01. Universidade Federal Rural de Pernambuco - UFRPE (Sede)
URI permanente desta comunidadehttps://arandu.ufrpe.br/handle/123456789/1
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Resultados da Pesquisa
Item Atividade antimicrobiana de análogos da piperina(2018-08-02) Bezerra, Leonardo Alexandre Barros; Ramos, Clécio Souza; http://lattes.cnpq.br/3782004073843685; http://lattes.cnpq.br/3961756201958567The structural modification of natural compounds is of significant importance for medicinal chemistry, from 1981 to 2014 1328 medicines were approved for commercialization, of which 51.5% are of natural origin and 26.8% are derived from phytochemicals. An example is the natural amide piperine, which is the target of several biological investigations, and which has demonstrated the potential to act as a precursor to new compounds with application in the modulation of biological phenomena with the 1,2,4 oxadiazole nucleus, which are a class of heterocyclic that exhibit a range of biological activities and that can be used for the synthesis of potential microbial agents. This work aims to report the extraction of piperine by microwave. Reflux hydrolysis of piperine to obtain piperinic acid in moderate yields. Obtaining the ethyl piperininate esters and 3,4 methylenedioxy ethyl cinnamate with excellent yields. The synthesis of amidoximes using the conventional methodology of stirring with hydroxylamine hydrochloride, sodium carbonate and the corresponding nitriles with the substituents (p-nitro, p-toluyl, m-toluyl, benzo, piperonyl, 4-pyridine) in yields of 37% -98%. Using the methodology of synthesis of oxadiazole by microwave using ethyl cyano acetate esters with piperonylamidoxime, ethyl ester 3,4-methylenedioxy cinnamate with 4-pyridine and p-toluyl amidoxime in the presence of K2CO3 and DMF. All oxadiazol precursors were elucidated by IV and the 1,2,4-oxadiazoles synthesized characterized by 1H and 13C NMR. Some compounds were tested bactericidal activities, where the 1,2,4-oxadiazoles presented excellent results against Staphylococcus aureus and Klebsiella pneumoniae and one of the compounds presented luminescent activity a little reported in the 1,2,4 oxadiazoles.Item Aplicações de reações multicomponentes em química medicinal(2021-12-20) Nascimento, Lídia Maria Barbosa do; Nascimento, André Augusto Pimentel Liesen; http://lattes.cnpq.br/8040722729889752; http://lattes.cnpq.br/1374229353141799The Multicomponent Reactions (RMCs) are very important reactions in the field of organic chemistry and have been expanding over the decades. These reactions start from 3 or more components to form a single product, in a method known as one-pot, that is, in a single container. Which brings many advantages due to meet the Green Chemistry principles, for being a linear and rapid synthesis, and still collaborate for the call “atomic economy”; in addition to forming complex molecules starting from simple and accessible precursors, as a basis for the formation of intermediaries or products with biological activities, thus bringing great collaborations and applications in Medicinal Chemistry. Many reactions are based on the principle of RMCs, among the best known and widely used are the reaction of Strecker, Hantzsch, Biginelli, Mannich, Passerini and Ugi, the last two being based on isocyanides.Item Avaliação in vitro de derivados 1,2-alcanodiamina frente ao Mycobacterium tuberculosis sensível e multidroga resistente(2019-07-09) Laet, João Paulo de Lucena; Pimentel, Lílian Maria Lapa Montenegro; Burgos, Fábia Regina Nascimento Fernando; http://lattes.cnpq.br/3776642205741967; http://lattes.cnpq.br/6066865382706623; http://lattes.cnpq.br/3972432719752724Mycobacterium tuberculosis (Mtb) is the causative agent of tuberculosis (TB), an infectious-contagious disease, considered one of the deadliest in the world. TB remains a major global public health problem and so far, there has been no effective way to eradicate it. A major change in TB trajectory occurred with the introduction of the first anti-TB drugs and consequently the emergence of resistance forms to antimycobacteria, resistant multidrug tuberculosis (MDR-TB) and extensively resistant tuberculosis (XDR-TB). From this, the need arises for new drugs to be proposed in the treatment of this disease. The present study aims to evaluate diamine derivatives, related to ethambutol, against sensitive Mtb and MDR. Ten compounds derived from the class 1,2-alkanediamine were synthesized and characterized