Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase

Szajnman, Sergio H.; Ravaschino, Esteban L.; Docampo, Roberto; Rodríguez, Juan B.

doi:10.1016/j.bmcl.2005.07.060

Cited by 75 publications

(64 citation statements)

References 43 publications

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“…It has been reported that amphotericin B complexed with cholesterol is at least four times more active than amphotericin B alone in L. donovani-infected hamsters [35]. Moreover, some fatty acid derivatives have been reported with antileishmanial and antimalarial activity [36][37][38][39]. Hence, remarkable antiprotozoal activity of the PE extracts of LC and LCC could be due to their fatty acids and sterol constituents.…”

Section: Discussionmentioning

confidence: 99%

Lycopodium clavatum and Lycopodium complanatum subsp. chamaecyparissus ekstrelerinin antiprotozoal aktivitesi ve sitotoksisitesi

Orhan¹,

Şener²,

Kaiser³

et al. 2013

Turk J Bioch

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Section: Discussionmentioning

confidence: 99%

Lycopodium clavatum and Lycopodium complanatum subsp. chamaecyparissus ekstrelerinin antiprotozoal aktivitesi ve sitotoksisitesi

Orhan¹,

Şener²,

Kaiser³

et al. 2013

Turk J Bioch

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“…Amides, being highly stable and easily available compounds, are substrates of choice, and the most commonly applied procedures are simple modifications of those elaborated for carboxylic acids. The most straightforward are reactions of N-acylamines and N-formylamines with phosphorus trichloride and phosphorous acid [30][31][32], phosphorus tribromide [33], or triphosgene [34], which provide a wide structural variety of 1-amino-1,1-bisphosphonic acids (compound 4, Scheme 3). They are based on modification of the first procedure elaborated by Plöger et al with formamide as a substrate [35].…”

Section: Synthesis From Amidesmentioning

confidence: 99%

“…Despite being readily available substrates, there is limited literature on their use for that purpose. The most popular route is the reaction of nitriles with phosphorous acid, in some cases prompted by phosphorus trichloride and phenylsulphonic or methylsulphonic acids [12,31,47,48]. The conditions of this reaction are sufficiently delicate to use peptidyl nitriles as substrates, which was demonstrated using cyanoethyl derivatives of dipeptides (for example, peptide 16, Scheme 9) [49].…”

Section: Synthesis From Nitrilesmentioning

confidence: 99%

Synthetic Procedures Leading towards Aminobisphosphonates

Chmielewska

Kafarski

2016

Molecules

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Abstract:Growing interest in the biological activity of aminobisphosphonates has stimulated the development of methods for their synthesis. Although several general procedures were previously elaborated to reach this goal, aminobisphosphonate chemistry is still developing quite substantially. Thus, innovative modifications of the existing commonly used reactions, as well as development of new procedures, are presented in this review, concentrating on recent achievements. Additionally, selected examples of aminobisphosphonate derivatization illustrate their usefulness for obtaining new diagnostic and therapeutic agents.

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“…A morbimortalidade da Doença de Chagas no Brasil é significativa, vitimando 25% ou mais dos indivíduos infectados, que adquirem cardiopatia chagásica crônica evolutiva (DIAS, 2000;SDR, 2002;SZAJNMAN et al, 2005).…”

Section: Doença De Chagasunclassified

Abordagem da Latenciação de Fármacos como Ferramenta para Descoberta de novos Antichagásicos

Serafim¹,

Chin²,

Ribeiro³

et al. 2011

RBM

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RESUMOA doença de Chagas, descoberta por Carlos Chagas há mais de um século, ainda constitui um grave problema de Saúde Pública. É considerada doença extremamente negligenciada, uma vez que afeta particularmente as populações dos países em desenvolvimento. Os pacientes dessa doença são, em sua maioria, de baixa renda e, não representando mercado, ficam excluídos do escopo e dos esforços de Pesquisa e Desenvolvimento das Indústrias Farmacêuticas. Estima-se que entre 8 e 11 milhões de indivíduos estejam infectados pelo Trypanosoma cruzi, agente etiológico da doença, e em, aproximadamente, 100 milhões, a população em risco na América Latina. Considerando que o tratamento da doença de Chagas continua sendo um desafio, pois apenas dois fármacos nitro-heterocíclicos são comercializados no mundo: nifurtimox e benznidazol, sendo este último o único fármaco disponível no mercado brasileiro; no entanto, esses fármacos são ativos na fase aguda da doença e o tratamento é ineficaz em pacientes na fase crônica, portanto, é relevante o desenvolvimento de agentes antichagásicos eficazes, principalmente para a fase crônica da doença. Este trabalho aborda a importância da latenciação para o desenvolvimento de novos pró-fármacos. Diversas técnicas metodológicas vêm sendo descritas na literatura, permitindo avanços significativos no planejamento e desenvolvimento de novos agentes antichagásicos, com ênfase na busca de pró-fármacos que permitem o aprimoramento do fármaco matriz.

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Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase

Cited by 75 publications

References 43 publications

Lycopodium clavatum and Lycopodium complanatum subsp. chamaecyparissus ekstrelerinin antiprotozoal aktivitesi ve sitotoksisitesi

Lycopodium clavatum and Lycopodium complanatum subsp. chamaecyparissus ekstrelerinin antiprotozoal aktivitesi ve sitotoksisitesi

Synthetic Procedures Leading towards Aminobisphosphonates

Abordagem da Latenciação de Fármacos como Ferramenta para Descoberta de novos Antichagásicos

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