounds are determined to be non-toxic and highly neuroprotective against H2O2-induced cell death in SK-N-SH cell lines.

Novel antimicrobial drugs are required to fight the serious global health challenge of antibiotic resistance. In this study, 12 hybrids ofdiarylsulfide (DAS) piperazine-amide 8a-l were synthesized. All the 12 compounds were assessed for the antibacterial study againstGram-positive and Gram-negative bacteria. Antibacterial structure-activity relationship (SAR) analysis revealed that disubstitutedcompounds, particularly 8h (3,4-dinitro) and 8j (2,4-dichloro), exhibited superior antibacterial activity and also states that ortho-substitutedcompounds performing better than para-substituted ones. Molecular docking studies further strengthened antibacterial efficacy ofdisubstituted compounds 8h (-7.58 kcal/mol) and 8j (7.14 kcal/mol) exhibited the highest binding affinity to the DNA gyr. A enzyme,interacting with essential residues critical for bacterial DNA replication. It was concluded that strong binding, alongside favourable lowerRMSD values, allows these compounds to effectively inhibit DNA gyrase. Therefore, these DAS piperazine-amide compounds representpromising lead compounds for further study as antibacterial agents.

In pursuit of a biodynamically potent molecule, we have attempted to synthesize derivatives of piperazine by incorporating them into the Rosuvastatin intermediate. The reason behind this is that heterocyclic compounds with nitrogen atoms in their ring structure, such as pyrimidine, have great potential as drug design scaffolds. By doping piperazine into the Rosuvastatin intermediate, a series of new derivatives made up of aryl-amides, acetamides, and sulfonamides were produced. These derivatives were then assessed for their antimicrobial activity, with a few showing promising results.

Background: Since time immemorial, humans have identified several herbs to treat various ailments. With the advancement of science and state-of-the-art technologies, different herbal extracts and chemical constituents of herbs were identified as therapeutic targets. Cyperus rotundus, also called mustaka, is one of the most ancient herbs widely distributed in tropical and subtropical regions across the globe. The tuberous and aerial parts of the herb were identified to possess various pharmacological properties. Objectives: This review focuses on the various phytocompounds of mustaka and how these compounds exert pharmacological effects and their mode of action. The molecular and cellular effects of mustaka were also discussed based on the preclinical and clinical reports available using an array of in vitro, in vivo, and ex vivo methodologies. Methods: The information from Google Scholar, Science direct, PUBMED, were reviewed with a special focus on the mode of action of C. rotundus from the data on animal and preclinical experiments to treat various diseases. Conclusion: Based on the literature available on C. rotundus in Google Scholar, Science Direct, and PubMed, the pharmacological properties of mustaka were reviewed with a particular focus on its neuropharmacological activities. The mode of action of C. rotundus and its bioactive metabolites at the molecular biology level were demonstrated based on animal and preclinical experiments to cure various ailments. These diverse effects prove C. rotundus as a valuable traditional medicine for treating various disorders.

Humans experience different kinds of stress as a part of the day to day activity. The manifestation of stress will aggravate based on the physical conditions of individuals and due to their socio-economic situation of living. Herbal extracts have long been used in the traditional systems of medicine for the treatment of various ailments because of their potent antioxidant activity and lesser or no side-effects. Recently, there is a surge of interest toward the search of natural substances with diverse pharmacological activities, that can scavenge free radicals and protect cells from oxidative damage and apoptosis because of the adverse effects associated with the use of conventional medicines. Celastrus paniculatus is an endangered medicinal plant used from years in the traditional Ayurvedic system of medicine. The review presents the diverse chemical constituents of C. paniculatus and their pharmacological actions such as neuroprotective, memory-enhancing, anti-depressant, anxiolytic, anti-aging, hypolipidemic, anticancerous, analgesic, anti-inflammatory, antioxidant, anti-apoptotic, gastroprotective, anti-ulcerative properties at the cellular and molecular level based on the pre-clinical and clinical reports available. In the present review, we gathered the information from sources such as Google Scholar, Science direct, PUBMED, and reviewed with a special focus on the mode of action of C. paniculatus at molecular biology from the data on animal and preclinical experiments to cure various ailments. These diverse medicinal values of C. paniculatus demonstrates its value as traditional medicine as a cure for multiple maladies.