FORMULATION AND EVALUATION OF NOVEL CHROMENE DERIVATIVE AS AN ANTI INFLAMMATORY AGENT USED FOR IBD

Objective: To formulate and evaluate an extended-release (ER) tablet of a new molecule, 2-amino-4-(4-bromophenyl)-7-hydroxy-4H-chromene-3- carbonitrile using a combination of two polymers (hydroxypropyl methyl cellulose [HPMC] K100 and HPMC phthalate) which control the rate and degree of the drug release through 12 hrs period and protect the drug release from acidic pH.Methods: Five batches of tablets (4HC1, 4HC2, 4HC3, 4HC4, 4HC5) were produced by direct compression method. Morphological evaluation of the powder blend was carried out by differential scanning calorimetry and Powered X-ray diffractometry. The evaluation studies such as flow properties, hardness, friability, drug content, and release study were conducted according to pharmacopoeial standards.Results: The physicochemical characteristics of all the granules and tablets were generally satisfactory. The drug release followed zero order, Higuchi model kinetics with diffusion and dissolution mediated mechanism. Tablets were evaluated for physicochemical parameters and promising. Stability studies indicated the dosage form is stable for 3 months at accelerated conditions.Conclusion: From the results received from all test, it was concluded that formulation 4HC4 are the most suitable choice for developing 12 hrs ERtablets. This finding reveals that a particular concentration of HPMC K100 was capable of producing ER.Keywords: Chromene derivative, Extended-release, Hydroxypropyl methylcellulose phthalate, Hydroxypropyl methylcellulose K100

INSILICO DESIGN, SYNTHESIS AND CHARACTERIZATION OF SOME NOVEL BENZOTHIAZOLE DERIVATIVES AS ANTI-CANCER AGENTS

Objectives: Cancer is a disease characterized by uncontrollable, irreversible, independent, autonomous, uncoordinated and relatively unlimited and abnormal over growth of tissues. Breast cancer is the second most common type of cancer after lung cancer. The aim of the study is to carry out the docking studies, synthesis and anti-tumour activities  of Benzothiazole derivatives containing oxadiazole groups or amino groups.Methods: The docking studies of benzothiazole derivatives were done with known anti-cancer targets like oestrogen receptor by using argus lab and auto dock programmes with the standard drug tamoxifen. Based upon  the results obtained from the molecular modeling, the derivatives were selected for the synthesis. The synthesized compounds were characterized by melting point, TLC, IR, 1H NMR, 13CNMR, MASS spectral data and screened for their in- vitro anti-cancer activities.Results: The docking scores obtained for benzothiazole derivatives (BT1,BT2,BT3,BT4) and std.tamoxifen  from the preliminary docking program by using  argusLab  were- 9.68,-9.4,-9.59, -11.1988,-9.71 and  by using autodock program were -6.29, -5.25,-7.19,-7.48,-3.86 respectively. All the four derivatives were synthesized, characterized and subjected to in vitro anticancer screening by MTT assay in breast cancer (MCF-7) cell lines. Compounds DBT1, DBT2, DBT3 were the most active compounds against MCF-7 cell lines with IC50 of 70.0, 64.0 and 65.0, respectively.Conclusion: All the four  derivatives show  good docking scores when compared to standard drug and can be concluded that all the synthesized benzothiazole  ligands show good anti-cancer property.Keywords: Benzothiazole, Oxadiazole, Estrogen receptor, Anticancer targets

REVIEW ON EVALUATING THE ROLE OF NSAIDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE

Recently, several studies have been reported that nonsteroidal anti-inflammatory drugs can fight against neurodegenerative disorders by various mechanisms. Currently, available therapies of neurodegenerative disorders (NDs) provide only symptomatic relief. This is the point at which we need an alternative that acts on the root cause of disease. Parkinson’s disease and Alzheimer’s disease are the two NDs concentrated here. Since the drug profile is already known, drug repurposing is a promising technique in research, thereby reducing the cost and period effectively. Epidemiological studies on various nonsteroidal anti-inflammatory drugs (NSAIDs) showed good results, but when it came to clinical studies the results are found to be poor. Hence, it can be concluded that NSAIDs provide its neuroprotective activity on its long-term use only, as the brain accessibility of this kind of drug is poor due to its lower lipophilicity

Pharmacogenomics: The Right Drug to the Right Person

Pharmacogenomics is the branch of pharmacology which deals with the influence of genetic variation on drug response in patients by correlating gene expression or single-nucleotide polymorphisms with a drug's efficacy or toxicity. It aims to develop rational means to optimize drug therapy, with respect to the patients genotype, to ensure maximum efficacy with minimal adverse effects. Such approaches promise the advent of personalized medicine, in which drugs and drug combinations are optimized for each individual's unique genetic makeup. Pharmacogenomics is the whole genome application of pharmacogenetics, which examines the single gene interactions with drugs

