Orientador: João Domingos Rodrigues / Resumo: O tomateiro é uma das mais importantes culturas no Brasil, sendo São Paulo o segundo estado que mais produz este vegetal no país, atrás apenas de Goiás. Além do efeito protetor e curativo dos fungicidas utilizados para este estudo, verificou-se que também têm efeito sobre a fotossíntese líquida da planta, devido à redução momentânea da respiração celular, processo fisiológico que compete com a fotossíntese. Dado o exposto, este estudo teve como objetivo determinar o efeito fisiológico de fungicidas sobre a atividade de enzimas antioxidantes, a fotossíntese e as características produtivas e de viabilidade econômica do tomateiro 'saladete', híbrido Caribe F1 cultivado em casa de vegetação. O experimento foi conduzido na Fazenda de Ensino, Pesquisa e Produção de São Manuel-SP, pertencente à FCA/UNESP. Utilizou-se o delineamento experimental de blocos casualizados, com oito tratamentos e quatro repetições, cada unidade experimental contendo sete plantas. Os tratamentos referem-se ao uso de fungicidas com efeitos fisiológicos, nomeadamente: T1 – Controle; T2 – Piraclostrobina (CT); T3 – CT+BOS; T4 – Boscalida (BOS); T5 – BOS+FP; T6 – Fluxapiroxade+Piraclostrobina (FP); T7 – FP+CT e T8 – FP+CT+BOS. Foram realizados cinco testes de quantificação de trocas gasosas, realizando-se essas análises em diferentes momentos após a pulverização dos fungicidas. Como resultados foi possível observar que os fungicidas de efeitos fisiológicos aplicados nessa pesquisa influenciam positivamente nas... (Resumo completo, clicar acesso eletrônico abaixo) / Doutor

(ENGLISH) Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate: Sarah Basem Bouz Supervisor: PharmDr. Jan Zitko, Ph.D. Title of diploma thesis: Derivatives of quinoxaline-2-carboxylic acid as potential antimicrobial compounds Despite the presence of well-established treatment plan, tuberculosis remains the number one killer of infections according to WHO. One of the reasons behind this failure in eradicating this infection is drug resistance. This fact potentiates worldwide efforts to develop new antituberculars. As part of our long-term research on pyrazine derivatives, we prepared a series of N-substituted quinoxaline-2-carboxamides, refer to fig. below. Quinoxaline-2-carboxylic acid was activated by oxalyl chloride and reacted with different anilines or benzylamines in the presence of pyridine at room temperature, overnight with stirring, and then obtained crudes were purified with flash chromatography. Final products were evaluated for in vitro antimicrobial activities against six mycobacterial strains, eight fungal stems, along with four gram positive and four gram negative bacteria of clinical importance. The most promising compound among all with broad spectrum of antimycobacterial activity (MICMtbH37Ra = 3.91...

DERIVATIVES OF 5-ALKYLPYRAZINE-2-CARBOXYLIC ACID AS POTENTIAL ANTI-INFECTIVES HALÍŘOVÁ MARTINA Department of Pharmaceutical Chemistry and Drug Analysis, Faculty of Pharmacy in Hradec Králové, Charles University, Czech Republic In our previous study, we have demonstrated that 5-alkylamino-N- phenylpyrazine-2-carboxamides with longer alkyl chain (C5-C8) exerted micromolar growth inhibition activity against M. tuberculosis H37Rv. We speculated that the long alkylamino chain could facilitate the penetration of lipophilic mycobacterial cell envelope. To test this hypothesis, we performed the amino to methylene isosteric exchange and designed a series of 5-alkyl-N-phenylpyrazine-2-carboxamides. 5- Alkylpyrazine-2-carboxylic acids (5-Ak-POA) were prepared by homolytic alkylation of commercially available pyrazine-2-carbonitrile by respective alkanoic acid, followed by hydrolysis of the carbonitrile group. Final derivatives were prepared by CDI mediated coupling of 5-Ak-POA with corresponding aniline at RT. Final compounds were described by melting point, elementary analysis, IR spectroscopy and 1 H, 13 C NMR. Then they were tested in vitro for antimycobacterial activity against M. tuberculosis H37Rv and several non-tuberculous mycobacterial strains. Several compounds exerted MIC of 3.13-6.25 µg mL-1 ....