he thermal behaviour in the solid state of various substituted aminobenzoic acids (3-aminobenzoic acid (3-ABA), 4-aminobenzoic acid (4-ABA), 3-aminosalicylic acid (3-ASA), 4-aminosalicylic acid (4-ASA), and 5-aminosalicylic acid (5-ASA), as well as the "parent" benzoic acid (BA) and salicylic acid (SA) as reference substances, and possible decomposition products: 2-aminophenol (2-AP), 3-aminophenol (3-AP) and 4-aminophenol (4-AP), has been examined. The various sets of isomers studied showed considerable and interesting differences. Most sublimed well before melting, generally with an increasing rate of mass loss beyond their very different melting points. The existence of ranges of isomers allows for the comparison of their behaviour, including such aspects as melting, vaporisation, and the influence of products on the course of decomposition of initially-solid reactants. The differences in behaviour of 4-ASA and 5-ASA were the most remarkable, with 5-ASA being far more stable and apparently not decarboxylating readily, while 4-ASA sublimed at temperatures below the melting point, becoming less stable and decarboxylating in the liquid form. There is also a marked difference in the thermal behaviour of 3-ASA, as compared with 4-ASA and 5-ASA. It decarboxylated at higher temperatures (260°C) than 4-ASA (150°C). The addition of the possible decomposition products to these compounds showed faster decomposition for 4-ASA mixed with 3-AP. The sodium salts of 3-ASA and 4-ASA decarboxylate while that of 5-ASA did not. Binary mixtures of the substances listed above with beta-cyclodextrin (BCD), hydroxypropylbeta-cyclodextrin (HPBCD) and gamma-cyclodextrin (GCD) were prepared (by simple physical mixing or by kneading with a solvent) and were then examined for possible interactions using DSC, TG-FTIR, HSM, XRD and NMR. Generally, kneaded mixtures showed greater changes in thermal behaviour from that of the individual components than the physical mixtures, but changes in the physical mixtures were also significant. Comparison of the effects of the different CDs on the thermal behaviour of individual ASA isomers showed that HPBCD has the greatest interaction with 3-ASA and 5-ASA, followed by GCD, while BCD generally showed the least interactions. For 4-ASA, the effect of GCD is more marked than for 3-ASA and 5-ASA. GCD has the largest molecular cavity.

Plants rely on innate immunity to perceive and respond to pathogenic microbes. Pathogenic microbes suppress and evade plant immune responses to obtain nutrients and multiply resulting in plant diseases and death. One battleground for the arms race between plants and microbial invaders is located in the leaf intercellular space, specifically between Pseudomonas bacteria and Arabidopsis. This thesis seeks to understand the virulence mechanisms that allow Pseudomonas bacteria to grow within the leaves of Arabidopsis and how the plant immune response reduces pathogen growth and reproduction. Some plant pathogens produce specific extracellular polysaccharides to potentially enhance pathogenicity during infection of plants. The objective of this thesis is to understand the importance of biofilms for Pseudomonas success and determine if Arabidopsis suppresses biofilm formation as part of the plant immune response. It was hypothesized that biofilm formation contributes to Pseudomonas success in planta and Arabidopsis suppresses biofilm formation during PAMP-Triggered Immunity (PTI) to reduce bacterial growth. Wild-type plants and defense mutants were infiltrated with flg22 or mock (water) treatments to induce or mock-induce PTI in plants, followed by observing GFP-expressing Pseudomonas via florescence microscopy to determine if biofilm-like aggregate formation was occurring. In vivo studies in this thesis indicate that biofilm-like aggregate formation contributes to bacterial success during Arabidopsis infection. Additionally, the phytohormone, salicylic acid (SA), accumulates in leaf intercellular spaces of resistant plants during PTI that suppresses biofilm formation, suggesting that SA acts as an anti-microbial and anti-biofilm agent that contributes to the suppression of pathogen growth during plant defense. / Thesis / Master of Science (MSc)

The introduction of the ether linkage into various compounds imparts physiological activity, hence the synthesis of various ether derivatives involving the phenol group seemed to be a possible route to tuberculostatic substances. The compounds reported in this work are to be tested for tuberculostatic properties by Parke, Davis and Company.

