SYNTHESIS, CHARACTERIZATION AND ANTHELMINTIC ACTIVITY OF ISATIN ANALOGS AGAINST PHERITIMA POSTHUMA

bjective: Isatin (1H-indole-2,3-dione), an endogenous compound identified in many organisms, shows a wide range of biological activities. In viewof these facts, in our present communication, we wish to report the synthesis and evaluation of some isatin analogs for anthelmintic activity againstPheritima posthuma.Methods: A series of 16 isatin analogs (3a-3p) have been synthesized, characterized by physical and spectral data (Fourier transform infrared,Hnuclear magnetic resonance and mass) and screened for anthelmintic activity against P. posthuma at various concentrations (5, 10, and 20 mg/ml).Results: All compounds were tested for the beginning of paralysis time followed by a time of the death of worms. All prototypes at the concentrationof 20 mg/ml showed significant activity (p<0.01) compared to that of control. The compounds 3f and 3i were found to possess significant activitycompared to standard albendazole (20 mg/ml).Conclusion: The study encourages us to consider a new molecular skeleton of isatin substituted at the first and third position by aryl groups withadequate spacers which may be identified as potential leads for the development of future studies in various in vivo models for anthelmintic activities.Keywords: Isatin, Synthesis, Spectral analysis, Pheritima posthuma, Anthelmintic activity

DENGUE FEVER: STAGES, COMPLICATION, DIAGNOSIS, AND PREVENTION STRATEGIES

Dengue fever virus (DENV) is said to be a single-stranded, positive-sense RNA virus that belongs to the family Flaviviridae and the genus is Flavivirus. The disease can be transmitted through infected blood products and also through organ donation. Vertical transmission (from mother to child) at the time of pregnancy or during birth has been reported. Other unusual reports showed man-to-man modes of transmission. Hemorrhagic fever is specified by hemorrhage, thrombocytopenia, leakage of blood plasma, or dengue shock syndrome. Dengue is basically transmitted by various species of mosquito among the genus Aedes, the most uniquely identified one is Aedes aegypti. There are four different but very closely related serotypes (DENV-1, DENV-2, DENV-3, and DENV-4) of the virus that causes Dengue. Lifelong immunity against the particular serotype that has caused the infection is believed to have been imparted upon recovery. However, cross-immunity to the other serotypes is either partial or temporary upon recovery and hence future infections by any of the other serotypes enhance the risk of developing severe dengue. Prevention is identified by reducing the habitat and the number of mosquitoes and also by limiting exposure to bites. Treatment of mild or moderate type is supportive, with oral or intravenous rehydration. The intravenous fluids and blood transfusion for more severe cases are found to be effective. The present study aimed to present brief and informative salient features of various facts regarding dengue, including its global incidence, structure, mode of transmission, clinical signs and symptoms, control, and preventive measures

A CONTROLLED RELEASE MICROSPHERE FORMULATION OF AN ANTI-DIABETIC DRUG AND CHARACTERIZATION OF THE MICROSPHERE

Objective: Here the objective of this study was to prepare and characterize sustained release metformin loaded microsphere formulation which was prepared by W1/O/W2 emulsion solvent evaporation technique.Methods: Guar gum and sodium alginate were used as a matrix building material, whereas ethyl cellulose was applied as a coating polymer. Here various formulations were prepared by changing the drug and guar gum ratio, and the subsequent drug entrapment efficiency (DEE) and drug release were compared and evaluated.Results: Scanning Electron Microscopy (SEM) studies revealed spherical particles with a smooth appearance. Fourier-transform infrared spectroscopy (FTIR) showed there was no interaction between the ingredients in the final formulation. X-ray Diffraction (XRD) studies showed the emergence of polymorphic forms in the final formulation. The drug entrapment in the final drug loaded microsphere formulations was varied from 30-66.78%. The drug release studies showed the continuous release of the drug through twelve hours. The optimized formulation (f2) found to release 71.5% of drugs at the end of the 12th hour following zero order release kinetics.Conclusion: The increase in gum concentration in the W1 phase, which enhances viscosity in the W1 phase, resulting in an increase in the drug entrapment up to an optimum level and a decrease in the release rate. So, it can prolong the action. So by using this tool, we can say that metformin loaded microsphere formulation would be a suitable pharmaceutical formulation for the treatment of diabetic patients in modern drug therapy for its prolonged action. Â

SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL (2-OXO-3-(ARYLIMINO) INDOLIN-1-YL)-N-ARYL PROPANAMIDES AS ANTI-HUMAN IMMUNODEFICIENCY AGENTS

Objective: Acquired immunodeficiency syndrome (AIDS) was first identified in the Western world in 1981. Since then, AIDS has been increasingly wide spreading, its rapid worldwide dissemination brought about by modern mass tourism. Isatin (1 H-indole-2, 3-Dione), an endogenous compound identified in many organisms, shows a wide range of biological activities. In view of the above details, we wish to report the synthesis and evaluation of novel isatin analogs, as promising anti-human immunodeficiency (HIV) agents.Methods: A series of novel isatin analogs (3a-3p) were synthesized, and their chemical structures were confirmed by nuclear magnetic resonance:1H, 13C, ESI-MS spectral data, and CHNS.Results: The compounds were evaluated as inhibitors of HIV type-1 in MT-4 cell cultures. Of these sixteen compounds, only 5 compounds showed potent anti-HIV activity.Conclusion: Evaluation of compound properties in silico showed that they possess significant drug-like characteristics

