40 research outputs found

    Development of novel therapeutic approaches: (I) Targeting allergic responses to peanuts and (II) Inhibition of DPP-IV enzyme involved in diabetes

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    There is an increase in prevalence of peanut allergy, especially in the western world. The only current treatment for peanut allergy is avoidance of peanut from diet and contact. Additionally, there is currently no specific vaccine that can be taken to decrease peanut allergies. The method of desensitizing a person allergic to peanut allergy is deemed unsafe as the smallest amount of peanut can trigger an anaphylaxis reaction. Thus, various allergoids were created by modifying major peanut protein allergen Ara h2 using various cross-linkers and modification agents in order to disrupt the binding surface epitopes of the antigen to antibody. Diabetes is also a growing problem that affects millions of people globally. Having diabetes is known to lead to various morbidity as well which can be detrimental to the patient and a burden to the economy. Various drugs are available as monotherapy for diabetes; however, we aimed to develop dual acting compounds that would not only control type 2 diabetes but also commonly associated diagnosis of hypertension as well. Thus, we have successfully synthesized and tested compounds in vitro as effective dipeptidyl peptidase-IV (DPP-IV) inhibitors and potentially effective in treating hypertension (future study) associated with diabetes by utilizing cyanopyrrolidines and Beta-amino alcohols scaffolds in the structure, respectively

    Carbon Articulating Backpack Spine

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    In the field, firefighters and Urban Search and Rescue (USAR) personnel need to transport variable loads efficiently, safely, and comfortably while simultaneously performing certain physical tasks. Current models of external and internal framed backpacks distribute the load of a pack efficiently, but do not allow for the natural movement of the wearer. Wolfpack Gear, Inc. proposed the need for a system which both effectively carries a load and allows for the unhindered natural movement of the user. The goal of this project was to design, build, and test an articulating backpack support system. The first stage of the project comprised of the groundwork necessary to establish a design concept: defining the problem, outlining the scope of the project, researching the current market and patents, and completing an extensive brainstorming and ideation phase. The second quarter of the project focused on turning the proposed concept into a concrete design through engineering analysis, extensive solid modeling, and initial prototyping. The final phase of the project was to construct a functional prototype that was then tested and iterated upon

    GSU Event Portal

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    GSU Event Portal focuses on providing an ease to people who wish to attend new events in a specific area of interest, where the events that are uploaded to the portal will be managed by the Event Organizers who are part of the portal. Portal provides free as well as paid events, so that people can choose events as per their interest. The portal provides Organizers the flexibility to create, manage, edit and remove events of any type and size. On the other side, Visitors can lookup events, they can save an event for their future interest and also pay for an event where applicable. The application provides a user-friendly interface so that the Organizers and the Visitors can get the benefits of the service provided by the event without any trouble. The application helps users to find an event they wish to attend with ease. They can browse events according to location, date and type. The main objective of the portal is advertising which helps the organizers to advertise their events and grab as much attention of the people to make their event more successful. This age is the age of technology and online advertising of event can help the organizers to attract more people in an easy way compared to paper advertisement. The people interested in an event, can even buy tickets of that event through this portal

    Kiewit Drone Progress Tracking Application

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    Kiewit is one of the largest construction companies in the world and has long pushed the standards for innovation within the construction industry. Kiewit operates on an initiative to be a data-driven organization. Construction projects track progress data for a variety of reasons, none more important than meeting contractual obligations. Keeping clients in tune with the status of a given project not only gives them peace of mind but also correlates directly with revenue. For solar projects, quantity claiming is done by walking up and down rows of solar panels, posts, and torque tubes across the project site and manually entering the status data. The project goal was to create a secondary automated version of the manual quantity claiming process for construction progress tracking. The Kiewit Drone Progress Tracking application serves as a digital management system that supports tracking the progress of solar panel construction sites in a more streamlined way. It hosts a machine learning model that was built in-house. It predicts the progress of the construction site based on drone-captured geo-location tagged images called GeoTIFFs. The application hosts these GeoTIFFs and allows for the creation and display of labels that ultimately help train and run the machine learning model. The development of this application will increase the training data used to impact the accuracy of the AI model, as well as improve accessibility and efficiency for the current solution and provide the platform for expansion to other construction project types

    A green bio-organic catalyst (taurine) promoted one-pot synthesis of (R/S)-2-thioxo-3,4-dihydropyrimidine(TDHPM)-5-carboxanilides: chiral investigations using circular dichroism and validation by computational approaches

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    Owing to the massive importance of dihydropyrimidine (DHPMs) scaffolds in the pharmaceutical industry and other areas, we developed an effective and sustainable one-pot reaction protocol for the synthesis of (R/S)-2-thioxo-DHPM-5-carboxanilides via the Biginelli-type cyclo-condensation reaction of aryl aldehydes, thiourea and various acetoacetanilide derivatives in ethanol at 100 °C. In this protocol, taurine was used as a green and reusable bio-organic catalyst. Twenty-three novel derivatives of (R/S)-TDHPM-5-carboxanilides and their structures were confirmed by various spectroscopy techniques. The aforementioned compounds were synthesized via the formation of one asymmetric centre, one new C–C bond, and two new C–N bonds in the final product. All the newly synthesized compounds were obtained in their racemic form with up to 99% yield. In addition, the separation of the racemic mixture of all the newly synthesized compounds was carried out by chiral HPLC (Prep LC), which provided up to 99.99% purity. The absolute configuration of all the enantiomerically pure isomers was determined using a circular dichroism study and validated by a computational approach. With up to 99% yield of 4d, this one-pot synthetic approach can also be useful for large-scale industrial production. One of the separated isomers (4R)-(+)-4S developed as a single crystal, and it was found that this crystal structure was orthorhombic