structurally by the pharmaceutical chemistry laboratories of the University of Salamanca and provided through international cooperation. For the biological tests, the standard reference strain H37Rv (ATCC 27294) was classified as a strain sensitive to all drugs used to treat TB and a clinical isolate of a patient affected by pulmonary tuberculosis with a MDR profile, provided by the Health Laboratory Public of Pernambuco. Minimum Inhibitory Concentration (MIC) determined the evaluation of compound activity in 96-well plates by the colorimetric microdilution method. For cytotoxicity (CC50) the MTT test (3- (4,5-dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide) was used with the J774A.1 cell line. The selectivity index (IS) was calculated by the ratio of MIC and CC50. The ten compounds tested had a MIC ranging from 4.0 to> 64.0 μM for strain H37Rv and MDR. With respect to CC50, the compounds had a concentration range ranging from 3.9 to 32.8 μM. Compound D15 exerted the best activity against the reference strain (H37Rv) and MDR strain (MDR 1576), however in the cytotoxicity test the compound that presented the best result was D10. Regarding the selectivity index, compounds A4 and A5 were the ones that obtained the best results even though they were below the ideal index. The compounds evaluated in this study showed moderate activity against Mtb and support the continuity of the study of 1,2-alkanediamine derivatives.Item Síntese de 2-aminoalquil-3-alquenil-1,4-naftoquinona funcionalizadas como matérias-primas na obtenção de novas moléculas bioativas(2022-06-07) Silva, Karolinny Gomes da; Camara, Celso de Amorim; http://lattes.cnpq.br/4500025814149366; http://lattes.cnpq.br/7894875948237128Quinones represent a large and varied family of metabolites of natural distribution. The interest in these substances has been intensified in recent years due to their pharmacological importance. The main interest in quinones comes from their capacity to induce oxidative stress in cells. This stress can also result from the action of many toxic environmental agents on living beings, such as gamma and ultraviolet radiation, ozone, and automobile pollutants in the air, as well as from certain substances in the food chain and from smoking. Natural and synthetic, quinones are substances known to possess potent and varied types of biological activities such as antitumor, molluscicidal, leishmanicidal, anti-inflammatory, antifungal, trypanocidal, antiprotozoal and inhibitors of the reverse transcriptase enzyme of the HIV-1 virus. The present work aims to establish a relationship between natural quinones and, by means of organic synthesis, obtain organic derivatives that possess biological activity.Item Modularidade aplicada à síntese de compostos bioativos(2022-06-06) Lima, Danielle Assis de Albuquerque; Nascimento, André Augusto Pimentel Liesen; http://lattes.cnpq.br/8040722729889752; http://lattes.cnpq.br/4620645760514341The synthesis of bioactive compounds is characterized by the high number of steps to obtain its final product, refining it to the maximum so that its biological activity demonstrates more efficiency, consequently making it a time-consuming process, and because of this, the idea of synthesis modular has become strongly promising. Modular Reactions have taken up a large space in the scope of organic synthesis, for bringing innovations and ways to speed up the obtaining of bioactive compounds for pharmacological use. Firstly, modular reactions draw attention because they are reactions that take advantage of the concept of modularity, which can be summarized in the idea of using so-called “building blocks”, where different compounds are used, participating in varied combinations, having as Consequently, the reduction in the number of steps and, on the other hand, presenting the possibility of increasing the production of analogues of the researched product in a timely manner, in addition to the production of new products with interesting biological properties. This synthesis strategy still gains a lot of space for presenting the possibility of automating the reactions, where the idea of automation is centered on increasing the productivity and the speed with which the compounds will be formed, being able to be done from a script to obtain the products, to computer programming and automation to carry out the syntheses. The implementation of modularity carries with it scientific innovations that help in the growing demand for new drugs.