672 research outputs found
SYNTHESIS OF COUMARIN HETEROCYCLIC DERIVATIVES WITH IN-VITRO ANTITUBERCULER ACTIVITY
In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be severe problem. The need of study was only because of there are many drugs in market to treat infection but most of the drugs are showing resistance because of the same it is difficult to treat the infection. In this study we chosen coumarin nucleus for study. Thus with the aim of developing novel molecule with improved potency for treating Mycobacterium tuberculosis H37Rv strain infections and with decreased probability of developing drug resistance. The synthesis of coumarin derivatives, starting from salicyaldehyde and ethyl acetoacetate, by conventional organic reaction and results of investigations of their anti-mycobacterial activity. MICs of the synthesized compounds are compared with existing drugs Cytotoxicity. Many compounds have shown promising activity while some were inactive. It was found that Compound A1, A2, B1, B2, C1, C2 have shown promising antitubercular activity against std. Streptomycin
Keywords: Coumarin derivative, well diffusion method, antitubercular activity
Synthesis of novel heterocyclic Quinolone compound for anti -tubercular activity
In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be severe problem. The need of study was only because of there are many drugs in market to treat infection but most of the drugs are showing resistance because of the same it is difficult to treat the infection. In this study we chosen quinolone nucleus for study and over it. Thus with the aim of developing novel molecule with improved potency for treating Mycobacterium tuberculosis H37Rv strain infections and with decreased probability of developing drug resistance. Methodology: The synthesis of Quinolone derivatives, starting from substituted aniline and ethyl acetoacetate, by conventional organic reaction and results of investigations of their anti-mycobacterial activity. Results: MICs of the synthesized compounds are compared with existing drugs Cytotoxicity. The substituted quinolones are synthesized by taking mixture of 7-substituted-2-(3-chloro-2-oxopropyl) quinolin-4(1H)-one and different secondary amines. Many compounds have shown promising activity while some were inactive. Conclusion: It was found that Compound A1, A3, B1, B3, have shown promising anti tubercular activity whereas compound A2, A4, B2, B4 were showing moderate anti tubercular activity against std. Streptomycin
Arbitration and Dispute Settlement in Foreign Indirect Investment. The increasing significance and use of arbitration in international loan agreements, syndicated loans and international bond issues
This dissertation examines the suitability of arbitration for the resolution of securities regulatory claims and it adoption globally, which has resulted in international arbitration becoming the favoured dispute resolution mechanism in the securities industry. The author explains that disputes arising out of international bilateral and syndicated loan agreements are generally considered to be arbitrable, while international bond disputes are often derived from the controversies over the application of mandatory national laws and the compliance with securities regulation provisions - so the arbitrability of international bond disputes depends on the acceptance of the arbitrability of securities regulatory claims
A monolithically integrated power JFET and Junction Barrier Schottky diode in 4H silicon carbide
Efficiency of power management circuits depends significantly on their constituent switches and rectifiers. The demands of technology are increasingly running up against the intrinsic properties of Si based power devices. 4H-Silicon Carbide (SiC) has superior properties that make it attractive for high power applications. SiC rectifiers are already a competitive choice and SiC switches have also been commercialized recently. Junction Barrier Schottky (JBS) diodes, which combine the advantages of PN and Schottky, have higher Figure of Merit (FOM) as rectifiers. Among switches, a robust and mature process has been developed for Silicon Carbide Vertical Junction Field Effect Transistors (VJFETs), which currently gives it the highest unipolar FOM. Switches are frequently combined with anti-parallel diodes in power circuits. This thesis describes the development of a SiC-based monolithically integrated power switch and diode. Monolithic integration increases reliability and efficiency, and reduces cost. Because of their superior properties and similarities in fabrication, we chose the SiC VJFET and JBS diode as the switch and rectifier. Detailed design, fabrication and characterization of the integrated switch to block above 800 V and conduct current beyond 100 A/cm2 is explained. In this process, the first physics-based 2-D compact model is developed for reverse leakage in a JBS diode as a function of design parameters. Since the gate-channel junctions of SiC VJFETs cannot be assumed to be abrupt, an existing analytical model for Si VJFETs is extended to account for graded gate-channel junctions. Using these analytical models, design rules are developed for the VJFET and JBS diode. Finite element simulations are used to find the best anode layout of the JBS diode and optimize electric field termination in the integrated device to ensure their capability to operate at high voltage. Finally, a spin-on glass based process is developed for filling the gate trenches of the VJFET to improve long-term robustness in extreme environments. The integrated power switch developed in this thesis points to the attractions of monolithic integration in SiC power circuits. Analytical compact design equations derived here will facilitate faster and easier design of switches and rectifiers for desired circuit operation.Ph. D.Includes bibliographical referencesIncludes vitaby Rahul Radhakrishna
