An Overview of Biological and Synthetic Aspects of Thiazole Derivatives in Heterocyclic Chemistry

These overviews signify a study covering the literature on thiazole derivatives in heterocyclic chemistry. This brief analysis as well provides a revise on current reports and demonstrates the utility and the effectiveness of this approach. The data on the process of synthesis, chemical reactions, and biological activity of these heterocycles available over the preceding years are assessing here. In the last few decades, a lot of effort has been prepared on thiazole ring to discover novel compounds associated to this scaffold. This review presents the advanced improvement on the proposed and growth of diverse thiazole derivatives. It is known as the building block in organic synthesis, which provides as an important outline for the improvement of diverse therapeutic agents and illustrate a broad variety of activities. These articles furnish a widespread explanation of the synthetic and biological value of thiazole engaged in the design and synthesis of diverse type of compounds encloses fused heterocyclic rings with more importance on latest literature

An Experimental-Based Analysis of Inter-BAN Co-Channel Interference Using the κ - μ Fading Model

In this communication, we empirically study and model the impact of co-channel interference and background noise (BN) on a body area network (BAN) operating at 2.48 GHz using the extremely generalized κ - μ fading model. The BAN measurements considered three nodes with the signal-of-interest (SoI) forming the link between two wearable devices located on the front-central-chest and front-central-waist of an adult male, while an interfering signal emanated from a third wearable device that was located on the front-central-waist of an adult female. Three environments were considered which are indicative of different environmental multipath conditions likely to be encountered by everyday BAN users, namely, an anechoic chamber, a reverberation chamber and an indoor laboratory. As well as this, the influence of different human mobility scenarios was studied. Utilizing the κ and μ parameter estimates, we then provide some useful insights into the outage performance of BAN systems in the presence of BN when both the SoI and the interferer undergo κ - μ fading

Future directions for the management of pain in osteoarthritis.

Osteoarthritis (OA) is the predominant form of arthritis worldwide, resulting in a high degree of functional impairment and reduced quality of life owing to chronic pain. To date, there are no treatments that are known to modify disease progression of OA in the long term. Current treatments are largely based on the modulation of pain, including NSAIDs, opiates and, more recently, centrally acting pharmacotherapies to avert pain. This review will focus on the rationale for new avenues in pain modulation, including inhibition with anti-NGF antibodies and centrally acting analgesics. The authors also consider the potential for structure modification in cartilage/bone using growth factors and stem cell therapies. The possible mismatch between structural change and pain perception will also be discussed, introducing recent techniques that may assist in improved patient phenotyping of pain subsets in OA. Such developments could help further stratify subgroups and treatments for people with OA in future

Are bisphosphonates effective in the treatment of osteoarthritis pain? A meta-analysis and systematic review.

Osteoarthritis (OA) is the most common form of arthritis worldwide. Pain and reduced function are the main symptoms in this prevalent disease. There are currently no treatments for OA that modify disease progression; therefore analgesic drugs and joint replacement for larger joints are the standard of care. In light of several recent studies reporting the use of bisphosphonates for OA treatment, our work aimed to evaluate published literature to assess the effectiveness of bisphosphonates in OA treatment

Small molecule inhibitors of Late SV40 Factor (LSF) abrogate hepatocellular carcinoma (HCC): evaluation using an endogenous HCC model

Hepatocellular carcinoma (HCC) is a lethal malignancy with high mortality and poor prognosis. Oncogenic transcription factor Late SV40 Factor (LSF) plays an important role in promoting HCC. A small molecule inhibitor of LSF, Factor Quinolinone Inhibitor 1 (FQI1), significantly inhibited human HCC xenografts in nude mice without harming normal cells. Here we evaluated the efficacy of FQI1 and another inhibitor, FQI2, in inhibiting endogenous hepatocarcinogenesis. HCC was induced in a transgenic mouse with hepatocyte-specific overexpression of c-myc (Alb/c-myc) by injecting N-nitrosodiethylamine (DEN) followed by FQI1 or FQI2 treatment after tumor development. LSF inhibitors markedly decreased tumor burden in Alb/c-myc mice with a corresponding decrease in proliferation and angiogenesis. Interestingly, in vitro treatment of human HCC cells with LSF inhibitors resulted in mitotic arrest with an accompanying increase in CyclinB1. Inhibition of CyclinB1 induction by Cycloheximide or CDK1 activity by Roscovitine significantly prevented FQI-induced mitotic arrest. A significant induction of apoptosis was also observed upon treatment with FQI. These effects of LSF inhibition, mitotic arrest and induction of apoptosis by FQI1s provide multiple avenues by which these inhibitors eliminate HCC cells. LSF inhibitors might be highly potent and effective therapeutics for HCC either alone or in combination with currently existing therapies.The present study was supported in part by grants from The James S. McDonnell Foundation, National Cancer Institute Grant R01 CA138540-01A1 (DS), National Institutes of Health Grant R01 CA134721 (PBF), the Samuel Waxman Cancer Research Foundation (SWCRF) (DS and PBF), National Institutes of Health Grants R01 GM078240 and P50 GM67041 (SES), the Johnson and Johnson Clinical Innovation Award (UH), and the Boston University Ignition Award (UH). JLSW was supported by Alnylam Pharmaceuticals, Inc. DS is the Harrison Endowed Scholar in Cancer Research and Blick scholar. PBF holds the Thelma Newmeyer Corman Chair in Cancer Research. The authors acknowledge Dr. Lauren E. Brown (Dept. Chemistry, Boston University) for the synthesis of FQI1 and FQI2, and Lucy Flynn (Dept. Biology, Boston University) for initially identifying G2/M effects caused by FQI1. (James S. McDonnell Foundation; R01 CA138540-01A1 - National Cancer Institute; R01 CA134721 - National Institutes of Health; R01 GM078240 - National Institutes of Health; P50 GM67041 - National Institutes of Health; Samuel Waxman Cancer Research Foundation (SWCRF); Johnson and Johnson Clinical Innovation Award; Boston University Ignition Award; Alnylam Pharmaceuticals, Inc.)Published versio