DETAILED VIEW ON REPURPOSED DRUGS, TRACKING OF VACCINES,AND BRIEF VIEW ON PROPHYLACTIC NANOMEDICINES AS AN ALTERNATIVE APPROACH AND PATIENT CARE FOR COVID-19

In December 2019, a rare case of pneumonia was reported in Wuhan, China. This was later analyzed and known to have similar characteristics as viral pneumonia caused by a novel coronavirus. Later, on 11 February 2020, the World Health Organization (WHO) officially named the disease as COVID19. The Severe acute respiratory syndrome coronavirus 2(SARS-CoV-2) ought to taint both the upper respiratory tract and the lower respiratory tract. This COVID-19 is spreading quickly with an immense rise in cases around the world. This infection's mechanism stays obscure, and the medications explicit for the infection were not grown at this point. Infection is highly contagious. Severe Acute Respiratory Syndrome Coronavirus 2(SARS-CoV-2) is one of seven kinds of crown infection, including the one which causes severe maladies like Middle East respiratory disorder (MERS) and abrupt, intense respiratory syndrome(SARS). Since its revelation, the infection has spread and has caused anxiety and fear among people. Recent vaccines are tracked, and clinical trials can bring an immediate protocol on a medication approach. By including different therapeutic approaches, it is easier to combat the disease quickly. With very low mortality and high transmission rate, new approaches to vaccines and nanomedicines bring down the spread. Controlled patient care is also crucial. On 11 March, the World Health Organization (WHO) declared the disease as 'global pandemic’. COVID-19, therefore, poses a significant threat to global public health. This article reviews the epidemiology, pathogenesis, and diagnostic methods. The review also focuses on repurposed drugs, traced vaccines, and a quick view of prophylactic nanomedicines as an alternative for COVID 19. For this review, the complete database has been collected from various search engines such as PubMed, ScienceDirect, Scopus, Elsevier, etc., from the year 2001-2020 using the following keywords

A Review on Oxadiazole

ABSTRACT Oxadiazoles are important five membered heterocyclic classes of compounds with 2 azo groups and one oxygen in its ring system. It is widely researched as a lead compound for designing potent bioactive agents. In this article we have reviewed on physical and chemical properties of oxadiazole, spectra and some methods for its synthesis. We have explored various pharmacological activities of oxadiazole derivatives like anti-inflammatory, anti-cancer, anti-fungal, anti-osteoporotic and anti-microbial. A brief on drugs containing oxadiazole ring and naturally occurring oxadiazole moiety have also been mentioned

IN SILICO DESIGN, SYNTHESIS, CHARACTERIZATION, IN VITRO ANTI-INFLAMMATORY, AND ANTIOXIDANT STUDIES OF 4-ARYL-4H-CHROMENE DERIVATIVES

Objective: The objective of the study was to explore in silico design, preparation, characterization, and evaluation in vitro of some novel 4H-chromene derivatives as anti-inflammatory and antioxidant agents.Methods: 4-phenyl-4H chromene derivatives were imperiled to in silico modeling studies at the molecular level. The ligands were docked against cyclooxygenase-2 (COX-2) receptor targets using Argus Lab. Based on the result, the derivatives were selected for wet lab synthesis. A highly efficient multicomponent reaction of 4H chromene was carried out by one-step condensation of aldehyde with malononitrile and resorcinol without catalyst in water under ultrasound irradiation. The prepared compounds were characterized by noting their melting point, ultraviolet (UV) spectroscopy, infrared (IR) spectroscopy, and thin layer chromatography (TLC) and were scrutinized for its in vitro anti-inflammatory and antioxidant activitives by in vitro cell culture studies. IR spectra of the two compounds were analyzed and studied. Thus, using melting point, TLC and UV spectroscopy the synthesized compounds were found to be pure and identified chemically. The synthesized compounds were then screened for in vitro antioxidant (by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydrogen peroxide free radical scavenging) activity and anti-inflammatory activity by Raw 264.7 cell lines.Result: From the study, it was noticed that chemical structure-2 showed better antioxidant and anti-inflammatory activitives than chemical structure. In the 4-phenyl-4H chromene derivatives, hydroxyl substitution at 7th position and electronegative halogen at 4th position showed better antioxidant and anti-inflammatory activities.Conclusion: The results disclosed that these synthesized derivatives be likely to have moderate action against COX-2 mediated diseases, thereby it may lessen inflammation and agony because of its antioxidant and anti-inflammatory activitives

Novel therapeutic approaches for the management of hepatitis infections

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