Nonhost resistance is a type of broad-spectrum resistance exhibited by a given plant species to most strains of a pathogen which are generally pathogenic to other plant species. In this study, we have examined the role of tobacco SABP2 (Salicylic acid-Binding Protein 2) in nonhost resistance. SABP2, a methyl salicylate esterase is a critical component of SA-signaling pathway in tobacco plants. The transgenic tobacco SABP2-silenced lines treated with tetraFA, a known inhibitor of esterase activity of SABP2 exhibited enhanced susceptibility to nonhost pathogen, Pseudomonas syringae pv. phaseolicola compared to the control plants. The increased accumulation of SABP2 transcripts upon Psp infection supports the involvement of SABP2 in nonhost resistance. The tetra-FA treated plants also showed delayed expression of pathogenesis related-1 gene upon Psp inoculations. The expression of nonhost marker genes CDM1 and HIN1 was also monitored in tobacco plants infected with host-pathogen P.s. pv. tabaci and P.s. pv. phaseolicola. Overall, results presented in this manuscript suggest that SABP2 has a role in nonhost resistance in tobacco plants.

Systemic acquired resistance (SAR) is a state of heightened defense which is induced throughout a plant by an initial infection; it provides long-lasting, broad-spectrum resistance to subsequent pathogen challenge. Recendy we identified a phloem-mobile signal for SAR which has been elusive for almost 30 years. It is methyl salicylate (MeSA), an inactive derivative of the defense hormone, salicylic acid (SA). This discovery resulted from extensive characterization of SA-binding protein 2 (SABP2), a protein whose high affinity for SA and extremely low abundance suggested that it might be the SA receptor. Instead we discovered that SABP2 is a MeSA esterase whose function is to convert biologically inactive MeSA in the systemic tissue to active SA. The accumulated SA then activates or primes defenses leading to SAR. SABP2's esterase activity is inhibited in the initially/primary infected tissue by SA binding in its active site; this facilitates accumulation of MeSA, which is then translocated through the phloem to systemic tissue for perception and processing by SABP2 to SA. Thus, while SABP2 is not the SA receptor, it can be considered the receptor for the SAR signal. This study of SABPs not only illustrates the unexpected nature of scientific discoveries, but also underscores the need to use biochemical approaches in addition to genetics to address complex biological processes, such as disease resistance.

Schiff bases are widely used both in technical practice and in the field of medicine. For their antimicrobial activities are studied as potential antimacterial and abtifungal drugs. With increasing level of resistence to currently drugs is the development of new substances very intense. Salicylanilides are a group of substances with antimicrobial activity and are also intensively studied. Based on that we were synthesized novel Schiff bases resulting from salicylic acid, respectively salicylanilides. It was concretely prepared five compounds: 5- chloro-N-{4-[phenyl(phenylimino)methyl]phenyl}-2-hydroxybenzamide, 5-bromo-N-{4-[ phenyl(phenylimino)methyl]phenyl}-2-hydroxybenzamide, 5-chloro-N-{4-[phenyl(3- chlorfenylimino)methyl]phenyl}-2-hydroxybenzamide, 5-chloro-N-{4-[phenyl(4- chlorfenylimino)methyl]phenyl}-2-hydroxybenzamide, 5-bromo-N-{4-[phenyl(4- chlorfenylimino)methyl]phenyl}-2-hydroxybenzamide. The reaction proceeded at the boiling point of the solvent, with catalytic amount of p-toluensulfonic acid. Most of the compounds were characterized by IR, H1 NMR, C13 NMR and melting point. The prepared compounds showed E/Z isomers on double bond, it is demonstrated on NMR specters.

