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Several new 3-substituted isoxazolecarboxamides have been prepared from aromatic and aliphatic aldehydes. A key step was a 1,3-dipolar cycloaddition of nitrile oxides to ethyl acrylate or methacrylate esters. Some of the amides showed high fungicidal activities against Alternaria alternate, Botrytis cinerea, Rhizoctonia solani, Fusarium culmorum, and Phytophthora cactorum strains.
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Plant endophytic fungi as a source of paclitaxel

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Endophytic fungi were isolated from different parts of the plants Corylus avellana (Corylaceae) and Ocimum basilicum (Lamiaceae) and then identified to the genus level based on the morphology of the fungal culture and the characteristics of the spores. The fungicidal and antitumor activity of isolates and extracts obtained from them was determined. We found that a few isolates from Corylus avellana and Ocimum basilicum produced metabolites that inhibited the growth of Oomycetes fungi to a highly significant extent. In the potato disc bioassay only an extract from the isolate C-9 showed an inhibitory action in tumor development. Paclitaxel presence in extract from the isolate C-9 was confirmed using the thin layer chromatography method (TLC) and UV-VIS spectroscopic analysis. The above results indicated that the tested samples revealed an antitumor activity. The detection of paclitaxel in the isolate C-9 suggests that the antitumor activity resulted probably from the presence of this taxane in the tested material.
Introduction: Type III Polyglandular Autoimmune Syndrome (PAS III) is composed of autoimmune thyroid diseases associated with endocrinopathy other than adrenal insufficiency. This syndrome is associated with organ-specific and organ-nonspecific or systemic autoimmune diseases. The frequency of PAS syndromes in diabetic children is unknown. Objectives: The aim of the study was to evaluate the incidence of PAS III in children with diabetes mellitus type 1. Patients and methods: The study consisted of 461 patients with diabetes mellitus type 1(T1DM), who were 1-19 years of age. TSH, free thyroxin, TPO autoantibodies, and thyroglobulin autoantibodies were determined annually. Autoimmune Hashimoto’s thyroiditis was diagnosed in children with positive tests for TPO Ab and Tg Ab and thyroid parenchymal hypogenicity in the ultrasound investigation. Elevated TSI antibodies were used to diagnose Graves’ disease. Additionally, Anti-Endomysial Antibodies IgA class were determined every year as screening for celiac disease. During clinical control, other autoimmune diseases were diagnosed. Adrenal function was examined by the diurnal rhythm of cortisol. Results: PAS III was diagnosed in 14.5% children: PAS IIIA (T1DM and autoimmune thyroiditis) was recognized in 11.1 % and PAS III C (T1DM and other autoimmune disorders: celiac disease, and JIA, psoriasis and vitiligo) in 3.5% children. PAS IIIA was more prevalent in girls than in boys – 78.4% versus 21.6% (p<0.05). PAS III was observed between 1-5 years of life in 66.6% children; the frequency decreased in consecutive years and successively increased in the adolescence period to 22.7%. Conclusions: PAS III occurs in 14.5% of children with DM type1 and the incidence is positively correlated with patients’ age and female gender. Children with PAS III should be carefully monitored as a group at risk for the development of other autoimmune diseases.
The activity of the cymiazol salts of oxalic and boric acids against Ascopharea apis fungi was examined. A method of synthesising cymiazol salts was elaborated. The pathogenic fungi were isolated from honeybees infected with chalk brood. Fungistatic and fungicidal properties of the salts were examined in vitro, though their efficacy was tested in vivo in the infected beehives of honeybee colonies. Although cymiazol oxalate showed a slightly higher inhibiting activity than borate (MIC = 0.008 mol/L and 0.012 mol/L, respectively), the latter is a definitely stronger fungicide (MFC > 0.032 mol/L for oxalate, as compared with 0.012-0.014 mol/L for borate). Used separately, none of these active ingredients (boric acid, oxalic acid, cymiazol) was effective as fungicide, exhibiting only fungistatic properties in tested concentrations. High fungicidal efficacy was displayed only by cymiazol borate. Studies on honeybee colonies confirmed the effectiveness of the salts of cymiazol in treating ascosphaeriosis. After 12-16 days of administering sugar syrup containing these preparations, either a considerable alleviation of the symptoms or even their complete abatement were observed. In families cured with a mixture of cymiazol oxalate and borate a complete abatement of symptoms was obtained. Cymiazol salts can be a valuable and safe supplement of fungicidal formulations used in apiculture.
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