A participatory physical and psychosocial intervention for balancing the demands and resources among industrial workers (PIPPI): study protocol of a cluster-randomized controlled trial

Background: Need for recovery and work ability are strongly associated with high employee turnover, well-being and sickness absence. However, scientific knowledge on effective interventions to improve work ability and decrease need for recovery is scarce. Thus, the present study aims to describe the background, design and protocol of a cluster randomized controlled trial evaluating the effectiveness of an intervention to reduce need for recovery and improve work ability among industrial workers. Methods/Design: A two-year cluster randomized controlled design will be utilized, in which controls will also receive the intervention in year two. More than 400 workers from three companies in Denmark will be aimed to be cluster randomized into intervention and control groups with at least 200 workers (at least 9 work teams) in each group. An organizational resources audit and subsequent action planning workshop will be carried out to map the existing resources and act upon initiatives not functioning as intended. Workshops will be conducted to train leaders and health and safety representatives in supporting and facilitating the intervention activities. Group and individual level participatory visual mapping sessions will be carried out allowing team members to discuss current physical and psychosocial work demands and resources, and develop action plans to minimize strain and if possible, optimize the resources. At all levels, the intervention will be integrated into the existing organization of work schedules. An extensive process and effect evaluation on need for recovery and work ability will be carried out via questionnaires, observations, interviews and organizational data assessed at several time points throughout the intervention period. Discussion: This study primarily aims to develop, implement and evaluate an intervention based on the abovementioned features which may improve the work environment, available resources and health of industrial workers, and hence their need for recovery and work ability

Antioxidant activity of tuberosin isolated from Pueraria tuberose Linn

Antioxidant activity of Pueraria tuberose DC, (PT) Leguminosae (Fabaceae) has already been reported by us and here an active compound has been isolated and its action on expression of iNOS protein has been explored by using LPS induced changes in attached rat peritoneal macrophage cell culture. The pure compound was isolated by column chromatography and its structure was characterized by spectral studies, which was identified as tuberosin (5 hydroxy 3,4,7,3',4' pentamethoxy flavone). Its antioxidant capacity was determined and compared with alcoholic extract as EC50 value for scavenging potential towards pre-generated monocation ABTS* radical, superoxide radicals, hydroxyl radicals, metal chelation property and on lipid peroxidation. Further, rat peritoneal macrophages were isolated, cultured and the attached macrophages were exposed to lipopolysaccharide (LPS) with different concentrations of tuberosin (pretreatment for 30 min). After 17 h the released NO content, in culture supernatant, was indirectly estimated as accumulated nitrite by Griess reagent. To understand the mechanism of action, the extent of expression of inducible nitric oxide synthase genes, the iNOS protein was assessed in macrophage lysate by using its antibody on western blot analysis. Tuberosin significantly scavenged all the species of FRs, described above and it also inhibited the LPS induced release of NO and amount of iNOS protein in macrophages. All the changes were significant and concentration dependent. Thus it could be suggested that tuberosin, is one of the active principles of Pueraria tuberose, which directly scavenges various species of Free radicals (FRs) and also inhibits LPS induced inflammatory changes in macrophages

Clinical study on the combined effectiveness of Mashasaptaka Kwatha and Marsha Nasya with Mashasaptaka Taila in Pakshaghata (cerebrovascular accident-infarct)

Background: Pakshaghata is one among Vataja Nanatmaja Vyadhis which are considered as Mahavyadhis. Pakshaghata can be correlated with Hemiplegia, the commonest pathology of which is cerebrovascular accident (stroke). Stroke is defined as sudden onset of neurologic deficit from vascular mechanism. 85% of all strokes are ischemic and 15% are hemorrhagic. Aims And Objectives: To evaluate the combined effectiveness of Mashasaptaka Kwatha and Marsha Nasya with Mashasaptaka Taila in the management of Pakshaghata (Cerebrovascular Accident-infarct). Methods: Thirty diagnosed subjects of Pakshaghata (CVA due to infarct) were administered with Mashasaptaka Kwatha and Marsha Nasya with Mashasaptaka Taila for 7 days. The data of patients was recorded before and after treatment using an elaborate proforma. Assessment was done based on the primary and secondary outcome measures. For statistical analysis, Wilcoxon Signed Rank test, McNemar tests were used. Results: In this study it was found that there was statistically significant relief in the symptoms of Pakshaghata (Cerbrovascular accident-infarct). Conclusion: Relief in the symptoms was achieved by the drugs having properties such as Vatakaphahara, Anulomana, Brimhana, Srotoshodhana etc. Hence, Mashasaptaka Kwatha and Marsha Nasya with Mashasaptaka Taila for 7 days is effective in the management of Pakshaghata (Cerebrovascular accident-infarct)