Abstract In the course of human medical history, if there¡¦s a drug that encompasses historic position and future possibilities, it is without a doubt, the aspirin. In the past ten years, new researches related to aspirin developed and opened new area and usages for this wonder drug. Treatments for newly diagnosed disease are also being expanded with new aspirin researches. Usage of medicine against infection can be traced back to 1500. Ebers Papyrus suggested the practice of using dried leaves to treat rheumatism pains and fight against infection through the salicylic acid effect. Later, it was discovered that salicylic acid from the tree bark contains medical value. This was how salicylic acid was obtained until a German named Herman Klobe discovered attaining salicylic acid chemically. Salicylic acid can assist in resisting rheumatism, which was confirmed in a clinical research in 1876. In Germany, 1887, while working in Bayer¡¦s paramedical factory, Felix Hoffman wanted to improve the terrible smell of salicylic acid, so his father, with rheumatism can better take the medicine. He added Acteyl to salicylic acid, which produced acetylsalicylic acid. With animal research, Heinrich Dressler found that this drug has the function of relieving pain and rheumatism. He named this drug aspirin and introduced it to the mass market. The Aspirin as we know today was born. Due to a long history of aspirin use, it¡¦s confirmed that except high dosage uses on children or teenagers suffering from chicken-pox or the flu, aspirin is a safe drug for adults. Clinical tests in the medical field has proven using 100grams of aspirin daily can contain Thromboxane A2 It¡¦s concentration will not affect cyclo system Endothelin cell COX-1. It also does not have any anti-infection effect, so it is safe to take along with other anti-infection drugs, to safely prevent strokes and heart attacks. This research make use of the 4P analysis to do all-round analysis at Aspirin 100 primary prevention And use its framework to simulate the strategy Afterward it use new management though to simulate the strategy "the blue ocean strategy" the analysis tool and framework of Aspirin 100. This research hope the result can make.

MRI can benefit from an increase in the sensitivity of contrast agents. The CEST MRI technique in particular suffers from very poor sensitivity when using diamagnetic contrast agents. Polymerized CEST MRI contrast agents could increase the sensitivity per macromolecule over monomer contrast agents. The increase in sensitivity is related to the increase in number of contrast agents per polymer. A contrast agent with increased sensitivity can be used to image on the molecular level in vivo, where the concentration of targets is very low. A polymerized diaCEST contrast agent was synthesized by coupling a salicylic acid analogue to a poly (acrylic acid) backbone. The CEST effect of the coupled analogue was compared to its uncoupled form for different concentrations and pH values. A RL-QUEST method was used to calculate the exchange rate of the analogue for different pH values before and after coupling. The polymerized diaCEST agent was attempted to be loaded into DOPC and bis-SorbPC liposomes, and was also attempted to be targeted to folate receptors in a KB cell culture. These studies establish the foundation for translation of polymerized diaCEST contrast agents to additional in vitro and in vivo investigations.

In this study, lipo-chitooligosaccharide (NodBj-V (C 18:1, MeFuc); LCO) 10-7M, extracted from Bradyrhizobium japonicum, was sprayed on the leaves of soybean cv. OAC Bayfield soybean and Evans x L66-2470 (carrying the rj1 mutation, and unable to nodulate). Leaf SA level and activities of the PR proteins chitinase, beta-1,3-glucanase and guaiacol peroxidase (GPOX) were quantified. Phenylalanine ammonia-lyase 1 (PAL1) and isoflavone synthase 2 (IFS2) relative gene expression levels in the sprayed leaves were quantified using quantitative real-time PCR. Messenger RNA abundance was quantified using microarrays. The treatment caused a transient increase in local salicylate levels 24 h after exposure, and a systemic increase in GPOX activity 48 h after exposure, in both soybean types. Of the selected 38 genes affected by the LCO treatment, 25 were stress-related. There were no significant differences in (A) chitinase and beta-1,3-glucanase activity, or (B) in PAL1 and IFS2 gene expression.