Quantum Secure Threshold Private Set Intersection Protocol for IoT-Enabled Privacy Preserving Ride-Sharing Application

The Internet of Things (IoT)-enabled ride sharing is one of the most transforming and innovative technologies in the transportation industry. It has myriads of advantages, but with increasing demands there are security concerns as well. Traditionally, cryptographic methods are used to address the security and privacy concerns in a ride sharing system. Unfortunately, due to the emergence of quantum algorithms, these cryptographic protocols may not remain secure. Hence, there is a necessity for privacy-preserving ride sharing protocols which can resist various attacks against quantum computers. In the domain of privacy preserving ride sharing, a threshold private set intersection (TPSI) can be adopted as a viable solution because it enables the users to determine the intersection of private data sets if the set intersection cardinality is greater than or equal to a threshold value. Although TPSI can help to alleviate privacy concerns, none of the existing TPSI is quantum secure. Furthermore, the existing TPSI faces the issue of long-term security. In contrast to classical and post quantum cryptography, quantum cryptography (QC) provides a more robust solution, where QC is based on the postulates of quantum physics (e.g., Heisenberg uncertainty principle, no cloning theorem, etc.) and it can handle the prevailing issues of quantum threat and long-term security. Herein, we propose the first QC based TPSI protocol which has a direct application in privacy preserving ride sharing. Due to the use of QC, our IoT-enabled ride sharing scheme remains quantum secure and achieves long-term security as well

Role of Herbal Medicine, Acupressure and Acupuncture in the Treatment of Irritable Bowel Syndrome

Irritable bowel syndrome (IBS), is a chronic functional gastrointestinal disease that is characterized by a variety of symptoms that have a major negative impact on patients’ quality of life. It affects 9–23% of the total population of the world. At this time, no medication that is capable of addressing all symptoms associated with IBS in an effective manner (antispasmodics, antidiarrheals, sedatives). More than half of patients may seek treatment for their gastrointestinal problems via the use of complementary and alternative medicine (CAM), which includes treatments like herbal medicine, acupuncture, and acupuncture. The objective of this chapter is to evaluate the effectiveness and safety of a herbal preparation, acupuncture, and acupressure treatment in patients diagnosed with IBS. Several sources were used to acquire the material, including review articles published in various publications that had keywords such as herbal drugs, acupuncture, acupressure, IBS and so on. The information was also gathered from the Internet. Herbal therapy and plant products are widely utilized to treat IBS. Acupuncture and acupressure have long been used successfully by patients to treat functional gastrointestinal problems. Multiple clinical studies have shown that their effectiveness and safety are superior to those of placebo and conventional medications. Herbal medications, acupressure, or acupuncture show clinically and statistically significant alleviation of IBS symptoms

MOLECULAR DOCKING STUDIES AND ADME PREDICTION OF NOVEL ISATIN ANALOGS AS HIV-1-RT INHIBITORS WITH BROAD SPECTRUM CHEMO THERAPEUTIC PROPERTIES

Molecular docking studies were performed on 100 newly designed isatin analogs by using Glide v 5.0 on the active site of four different enzymes namely HIV-1 reverse transcriptase (PDB ID 1RT2), glucosamine 6-phosphate (GlcN6P) (PDB ID 2VF5), mycobacterium tuberculosis-CYP51 (PDB code 1EA1) and candida albicans (CACYP51) (PDB code chimeric-1EA1) to study the binding mode of these analogs to study the binding mode of these analogs. Binding mode analysis of the compounds with the highest docking scores (-8.31,-5.90,-7.16,-6.395 and -8.14) was carried out and were compared with that of the co crystallized ligands TNK651, glucosamine (GLP) and fluconazole(TPF) in the active sites of  1RT2, 2VF5,1EA1 , and chimeric 1EA1respectively. ADME properties of all the newly designed isatin analogs 1-100 was calculated by Qik Prop v3.0. All the designed compounds were found to exhibit lead like properties from the calculated ADME properties. Results of these docking analyses can be well used for the design and development of novel isatin analogs possessing HIV-1- RT inhibitory activity with broad spectrum chemotherapeutic properties. KEYWORDSIsatin analogs, Docking, HIV, NNRTIs , NNIBP , Lipinski's rule ,ADM

Research And Review: Drugs And Drugs Development Based On Novel Drug Delivery System

Nanotechnology alludes to the creation and use of materials whose constituents exist at the nanoscale; by tradition, be up to 100 nm in size. Nanoparticles are being utilized for different purposes, from medicinal medications, utilizing in different parts of industry generation, for example, sun based and oxide fuel batteries for vitality stockpiling, to wide fuse into assorted materials of ordinary utilize, for example, makeup garments, optical gadgets, bactericidal, electronic, sensor innovation, organic marking and treatment of diseases. The primary objective for growing such conveyance frameworks is to limit sedate corruption and misfortune, to avoid unsafe reactions and to expand bioavailability. Focusing on the capacity to guide the medication stacked framework to the site of intrigue. These new techniques, frequently called medication conveyance frameworks, depend on interdisciplinary methodologies that consolidate polymer science, pharmaceutics, bio-conjugate science, and atomic science. This work is solemnly for instructive reason and may help in research and scholastics