SYNTHESIS AND PHARMACOLOGICAL EVALUATION: ANTIMICROBIAL, ANTI-INFLAMMATORY, ANALGESIC, ULCEROGENIC PROPERTIES OF SEVERAL BIS-HETEROCYCLIC DERIVATIVES

In Medicinal chemistry, heterocyclic derivatives contributed the largest classical division of organic chemistry. Thiadiazole compounds have been know many biological activities such as hypoglycemic, anticancer, anti-inflammatory, anti-asthmatic, antihypertensive and etc. On this research, several 1,1-Bis [2-{2-(5-(arylidene)imino-1,3,4-thiadiazol-2-yl) methyl amino}- 1,3,4-thiadiazo-5-yl] cyclopropane 5(a-h) have been synthesized from cyclopropane dicarboxylic acid comprising thiadiazole moieties. All the synthesized compounds have been characterized by elemental (C,H,N) and spectral (I.R., 1H- NMR, Mass) analysis. Furthermore, all synthesized compounds were screened for their antifungal, antimicrobial, anti-inflammatory, analgesic, ulcerogenic and toxic activities. The Compound 5f, 3-chlorophenyl substituted was found the most potent in antimicrobial spectrum against all the used microbes. On the other hand, compound 5g, 4-hydroxy-3-methoxy phenyl substituted was found the most potent in anti-inflammatory, analgesic, and ulcerogenic activities which further evaluated for lesser toxicity test.Key words: Bis-phenylarylidinylthiadiazolidinone cyclopropane, anti-microbial, anti-inflammatory, analgesic, ulcerogenic and toxicity studie

Final Report - Augmenting Bridge Inspection with Augmented Reality and Haptics based Aerial Manipulation

Insight and leverage from prior project identified the need for haptics; the inspector’s sense of touch is often used in bridge assessment. Envisioned is the augmentation of bridge personnel by providing a haptics-based aerial manipulator. Such a manipulator would reduce needs to ascend elevated structures like under bridge decks and cabling. There is recent work that uses haptics in aerial manipulation. But these center on autonomous multi-drone flight formation for aerial shows or cooperative object delivery and are relatively straight-forward. The sense of touch is used to provide spatial distance between drones. By contrast, this proposal’s novelty and merit are centered on human-in-the-loop aerial manipulation. The notion is that the expert bridge worker remotely configures the aerial manipulator to “probe” areas of interest and “operate” maintenance procedures. This project integrates haptics, augmented reality, and drone mounted arm. The specific objective is to characterize haptics and AR for their applicability to perform remote probing (i.e. inspection) and operation (i.e. maintenance)

The synthetic bacterial lipopeptide Pam3CSK4 modulates respiratory syncytial virus infection independent of TLR activation

Respiratory syncytial virus (RSV) is an important cause of acute respiratory disease in infants, immunocompromised subjects and the elderly. However, it is unclear why most primary RSV infections are associated with relatively mild symptoms, whereas some result in severe lower respiratory tract infections and bronchiolitis. Since RSV hospitalization has been associated with respiratory bacterial co-infections, we have tested if bacterial Toll-like receptor (TLR) agonists influence RSVA2- GFP infection in human primary cells or cell lines. The synthetic bacterial lipopeptide Pam3-Cys-Ser-Lys4 (Pam3CSK4), the prototype ligand for the heterodimeric TLR1/TLR2 complex, enhanced RSV infection in primary epithelial, myeloid and lymphoid cells. Surprisingly, enhancement was optimal when lipopeptides and virus were added simultaneously, whereas addition of Pam3CSK4 immediately after infection had no effect. We have identified two structurally related lipopeptides without TLR-signaling capacity that also modulate RSV infection, whereas Pam3CSK4-reminiscent TLR1/2 agonists did not, and conclude that modulation of infection is independent of TLR activation. A similar TLR-independent enhancement of infection could also be demonstrated for wild-type RSV strains, and for HIV-1, measles virus and human metapneumovirus. We show that the effect of Pam3CSK4 is primarily mediated by enhanced binding of RSV to its target cells. The Npalmitoylated cystein

