Design, Synthesis, Characterization and Biological Evaluation of Some Novel Benzimidazole Schiff Base Derivatives as Antitubercular Agents Targeting Glutamine Synthetase 1

Based on the various medicinal chemistry journals Glutamine synthetase1 was selected as the target for the study. ➢ A database of 500 molecules with high prospects of inhibiting the target Glutamine synthetase was carefully chosen by making changes to the known hit molecules, i.e., Benzimidazole chalcones. ➢ The molecules were subjected to toxicity assessment by OSIRIS® property explorer. ➢ In-silico drug likeness properties of the designed molecules were determined by using the MOLINSPIRATION® software. ➢ 500 molecules were docked against the target protein using AutoDock 4 ®. ➢ Five molecules with good docking score [lower binding energy] and interactions were shortlisted and optimized for the synthesis. ➢ Compounds were synthesized with satisfactory yield and labelled as BK-1, BK-2, BK-3, BK-4 and BK-5. ➢ Purity of the synthesized compounds was ensured by repeated recrystallization and the compounds were evaluated by TLC and Melting point. ➢ The characterization of the synthesized compounds was done using Infra-red spectroscopy, Liquid Chromatography-Mass spectrometric methods [LC-MS] and Nuclear Magnetic Resonance [H1 NMR] spectroscopy methods. ➢ The pure compounds were screened for Anti-mycobacterial activity by in-vitro Microplate Alamar Blue Assay [MABA]. MIC of synthesized compound were found in the range of 50μg/ml 3.12 μg/ml. ➢ Acute oral toxicity study was conducted on albino wistar rats and all the compounds were found to be safe and non-toxic. CONCLUSION: ✓ Novel Benzimidazole chalcone derivatives were found to be capable of inhibiting the target enzyme Glutamine synthetase 1which is essential for the synthesis of mycobacterium cell wall. ✓ The docking score of the designed compound range between -8.56 to -5.87 Kcal/mol. ✓ All the compounds inhibited the Mycobacterium tuberculosis in the range of 3.12μg/ml to 50μg/ml. ✓ The acute toxicity studies revealed that all the compounds are safe and non-toxic. ✓ The MABA test was carried out using H37Rv strain which is non- pathogenic. Hence further studies should be carried out using clinical isolates i.e, Pathogenic strain. ✓ Further structural refinement of the synthesized compounds is expected to yield promising drug candidate against Mycobacterium tuberculosis

Analysis of Coverage in LoRa using secured IoT Systems

Long Range (LoRa) is an unlicensed Low Power Wide Area Network for the application of the Internet of Things (IoT). This LoRa technology is mainly suitable for smart city applications since this technology consumes low power, low cost, and transfer information over a long distance. This technology proposes a new communication standard to tackle discrete IoT applications. This technology works based on Chirp Spread Spectrum (CSS) technique with a larger bandwidth. LoRa deploys the whole channel bandwidth to transmit the signal which results in, to avoid channel noise, Doppler impacts, and fading. This paper mainly focuses on the impact of three parameters namely, Code Rate (CR), Spreading Factor (SF), Bandwidth (BW). Furthermore, analysis the effect of the data rate and transmission time using Code Rate (CR), Spreading Factor (SF), and Bandwidth to extend coverage

Supersonic Crossflow Transition Control in Ground and Flight Tests

This paper describes the use of distributed-roughness-element (DRE) patterns along a Mach 2 design swept-wing leading edge to increase the laminar flow extent and thereby reduce drag. One swept-wing model was tested in a supersonic wind tunnel as well as beneath a supersonic flight vehicle. Wing model surface data acquired during these tests included pressures, temperatures, and boundary-layer transition locations. Similarities and differences in experimental results are discussed. While wind tunnel and flight results show some differences, the wind tunnel results still provide key insights necessary for understanding how to design effective DRE patterns for use in flight applications. Experimental results demonstrate a DRE flow control effect observed in flight similar to that observed in the wind tunnel. Finally, a different perspective is discussed concerning what flow control role RE patterns might perform in any future swept-wing laminar flow control applications

PRESSURE EFFECT ON CRYSTAL STRUCTURE OF BISMUTH TUNGSTATE Bi2WO6

The structural phase transitions in Bi2WO6 have been investigated by neutron diffraction and Raman spectroscopy at high-pressures. Two phase transitions under pressure were ob-served in the pressure range up to 7 GPa, which are associated with rotations and tilts of the octahedral WO6.The work was supported by the Russian Foundation for Basic Research, grant RFBR N19-52-45009 IND_a

Industrial fisheries off Madras coast based on exploratory surveys during 1973-1980

At the Madras Research Centre of CMFRI, there existed data for areas (Fig. 1) south of 15°40'N Upto the latitude zone of I0°40'N off Velanganni in depths ranging from 10 to 130 m for a eight year period From 1973 to 1980. The results of analysis of these data are presented here with a view to providing information on and extending our knowledge about the spatial and seasonal distribution of various indusirially important fisheries as also their resource potential along the north Tamil Nadu-South Andhra Coast

Cardio-Protection of Salvianolic Acid B through Inhibition of Apoptosis Network

Targeting cellular function as a system rather than on the level of the single target significantly increases therapeutic potency. In the present study, we detect the target pathway of salvianolic acid B (SalB) in vivo. Acute myocardial infarction (AMI) was induced in rats followed by the treatment with 10 mg/kg SalB. Hemodynamic detection and pathological stain, 2-dimensional electrophoresis, MALDI-TOF MS/MS, Western blot, pathway identification, apoptosis assay and transmission electron microscope were used to elucidate the effects and mechanism of SalB on cardioprotection. Higher SalB concentration was found in ischemic area compared to no-ischemic area of heart, correlating with improved heart function and histological structure. Thirty-three proteins regulated by SalB in AMI rats were identified by biochemical analysis and were classified as the components of metabolism and apoptosis networks. SalB protected cardiomyocytes from apoptosis, inhibited poly (ADP-ribose) polymerase-1 pathway, and improved the integrity of mitochondrial and nucleus of heart tissue during AMI. Furthermore, the protective effects of SalB against apoptosis were verified in H9c2 cells. Our results provide evidence that SalB regulates multi-targets involved in the apoptosis pathway during AMI and therefore may be a candidate for novel therapeutics of heart diseases