    A green bio-organic catalyst (taurine) promoted one-pot synthesis of (R/S)-2-thioxo-3,4-dihydropyrimidine(TDHPM)-5-carboxanilides: chiral investigations using circular dichroism and validation by computational approaches

    Get PDF
    Owing to the massive importance of dihydropyrimidine (DHPMs) scaffolds in the pharmaceutical industry and other areas, we developed an effective and sustainable one-pot reaction protocol for the synthesis of (R/S)-2-thioxo-DHPM-5-carboxanilides via the Biginelli-type cyclo-condensation reaction of aryl aldehydes, thiourea and various acetoacetanilide derivatives in ethanol at 100 °C. In this protocol, taurine was used as a green and reusable bio-organic catalyst. Twenty-three novel derivatives of (R/S)-TDHPM-5-carboxanilides and their structures were confirmed by various spectroscopy techniques. The aforementioned compounds were synthesized via the formation of one asymmetric centre, one new C–C bond, and two new C–N bonds in the final product. All the newly synthesized compounds were obtained in their racemic form with up to 99% yield. In addition, the separation of the racemic mixture of all the newly synthesized compounds was carried out by chiral HPLC (Prep LC), which provided up to 99.99% purity. The absolute configuration of all the enantiomerically pure isomers was determined using a circular dichroism study and validated by a computational approach. With up to 99% yield of 4d, this one-pot synthetic approach can also be useful for large-scale industrial production. One of the separated isomers (4R)-(+)-4S developed as a single crystal, and it was found that this crystal structure was orthorhombic

    Click-chemistry mediated synthesis of OTBN-1,2,3-Triazole derivatives exhibiting STK33 inhibition with diverse anti-cancer activities

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    There is a continuous and pressing need to establish new brain-penetrant bioactive compounds with anti-cancer properties. To this end, a new series of 4′-((4-substituted-4,5-dihydro-1H-1,2,3-triazol-1-yl)methyl)-[1,1′-biphenyl]-2-carbonitrile (OTBN-1,2,3-triazole) derivatives were synthesized by click chemistry. The series of bioactive compounds were designed and synthesized from diverse alkynes and N3-OTBN, using copper (II) acetate monohydrate in aqueous dimethylformamide at room temperature. Besides being highly cost-effective and significantly reducing synthesis, the reaction yielded 91–98 % of the target products without the need of any additional steps or chromatographic techniques. Two analogues exhibit promising anti-cancer biological activities. Analogue 4l shows highly specific cytostatic activity against lung cancer cells, while analogue 4k exhibits pan-cancer anti-growth activity. A kinase screen suggests compound 4k has single-digit micromolar activity against kinase STK33. High STK33 RNA expression correlates strongly with poorer patient outcomes in both adult and pediatric glioma. Compound 4k potently inhibits cell proliferation, invasion, and 3D neurosphere formation in primary patient-derived glioma cell lines. The observed anti-cancer activity is enhanced in combination with specific clinically relevant small molecule inhibitors. Herein we establish a novel biochemical kinase inhibitory function for click-chemistry-derived OTBN-1,2,3-triazole analogues and further report their anti-cancer activity in vitro for the first time

    Click-chemistry mediated synthesis of OTBN-1,2,3-Triazole derivatives exhibiting STK33 inhibition with diverse anti-cancer activities

    Get PDF
    There is a continuous and pressing need to establish new brain-penetrant bioactive compounds with anti-cancer properties. To this end, a new series of 4′-((4-substituted-4,5-dihydro-1H-1,2,3-triazol-1-yl)methyl)-[1,1′-biphenyl]-2-carbonitrile (OTBN-1,2,3-triazole) derivatives were synthesized by click chemistry. The series of bioactive compounds were designed and synthesized from diverse alkynes and N3-OTBN, using copper (II) acetate monohydrate in aqueous dimethylformamide at room temperature. Besides being highly cost-effective and significantly reducing synthesis, the reaction yielded 91–98 % of the target products without the need of any additional steps or chromatographic techniques. Two analogues exhibit promising anti-cancer biological activities. Analogue 4l shows highly specific cytostatic activity against lung cancer cells, while analogue 4k exhibits pan-cancer anti-growth activity. A kinase screen suggests compound 4k has single-digit micromolar activity against kinase STK33. High STK33 RNA expression correlates strongly with poorer patient outcomes in both adult and pediatric glioma. Compound 4k potently inhibits cell proliferation, invasion, and 3D neurosphere formation in primary patient-derived glioma cell lines. The observed anti-cancer activity is enhanced in combination with specific clinically relevant small molecule inhibitors. Herein we establish a novel biochemical kinase inhibitory function for click-chemistry-derived OTBN-1,2,3-triazole analogues and further report their anti-cancer activity in vitro for the first time

    Hip Braces As A Conservative Treatment Alternatives For Patients With Femoroacetabular Impingement

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    Femoroacetabular Impingement (FAI) in the hip is defined as the abnormal bone geometry in the proximal femur (ball) and/or the acetabulum rim (socket) that causes impingement of the soft tissue between the articulating bone. This bone abnormality often leads to pain in the hip, a reduced range of motion, and early-onset osteoarthritis. Since the FAI injury mechanism is mechanical in nature, treatment regiments must address the altered mechanics to be effective. A conservative treatment utilizing hip braces to address the injury mechanism was studied. Two hip braces, the SERF Brace and a modified Groin Brace, were tested under a slow walking, fast walking, and a slow jogging condition in healthy controls using motion capture. The data collected suggested both braces alter the hip motions in favor of addressing the injury mechanisms faced by FAI patients. Therefore, hip braces may be used as a conservative treatment to alter hip motions to decrease the injury-inducing mechanism associated with FAI
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