Modeling Hose Dynamics for Unmanned Aerial Vehicles

Bridges and other large pieces of infrastructure accumulate massive amounts of dirt, dust, and other particulates that can obscure the structure when scanning to discern structural integrity. Traditionally, these particulates have been removed by humans operating handheld compressed-air hoses, often while mounting ladders -- a risky and inefficient task. To improve infrastructure scanning, unmanned aerial vehicles (UAV) equipped with hoses could be used to clean the structure in place of the current method. The challenge in equipping a UAV with a hose is compensating for the reaction forces and torques produced by fluids expelled by the hose. In order to counteract these reaction forces and torques, the process should be carefully modeled and incorporated in the controller architecture

QUINOLIN-6-AMINES: SYNTHESIS AND BIOLOGICAL EVALUATION

Some novel 2[(achloromethoxy) methyl] thio-N-substituted phenyl [1,2,4] triazolo[1,5-a) quinolin-6-amines have been derived from 5-bromocoumarin. All the synthesized compounds have been characterized by elemental and spectral (I.R., ¹H-NMR, Mass) analysis and evaluated for their antimicrobial, insecticidal and anthelmintic activities

Airway response to respiratory syncytial virus has incidental antibacterial effects

RSV infection is typically associated with secondary bacterial infection. We hypothesise that the local airway immune response to RSV has incidental antibacterial effects. Using coordinated proteomics and metagenomics analysis we simultaneously analysed the microbiota and proteomes of the upper airway and determined direct antibacterial activity in airway secretions of RSV-infected children. Here, we report that the airway abundance of Streptococcus was higher in samples collected at the time of RSV infection compared with samples collected one month later. RSV infection is associated with neutrophil influx into the airway and degranulation and is marked by overexpression of proteins with known antibacterial activity including BPI, EPX, MPO and AZU1. Airway secretions of children infected with RSV, have significantly greater antibacterial activity compared to RSV-negative controls. This RSV-associated, neutrophil-mediated antibacterial response in the airway appears to act as a regulatory mechanism that modulates bacterial growth in the airways of RSV-infected children

Investigation of the presence of human or bovine respiratory syncytial virus in the lungs of mink (Neovison vison) with hemorrhagic pneumonia due to Pseudomonas aeruginosa

<p>Abstract</p> <p>Background</p> <p>Hemorrhagic pneumonia is a disease of farmed mink (<it>Neovison vison</it>) caused by <it>Pseudomonas aeruginosa</it>. The disease is highly seasonal in Danish mink with outbreaks occurring almost exclusively in the autumn. Human respiratory syncytial virus (RSV) has been shown to augment infection with <it>P. aeruginosa</it> in mice and to promote adhesion of <it>P. aeruginosa</it> to human respiratory cells.</p> <p>Findings</p> <p>We tested 50 lung specimens from mink with hemorrhagic pneumonia for bovine RSV by reverse transcriptase polymerase chain reaction (PCR) and for human RSV by a commercial real-time PCR. RSV was not found.</p> <p>Conclusions</p> <p>This study indicates that human and bovine RSV is not a major co-factor for development of hemorrhagic pneumonia in Danish mink.</p

Final Report - Integration of Aerial Manipulation, Haptics-based Human-in-the- Loop Control, and Augmented Reality for Bridge Deck Hosing

This Year 5 and Year 6 report integrates the designs, analyses, and results of the previous years. These have culminated into the design, development and deployment of a hosing-drone. This drone carries and 3000 PSI (pounds per square inch) pressure washer often used to clean bridges. This accomplishment leverages the work in aerial manipulation, human-in-the-loop control, haptics, and augmented- and virtual-reality (AR/VR) executed in prior years. Additionally, this report presents results using a cable-driven parallel robot (CDPR) and telescopic mast. This robot provides another platform that has applications in bridge inspection, maintenance and repair

Invasive Pneumococcal Pneumonia and Respiratory Virus Co-infections

Each year, especially in the winter, many get sick and some die of invasive pneumococcal pneumonia. Does this type of pneumonia increase in the winter because people are in closer contact indoors?  Or are people more susceptible to this bacterial disease after having had a seasonal respiratory virus infection?  A season-by-season analysis found an association between pneumococcal pneumonia and two viruses (influenza and respiratory syncytial virus). The association varied by season and was strongest when the predominant influenza virus subtype was H3N2. Vaccination against influenza and RSV should also help protect against pneumococcal pneumonia