Acne affects as many as 80% of young adults and adolescents all over the world. This detrimental condition can be classified into four stages: (a) open comedo (blackhead), (b) closed comedo (whitehead), (c) papule and (d) pustule (Russell, 2000:357-366). There are various factors that can lead to acne outbreaks which include: (a) hormone level changes during the menstrual cycle in women, (b) certain drugs (i.e. lithium), (c) certain cosmetics and (d) environmental conditions such as humidity (University of Maryland, 2009:1). The skin performs a variety of functions which include the two major functions: (a) the containment and (b) the protection of the internal organs of the body. The containment function relates specifically to the ability of the skin to confine the underlying tissues and restrain their movement from place to place. The protective function, on the other hand, relates to the ability of the skin to act as a microbiological barrier to most micro-organisms; a chemical barrier to exogenous chemical compounds; barrier to radiation and electrical shock; and mechanical barrier to impact (Danckwerts, 1991:315). Niacinamide and salicylic acid were chosen in combination, due to the beneficial effects that they have on acne. Niacinamide has an anti-inflammatory action on acne; which reduces redness, dryness and irritation caused by Propioni-bacterium acnes that live in the clogged pores of pimples (Acnetreatmentlab, 2008:1). Salicylic acid is a keratolytic and keratoplastic agent. It is used in combination with other ingredients to enhance the shedding of corneocytes. This causes penetration into the skin to be very difficult (SAMF, 2005:177). The solubility of niacinamide and salicylic acid in PBS (pH 7.4 at 32°C) were 212.95 mg/ml and 4.07 mg/ml, respectively. The log D values of niacinamide and salicylic acid were determined to be -0.32 and 0.33, respectively. According to the solubility of niacinamide and salicylic acid it was expected that both of the active ingredients would permeate through the skin. However, it is expected that niacinamide will depict enhanced permeation with respect to salicylic acid. The results of the log D for both of the active ingredients indicate that there would not be optimal permeation. This study involved the formulation of four different acne preparations (Pheroid™cream, Pheroid™gel, cream and gel), combining niacinamide and salicylic acid. The evaluation of stability parameters for the different formulations indicated that none of the formulations was stable under the different storage conditions determined by the Medicines Control Council. Nevertheless, the cream and gel were the most stable of the four formulations. Visual assessment of the Pheroid™ formulations with the confocal laser scanning microscopy (CLMS) was conducted and inconclusive evidence to whether the active substances were entrapped within the Pheroids™, was obtained. Franz cell diffusion studies indicated that the cream (in the case of niacinamide) and gel (in the case of salicylic acid) depicted the highest average and median flux from hours 6 to 12. Results of the tape stripping studies showed that with the gel formulation, concentrations of 2.060 ug/ml and 44.749 ug/ml niacinamide were obtained in the epidermis and dermis respectively. After the Pheroid™ gel was applied, tape stripping depicted only 1.587 ug/ml niacinamide in the epidermis with respect to 22.764 ug/ml niacinamide in the dermis. The cream formulation, on the other hand, showed niacinamide concentrations of 2.001 ug/ml in the epidermis and 13.363 ug/ml in the dermis, whereas with the Pheroid™ cream formulation, concentrations of 1.097 ug/ml and 18.061 ug/ml were obtained in the epidermis and dermis respectively. Tape stripping results depicted that with the gel formulation, concentrations of 2.113 ug/ml and 49.519 ug/ml salicylic acid were obtained in the epidermis and dermis respectively, whereas the Pheroid™ gel formulation showed salicylic acid, concentrations of 1.114 ug/ml in the epidermis and 95.360 ug/ml in the dermis. The cream formulation, however, depicted salicylic acid concentrations of 0.758 ug/ml in the epidermis and 44.729 ug/ml in the dermis. Lastly, after the Pheroid™ cream was applied, salicylic acid concentrations of 0.411 ug/ml and 48.424 ug/ml in the epidermis and dermis respectively, were measured. It could, therefore, be concluded that both niacinamide and salicylic acid tend to concentrate more in the dermis, irrespective of the formulation. This may be an advantage since acne is usually targeted in the dermis and epidermis. / Thesis (M.Sc. (Pharmaceutics))--North-West University, Potchefstroom Campus, 2010.