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Sintese e avalia??o de atividade tripanocida de novos heterociclos da classe dos 1,2,4-OXADIAZ?IS, derivados e an?logos da amida natural piperina. / SYNTHESIS AND EVALUATION OF TRIPANOCIDAL ACTIVITY OF NEW HETEROCYCLES OF THE 1,2,4-OXADIAZIAL CLASS, DERIVATIVES AND ANALOGS OF THE NATURAL AMID PIPERINA.Soares, Breno Almeida 25 September 2009 (has links)
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Previous issue date: 2009-09-25 / Coordena??o de Aperfei?oamento de Pessoal de N?vel Superior, CAPES, Brasil. / This work is part of a research project which investigates the utilization of abundant
and accessible natural products in the synthesis of new molecules with potential activity
against Chagas? disease. Recent studies carried out in our laboratory showed activity
against Trypanosoma cruzi for piperine, a major component of Piper nigrum and for a
series of its derivatives and analogues. Using bioisosterism as a strategy for molecular
modification, we describe here the design, synthesis and antiparasitic evaluation of
class of derivatives of 1,2,4-oxadiazole. The key step of the synthetic strategy used
involved the SNAC reaction of the benzamidoxima with acid chlorides followed by
cyclization, which allowed the preparation of eight new 1,2,4-oxadiazole The evaluation
of the toxic activity of these new derivatives against epimastigote form of T. cruzi
confirmed the bioisosteric relationship between the natural amide and the new products
prepared, showing the oxadiazole 55 direct derived from piperine, as the most active
compound in the series. / Este trabalho se insere numa linha de pesquisa que visa a utiliza??o de produtos
naturais abundantes e access?veis na s?ntese de novas mol?culas com potencial atividade
anti-chag?sica. Estudos recentes em nosso laborat?rio demonstraram a atividade
antiparasit?ria da piperina e de uma s?rie de derivados e an?logos sobre o Trypanosoma
cruzi, agente etiol?gico da doen?a de Chagas. Utilizando o bioisosterismo como
estrat?gia de modifica??o molecular, descrevemos aqui o planejamento, a s?ntese e a
avalia??o antiparasit?ria de derivados da classe dos 1,2,4-oxadiaz?is. A etapa-chave da
estrat?gia sint?tica utilizada envolveu a rea??o de SNAC da benzamidoxima com cloretos
de ?cidos, seguida de cicliza??o, que permitiu a prepara??o de oito novos 1,2,4-
oxadiaz?is. A avalia??o da atividade t?xica destes novos derivados contra a forma
epimastigota do T. cruzi confirmou a rela??o bioisost?rica entre a amida natural e os
novos derivados preparados, evidenciando o oxadiazol 55 derivado direto da piperina,
como o composto mais ativo da s?rie.
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Avalia??o de antiparasit?rios sobre o perfil enzim?tico e exame androl?gico em Nelore. / Anti-parasitic evaluation on the enzymatic profile and andrologic exam in Nelore.Almeida, Jaci de 10 December 2010 (has links)
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Previous issue date: 2010-12-10 / Ectoparasite affects in the animals, carrying great prejudices to the health and considerable
economic losses. Antiparasitic utilization of wide action spectrum has been assisting in the
losses reduction in consequence of these infestations. They were objectives of this work,
evaluate of the treatment antiparasitic effects, in therapeutic doses, in the preventive control
of the natural infestations for Dermatobia hominis and Haematobia irritans, and about the
andrological characteristics, enzymatic profile (AST and ALT) and her correlations in Nelore
bulls seminal caracteristics. They were used 20 bulls from 24 to 30 age months, managed in
grazing system (Brachiaria decumbens and B. brizantha). The experiment was executed in
completely randomized design with four treatments (T1 = Control, without medication; T2 =
Ivermectina injet?vel to 3,15%; T3 = Fipronil ?pour-on? e T4 = Doramectina to 1%), three
applications (0, 60 and 120 days), five repetitions (bulls) and five semen collections (D0, D15,
D30, D45 and D60). The animals were submitted to andrological examinations biweekly inside
the periods, being evaluated the ponderal, testicular and seminal characteristics, and the
enzymatic profiles. In the statistical analyses were used Anova and comparisons between
averages according to de Kruskal-Wallis e Bonferroni Tests in the GraphPad Prism? vers?o
4.0 to Windows?. The obtained results indicate that (a) the antiparasitic treatments used in the
preventive control in the natural infestations of ectoparasites do not influence negatively the
ponderal and reproductive characteristics, and (b) the enzymes analyses AST and ALT, in the
sanguine serum, evidenced do not be efficient methodology for evaluation of Nelore bull
spermatogenesis implication. The prophylactic application of the antiparasitic drugs, in the
pre-breeding season, in bulls created extensive is an efficient technique of ectoparasitism
natural control to D. hominis and H. irritans, being the product choice be entailed to the
application practicability and to the cost in each region. / Os ectoparasitas afetam os animais, acarretando grandes preju?zos a sa?de e consider?veis
perdas econ?micas. A utiliza??o de antiparasit?rios de amplo espectro de a??o tem auxiliado
na redu??o de perdas em decorr?ncia dessas infesta??es. Foram objetivos desse trabalho,
avaliar os efeitos dos tratamentos antiparasit?rios, em doses terap?uticas, no controle
preventivo da infesta??o natural por Dermatobia hominis e Haematobia irritans, sobre as
caracter?sticas androl?gicas, perfil enzim?tico (AST e ALT) e correla??es nas caracter?sticas
seminais de touros Nelore. Foram utilizados 20 touros de 24 a 30 meses de idade, criados a
pasto (Brachiaria decumbens e B. brizantha). O experimento foi executado em delineamento
inteiramente casualizado com quatro tratamentos (T1 = Controle, sem medica??o; T2 =
Ivermectina injet?vel a 3,15%; T3 = Fipronil ?pour-on? e T4 = Doramectina a 1%), tr?s
aplica??es dos tratamentos (0, 60 e 120 dias), cinco repeti??es (touros) e cinco coletas de
s?men (D0, D15, D30, D45 e D60). Os animais foram submetidos a exames androl?gicos
quinzenais dentro dos per?odos, sendo avaliadas as caracter?sticas ponderais, testiculares,
seminais e perfil enzim?tico. Nas an?lises estat?sticas foram utilizados Anova e compara??es
entre m?dias de acordo com os testes de Kruskal-Wallis e Bonferroni no programa GraphPad
Prism? vers?o 4.0 para Windows?. As an?lises dos resultados obtidos indicam que (a) os
tratamentos antiparasit?rios empregados no controle preventivos na infesta??o natural de
ectoparasitos n?o influenciam negativamente as caracter?sticas ponderais e reprodutivas, e (b)
as an?lises das enzimas AST e ALT, no soro sangu?neo, evidenciaram n?o ser metodologia
eficiente para avalia??o de comprometimento da espermatog?nese de reprodutores bovinos da
ra?a Nelore. A aplica??o antiparasit?ria profil?tica, na pr?-esta??o de monta, em touros
criados extensivamente ? uma t?cnica eficiente para o controle de ectoparasitismo natural por
D. hominis e H. irritans, devendo a escolha do produto estar vinculada ? praticidade de
aplica??o e ao custo em cada regi?o.
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