CYBER PORNOGRAPHY ADDICTION AMONGST MEDICAL STUDENTS OF WESTERN RURAL MAHARASHTRA
Introduction: Cyberpornography is an act of using cyberspace to create, display, distribute, impart or publish pornography or obscene materials, especially materials depicting children engaged in sexual acts with adults. Cyberpornography on one hand, has opened up the new terrain of \u27safe sex\u27, and a positive space for sexual non-conformists. At the same time, it has negatively impacted many offline relations, and a new space for sexual predation and exploitation. Objective: To find out the prevalence, type and form of risk towards cyber pornography addiction amongst the students. Methods & Materials: A prospective cross sectional study was conducted after obtaining an ethical approval from the institute and an informed consent from volunteers fulfilling the eligibility criteria. The Internet sex screening test (ISST) questionnaire with score sheet was used and was collected by complete anonymity and confidentiality. 300 medical students were considered for the study and data collected was analysed by Microsoft-office excel. Results: 57.15% of the volunteer are in low-risk group whereas 30% are vulnerable and 12.85% are in highest-risk group. For boys, 65% are vulnerable whereas 21% in low-risk and the remaining 14% are in highest-risk group. For girls, 73% are in a low-risk, 19% are vulnerable and 8% are in highest-risk group. Conclusion: It is concluded that the majority of boys come under vulnerable category whereas the girls comes in low-risk group showing male preponderance towards addiction. The study reveals that, questions coming under the subgroup of online sexual behaviour-isolated have been answered the maximum number of times, by both the sexes. Whereas, the questions coming under the subgroup of online sexual spending has been answered the least by both the sexes.
KEYWORDS: Cyberpornography; Addiction; Sexual behaviour; ISST Questionnaire
Effectiveness of brief counseling (5As): Antenatal tobacco cessation support program among pregnant women availing antenatal care
Introduction:
It is likely that a pregnant woman is more motivated and receptive to accepting healthy habits and practices if talked about the benefits to the fetus. When explained about the harmful effects of tobacco on the health of the baby, the mother can be encouraged to modify her tobacco consumption habits and work toward quitting tobacco.
Aim:
Our aim was to study the effectiveness of brief counseling (5As)—Antenatal Tobacco Cessation Support Program among pregnant women availing antenatal care (ANC).
Methodology:
A quasi-randomized study design was used to conduct the study. The participants were identified by screening during ANC visits, and women consuming tobacco were subjected to detailed history taking and very brief counseling with the help of 5A’s framework.
Results:
We found that Mishri was the commonest form of tobacco consumed by these women. Around 93.33% of the women consume Mishri, followed by 6.66% of women consuming chewing tobacco. The method of brief counseling made an impact in the cessation of tobacco consumption in 13.37% of the study subjects.
Conclusion:
We conclude that the use of brief counseling and motivational interviewing is feasible in most settings without inhibiting the other important aspects of ANC or disrupting the patient flow
Antidiabetic and antihyperlipidemic effects of crude fractions and isolated compound from Striga orobanchioides Benth on streptozotocin induced diabetic rats
BACKGROUND: Striga orobanchioides Benth is a traditionally used Ayurvedic medicinal plant for the treatment of diabetes. Scientific validation of the claim is studied in this research. The significant bioactivity of the plant components is obligatory for its use in medicine. OBJECTIVE: The present work is to extract bioactive fractions and chemicals, biological activity of the chemicals and to identify potentially bioactive compound(s) from ethanolic extract of the plant. MATERIALS AND METHODS: Ethanolic extract of the authenticated plant was fractionated and subjected to in vitro and in vivo antidiabetic and antihyperlipidemic activity. In vitro α-amylase and α-glucosidase enzyme activity was carried out on digestive enzyme. Streptozotocin (STZ) induced diabetes mellitus in rats model was preferred for in vivo activity where antidiabetic parameters body weight, urine volume, blood glucose level, glycosylated hemoglobin, serum insulin, liver glycogen and lipid profile as an antihypertensive parameters were assessed. Isolation of bioactive compounds was carried out by chromatographic techniques and identification of the compound was done by FTIR, Mass spectrometry and NMR spectroscopy. The molecular docking study with α-amylase, α-glucosidase, dipeptidyl peptidase-IV (DPP-IV), glucokinase (GK) as diabetic markers and on 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) and Niemann-Pick C1-Like 1 (NPC1L1) was carried out. RESULTS: Ethyl acetate-methanol fraction of the ethanol extract showed presence of pentacyclic triterpenoids (81.5% w/w) in GC-HRMS study. Spectroscopic analysis of the isolated compound revealed presence betulin. In vitro antidiabetic activity pointed out robust inhibition of the digestive enzymes by the fractions known as bioactive fraction and betulin. Betulin at a dose of 40 mg/kg treated group showed significant improvement of diabetic conditions. The gene expression studies revealed that betulin in 40 mg/kg dose has positive effects for carbohydrate metabolism in liver, lowers the hepatic inflammation and increases insulin secretion. The plant compound demonstrated significant inhibitory potential on α-amylase, α-glucosidase, DPP-IV and GK enzymes in silico. CONCLUSION: The biological study reveals that betulin could dominate the succession of diabetes in dose dependent manner. The plant and specifically Betulin exerts a significant antidiabetic and antihyperlipidemic effects that are more possibly through stimulation of insulin secretion, increase in PPAR-α level with an increase in GRIA2 mRNA expression
