Abstract:: Indole moiety is often found in different class of pharmaceutically active molecules having various biological activities including anticancer, anti-viral, anti-psychotic, anti-hypertensive, anti-migraine anti-arthritis and analgesic activities. Due to enormous applications of indole derivatives in pharmaceutical chemistry, a number of conventional synthetic methods as well as green methodology have been developed for their synthesis. Green methodology has many advantages including high yields, short reaction time, and inexpensive reagents, highly efficient and environmentally benign over conventional methods. Currently, the researchers in academia as well as in pharmaceutical industries have been developing various methods for the chemical synthesis of indole based compounds via green approaches to overcome the drawbacks of conventional methods. This review reflects last ten years developments of the various greener methods for the synthesis of indole derivatives by using microwave, ionic liquids, water, ultrasound, nanocatalyst, green catalyst, multicomponent reaction and solvent-free reactions etc. (please see the scheme below). Furthermore, the applications of green chemistry towards developments of indole containing pharmaceuticals and their biological studies have been represented in this review.
In this review, we emphasized important biomarkers, pathogenesis, and newly developed therapeutic approaches in the treatment of colorectal cancer (CRC). This includes a complete description of small-molecule inhibitors, phytopharmaceuticals with antiproliferative potential, monoclonal antibodies for targeted therapy, vaccinations as immunotherapeutic agents, and many innovative strategies to intervene in the interaction of oncogenic proteins. Many factors combine to determine the clinical behavior of colorectal cancer and it is still difficult to comprehend the molecular causes of a person's vulnerability to CRC. It is also challenging to identify the causes of the tumor's onset, progression, and responsiveness or resistance to antitumor treatment. Current recommendations for targeted medications are being updated by guidelines throughout the world in light of the growing number of high-quality clinical studies. So, being concerned about the aforementioned aspects, we have tried to present a summarized pathogenic view, including a brief description of biomarkers and an update of compounds with their underlying mechanisms that are currently under various stages of clinical testing. This will help to identify gaps or shortfalls that can be addressed in upcoming colorectal cancer research.
Background: In terms of death rates, occurrence, costs, and prevalence, respiratory tract diseases, which include minor issues like the common cold and life-threatening ones like bacterial pneumonia, lung cancers, and tuberculosis, are extremely significant. People have been worried about their health for a long time because of respiratory diseases. Old-style medication has tended to these diseases; however, the accumulation of information produced by elective methodologies, among which medication assumes a significant role, is insignificant. Phytotherapy has consistently given proficient solutions for constant and moderate wellbeing inconveniences and, occasionally, for intense and serious problems. Alleviating the aggravated nasal sections and aviation routes was a shared need in antiquated societies. In this study, we conducted a systematic literature review to gain evidence about herbal products and their phytoconstituents that play a role in respiratory illness. We also predicted the physicochemical properties of various phytoconstituents from therapeutic plants employed to cure respiratory ailments (such as asthma, COPD, cough, tuberculosis, etc.). Objectives: The main objective of this critical study is to explore phytotherapy-based molecules for respiratory illnesses. The physicochemical properties of already isolated compounds have been evaluated to screen for the drug-like behavior of phytoconstituents. Methodology: A wide variety of literature has been collected from PubMed, Google Scholar, Medline, and other scientific databases. After an exhaustive review, the chemical structures of phytoconstituents responsible for curing respiratory illness were sketched in ChemDraw Ultra 8.0, and these structures have been taken for further analysis of the physicochemical properties of these phytoconstituents. The crucial parameters of phytoconstituents' physicochemical properties were analyzed using the pkCSM webserver. Result: The results suggest that a variety of phytoconstituents have the potential to treat respiratory illnesses, and the physicochemical parameters reveal that 65 compounds out of 130 screened compounds exhibit Lipinski's rule of five and Veber's rule, while others don't obey these rules. Compounds with optimal physicochemical properties could be promising candidates for emerging respiratory illness treatments. Conclusion: This critical review highlights the possible therapeutic potential of plant-based medicine to cure respiratory illnesses. The finding shows that a wide range of alkaloids, glycosides, terpenoids, and flavonoids isolated from different herbs may be able to treat respiratory problems. More research is needed to find out the IC50 and MIC values of these compounds against respiratory pathogens like S. pneumoniae and M. tuberculosis.
Diabetes Mellitus [DM] is a long-term metabolic condition that is characterized by excessive blood glucose. DM is the third most death-causing disease, leading to retinopathy, nephropathy, loss of vision, stroke, and cardiac arrest. Around 90% of the total cases of diabetic patients have Type II Diabetes Mellitus[T2DM]. Among various approaches for the treatment of T2DM. G protein-coupled receptors [GPCRs] 119 have been identified as a new pharmacological target. GPR119 is distributed preferentially in the pancreas β-cells and gastrointestinal tract [enteroendocrine cells] in humans. GPR119 receptor activation elevates the release of incretin hormones such as Glucagon-Like Peptide [GLP1] and Glucose Dependent Insulinotropic Polypeptide [GIP] from intestinal K and L cells. GPR119 receptor agonists stimulate intracellular cAMP production via Gαs coupling to adenylate cyclase. GPR119 has been linked to the control of insulin release by pancreatic β-cells, as well as the generation of GLP-1 by enteroendocrine cells in the gut, as per In vitro assays. The dual role of the GPR119 receptor agonist in the treatment of T2DM leads to the development of a novel prospective anti-diabetic drug and is thought to have decreased the probability of inducing hypoglycemia. GPR119 receptor agonists exert their effects in one of two ways: either by promoting glucose absorption by β-cells, or by inhibiting α-cells' ability to produce glucose. In this review, we summarized potential targets for the treatment of T2DM with special reference to GPR119 along with its pharmacological effects, several endogenous as well as exogenous agonists, and its pyrimidine nucleus containing synthetic ligands.
1. Let f(t) be a perodic function with period 2π and integrable in the sense of Lebesgue over (–π, π), then its Fourier series is
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