Prodrug Design
Mostrando 1-12 de 14 artigos, teses e dissertações.
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1. 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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2. Antimaláricos potenciais: pró-fármacos poliméricos e formas de liberação controlada de artemisinina / Potential antimalarial agents: polymer prodrugs and controlled release formulations of artemisinin
A malária ainda constitui grave problema de saúde pública, estando presente principalmente em países em desenvolvimento. Acredita-se que 40% da população mundial vivam em áreas endêmicas para esta parasitose. No Brasil, cerca de 600 mil novos casos aparecem a cada ano, merecendo realce a Amazônia, que corresponde a 99% dos casos brasileiros. Dentre
Publicado em: 2006
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3. Bifosfonatos (BFs) como transportadores osteotrópicos no planejamento de fármacos dirigidos
Drug therapy involving bone tissue diseases is difficult, calling for the design of specific drugs. The present paper is a brief review of a new site-directed system termed ODDS (osteotropic drug delivery system), based on a latenciation process, using bisphosphonates as bone carriers. This is an important tool for the rational prodrug design for obtaining s
Química Nova. Publicado em: 2004-06
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4. Optimisation of the lipase-catalysed preparation of a nucleoside prodrug model using an experimental design methodology
The preparation of 2', 3'-di-O-hexanoyluridine (2) by a Candida antarctica B lipase-catalysed alcoholysis of 2', 3', 5'-tri-O-hexanoyluridine (1) was optimised using an experimental design. At 25 ºC better experimental conditions allowed an increase in the yield of 2 from 80% to 96%. In addition to the yield improvement, the volume reaction could be diminis
Química Nova. Publicado em: 2004-06
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5. Oral Bioavailability and Pharmacokinetics of Trovafloxacin in Patients with AIDS
Trovafloxacin pharmacokinetics were evaluated in 12 subjects with AIDS. By using a randomized design, single 200-mg doses of oral trovafloxacin and intravenous alatrofloxacin were administered. The mean absolute bioavailability was 91%. The pharmacokinetics of trovafloxacin when administered orally as the active form or intravenously as the prodrug (alatrofl
American Society for Microbiology.
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6. Nucleic acid-triggered catalytic drug release
We propose a concept for the rational design and synthesis of highly selective chemotherapeutic agents that makes direct use of genetic information about the disease state. The key idea is to use the mRNA or DNA specific to the disease state to trigger the catalytic release of a cytotoxic drug by promoting the association of a prodrug with a catalyst ca
The National Academy of Sciences.
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7. Pharmacokinetics of cefetamet pivoxil (Ro 15-8075) with ascending oral doses in normal healthy volunteers.
The pharmacokinetics of cefetamet pivoxil during administration of ascending oral doses were studied in 16 male normal healthy volunteers (age, 24.5 +/- 2.1 years; weight, 73.5 +/- 8.5 kg). The subjects were randomly assigned to four oral treatments of 500, 1,000, 1,500, and 2,000 mg of cefetamet pivoxil according to a four-by-four Latin square design. After
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8. Studies on a novel series of acyl ester prodrugs of prostaglandin F2 alpha.
A novel series of prostaglandin F2 alpha (PGF2 alpha) prodrugs, with acyl ester groups at the 9, 11, and 15 positions, was prepared in order to design clinically acceptable prostaglandins for treating glaucoma. Studies involving isolated esterases and ocular tissue homogenates indicated that 9-acyl esters cannot provide a prodrug since PGF2 alpha would not b
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9. DB75, a Novel Trypanocidal Agent, Disrupts Mitochondrial Function in Saccharomyces cerevisiae
The aromatic diamidines represent a class of compounds with broad-spectrum antimicrobial activity; however, their development is hindered by a lack of understanding of their mechanism of antimicrobial action. DB75 [2,5-bis(4-amidinophenyl)furan] is a trypanocidal aromatic diamidine that was originally developed as a structural analogue of the antitrypanosoma
American Society for Microbiology.
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10. Synergism between Amodiaquine and Its Major Metabolite, Desethylamodiaquine, against Plasmodium falciparum In Vitro
The in vitro activity of the prodrug amodiaquine and its metabolite monodesethyl-amodiaquine has been studied for three strains of Plasmodium falciparum: LS-2, LS-3, and LS-1. Both compounds showed significant activity against all three strains; the activity of amodiaquine was slightly higher than that of the metabolite. By use of a checkerboard design, inte
American Society for Microbiology.
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11. Novel Azasterols as Potential Agents for Treatment of Leishmaniasis and Trypanosomiasis
This paper describes the design and evaluation of novel azasterols as potential compounds for the treatment of leishmaniasis and other diseases caused by trypanosomatid parasites. Azasterols are a known class of (S)-adenosyl-l-methionine: Δ24-sterol methyltransferase(24-SMT) inhibitors in fungi, plants, and some parasitic protozoa. The compounds prepared sh
American Society for Microbiology.
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12. Pharmacokinetics of intravenous cefetamet (Ro 15-8074) and oral cefetamet pivoxil (Ro 15-8075) in young and elderly subjects.
The purpose of this investigation was to evaluate the effect of advanced age on the pharmacokinetics of cefetamet and its prodrug, cefetamet pivoxil. A secondary objective of this study was to assess the effect of food on the absorption of cefetamet pivoxil in the elderly. Twenty-four healthy subjects (twelve young and twelve elderly) received (in a Latin sq