Prodrugs
Mostrando 1-12 de 76 artigos, teses e dissertações.
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1. Diacetate Naphthoquinone Derivatives Tethered to 1,2,3-Triazoles: Synthesis and Cytotoxicity Evaluation in Caco-2 Cells
Acetylated compounds prepared from naphthoquinones have been reported as antitumoral prodrugs. Exploring the synthetic versatility of the naphthoquinone and triazolic nuclei, herein we report a simple and efficient synthetic route to prepare a series of sixteen prodrugs prototype of 1,2,3-triazoles-naphthoquinodoic acetyl derivatives. The compounds 10a-10h a
Journal of the Brazilian Chemical Society. Publicado em: 2022
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2. Synthesis and Evaluation of Fenofibric Acid Ester Derivatives: Studies of Different Formulation with Their Bioavailability and Absorption Conditions
A series of fenofibric acid ester pro-drugs (JF-1-7) were synthesized. The pharmacokinetic properties of these pro-drugs were examined after oral administration to rats at a dose of 20 mg kg-1 to evaluate the relative bioavailability in rats. The bioavailability of the ester compounds, JF-1, 2, 3, 4, 5, 6, and 7, was significantly higher than that of fenofib
J. Braz. Chem. Soc.. Publicado em: 2020-02
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3. Design, synthesis, biological evaluation, and nitric-oxide release studies of a novel series of celecoxib prodrugs possessing a nitric-oxide donor moiety
A new group of hybrid nitric oxide-releasing anti-inflammatory drugs (NONO-coxibs), in which an O 2-acetoxymethyl-1-(N-ethyl-N-methylamino)diazen-1-ium-1,2-diolate NO-donor moiety is attached directly to the carboxylic acid group of 1-(4-aminosulfonylphenyl)-5-aryl-1H-pyrazol-3-carboxylic acids (6a-c), were synthesized. A low amount of NO was released from t
Braz. J. Pharm. Sci.. Publicado em: 08/04/2019
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4. Anti-Sporothrix brasiliensis activity of different pyrazinoic acid prodrugs: a repurposing evaluation
From drug repurposing studies, this work aimed to evaluate the activity of different pyrazinoic acid (POA) derivatives against Sporothrix brasiliensis. The POA esters were prepared and characterized as previously reported by classical esterification reactions, with good to excellent yields. Sporothrix brasiliensis isolates from cats (n=6) and standard strain
Braz. J. Pharm. Sci.. Publicado em: 08/04/2019
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5. Cancer, Photodynamic Therapy and Porphyrin-Type Derivatives
ABSTRACT This review has two parts. The first one gives an approach to interdisciplinary studies against cancer carried out by many scientists using porphyrin-type substrates as photosensitizers in PDT. Intensive studies were performed for almost six decades. The successes really started in 1993 with the first formulation patented under the trade name Photof
An. Acad. Bras. Ciênc.. Publicado em: 2018
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6. Identification of a type I nitroreductase gene in non-virulent Trypanosoma rangeli
ABSTRACT Trypanosomatid type I nitroreductases (NTRs), i.e., mitochondrial enzymes that metabolise nitroaromatic pro-drugs, are essential for parasite growth, infection, and survival. Here, a type I NTR of non-virulent protozoan Trypanosoma rangeli is described and compared to those of other trypanosomatids. The NTR gene was isolated from KP1(+) and KP1(-) s
Mem. Inst. Oswaldo Cruz. Publicado em: 2017-07
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7. Prodrugs available on the Brazilian pharmaceutical market and their corresponding bioactivation pathways
O objetivo do trabalho foi ressaltar a importância do planejamento de pró-fármacos para a terapia, por meio de exemplos disponíveis no mercado farmacêutico brasileiro. Os princípios da latenciação são sucintamente discutidos. Apresentam-se exemplos de pró-fármacos de muitas classes terapêuticas importantes e as vantagens relativas aos fármacos d
Brazilian Journal of Pharmaceutical Sciences. Publicado em: 2010-09
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8. Evaluation of the influence of base and alkyl bromide on synthesis of pyrazinoic acid esters through fatorial design
Pyrazinoic acid esters have been synthesized as prodrugs of pyrazinoic acid. In the literature, its preparation is reported through the reaction of pyrazinoyl chloride with alcohols and the reaction with DCC/DMAP. In this work, it is reported a 2² factorial design to evaluate the preparation of these esters through the substitution of alkyl bromides with ca
Química Nova. Publicado em: 2009
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9. Synthesis, characterization and pharmacological evaluation of amide prodrugs of Flurbiprofen
O flurbiprofen (FB) apresenta efeitos colaterais comuns às drogas do tipo NSAIDs (Non-steroidal anti-inflammatory drugs - drogas não esteróides anti-inflamatórias), devido à presença do grupo carboxílico livre. O objetivo desse estudo foi retardar esses efeitos adversos de origem gastrointestinal. Dez pró-fármacos derivados do FB foram sintetizados
Journal of the Brazilian Chemical Society. Publicado em: 2008
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10. Importância do metabolismo no planejamento de fármacos
It is widely recognized that pharmacokinetic optimization needs to be addressed early in drug discovery to reduce the high failure rate in bringing drugs to market. Poor absorption, too short duration of action due to high elimination rate, or the presence of active metabolites are examples of properties that can potentially lead to unsuccessful clinical pro
Química Nova. Publicado em: 2007-02
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11. Pró-fármaco ativado por enzima, uma estratégia promissora na quimioterapia
Strategies that promote selective activation of prodrugs by enzymes can be divided into two major classes: 1) deliver of a monoclonal antibody-enzyme immunoconjugate that can recognize a specific antigen and promote the prodrug to a citotoxic drug, with a high selectivity for the target cells, and 2) selective gene delivery encoding an enzyme that can promot
Química Nova. Publicado em: 2006-12
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12. Synthesis and antimycobacterial activity of pyrazinoic acid esters and quinolones / Síntese e atividade antimicobacteriana de ésteres do ácido pirazinóico e quinolonas
Tuberculosis affects over than one billion people around the world. Since the discovery of rifampin, in 1965, no one another important drug was introduced in therapeutics. Pyrazinamide, one of the drugs available in therapy of tuberculosis, is nowadays considered a bioprecursor of pyrazinoic acid, because resistant bacterias do not express an enzyme, pyrazin
Publicado em: 2006