Structure based drug discovery, docking modelling, synthesis and anticonvulsant pharmacological activity of new quinoline derivatives
Novel series of (2-(substituted-phenyl) quinoline-4-yl) (3-(substituted phenyl)-5-phenyl-1H-pyrazol-1-yl) methanone derivatives was carried out docking, modelling and synthesized. The chemical structures of synthesized derivatives were determined by their IR, 1HNMR, MS analysis data, correlate with docking modelling binding affinity and anticonvulsant activity by using mice in MES model. The synthesized derivatives anticonvulsant activity(3-(5-chlorophenyl)-5-phenyl-1H-pyrazol-1-yl) (2-(2-chlorophenyl) quinoline-4yl) methanone(4a) have showed greater as compared to other derivatives according to 25,50 and 100mg/ml concentration as compared to Phenytoin std. drug
Eruptions in focus: cefadroxil and the uncommon realm of fixed-drug reactions: a case report
This case report explores a rare case of localized fixed-drug eruption (FDE) induced by cefadroxil, a first-generation cephalosporin. FDE, characterized by recurrent lichenoid lesions at specific sites upon drug exposure, is an immunological cutaneous adverse reaction. The incidence of FDE due to cephalosporins is infrequently reported, making this case noteworthy. We present a 51-year-old male who developed brownish-black patches and painful blisters on his extremities after initiating treatment with Cefadroxil for a minor toe injury. The patient's symptoms, clinical course, and subsequent recovery are detailed. Treatment involved corticosteroids, antibiotics, and topical agents. The report also provides immunological insights into FDE pathogenesis, involving CD8+ memory T cells, cytokine production, and the role of CD4+ regulatory T cells. While the exact pathogenesis of FDE remains elusive, this report sheds light on the mechanisms contributing to the self-limited nature of these eruptions. Causality assessment using the Naranjo algorithm categorized the association between cefadroxil and FDE as probable. This case report contributes to the limited literature on FDE caused by cephalosporins and underscores the importance of recognizing and managing such dermatological reactions. The broader implications of understanding FDE pathogenesis and the rarity of cephalosporin-induced cases provides valuable insights for clinicians and researchers
Antidiabetic and Antihyperlipidemic activities of Feronia elephantum gum in streptozotocin induced diabetic rats.
Gum of the plant Feronia elephantum Correa (Rutaceae) is useful in the treatment of diabetes in primitive books and conventional medicine. The present study was aimed to evaluate antidiabetic effect of Feronia elephantum gum extract in different doses along with antihyperlipidemic activity. In vitro antidiabetic activity was studied by inhibition of alpha amylase and alpha glucosidase enzymes. We have tried to separate some of fatty material from the feronia gum and assessed the pharmacological activity. Polyethylene glycol was converted to PEG-COOH using succinic anhydride by using conjugation chemistry technique and then was allowed to react with NHS (n- hydroxyl succinimide) to synthesize PEG-NH2 complex. Conjugation of plant compound containing COOH terminal was synthesized in the final reaction. The presence of Nitrogen and oxygen was identified in elemental CHN analysis. The conjugated compound was studied by NMR spectroscopy to find out the compounds conjugated with PEG complex. Single intraperitoneal injection of STZ at 55 mg/kg was used for induction of diabetes. Feronia gum aqueous extract was studied for pharmacological activities at a dose of 200 mg/kg, 300 mg/kg and 400 mg/kg and was compared with diabetic control group using Metformin as a standard drug. Real Time Polymerase chain reaction was carried out to study the mRNA expression of IRS2 gene, PPARα gene and GRIA2 gene. FGE 400 showed significant inhibition for alpha amylase and alpha glucosidase enzymes. Increased blood glucose level, glycosylated hemoglobin, body weight and urine volume was significantly decreased by treatment with FGE 400. Antidiabetic activity of FGE 400 was supported by insulin content, liver glycogen, antioxidant enzymes (CAT, SOD, GPx , GST); hepatic glucose metabolic enzymes (Glucokinase, Glucose 6 phosphate dehydrogenase, glucose 6 phosphatase, fructose 1, 6 bisphosphatase), liver damage markers (SGOT, SGPT, ALP), histopathology study of pancreas and liver. FGE400 has positive effects for carbohydrate metabolism in liver (IRS2 gene), lowers the hepatic inflammation (PPARα gene) and increases insulin secretion (GRIA2 gene). From the study it can be concluded that Feronia elephantum gum extract is having prominent antidiabetic and antihyperlipidemic activities in dose dependent manner. Further studies are required for isolation and characterization of active chemical constituents
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