Compositor musical e professor: uma visão comparativa

Barreiro, Aguida C. M.; Barreiro, Daniel Luís

doi:10.11606/issn.2316-9125.v0i21p43-53

Cited by 2 publications

(2 citation statements)

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“…The next step involves the techniques required to derive new analogs, homologues, or structural congeners with improved pharmacological properties. For this purpose, general processes of simplification and molecular association have been applied [102][103][104] . In summary, the final product was designed by the partial molecular modification of the prototype compound with the inclusion or exclusion of chemical structures that favor greater potency, stability, and safety characteristics than the original compound 68 .…”

Section: Structural Modificationmentioning

confidence: 99%

Searching for new antifungals for the treatment of cryptococcosis

Sousa

Almeida

Frickmann

et al. 2023

Rev. Soc. Bras. Med. Trop.

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There is a consensus that the antifungal repertoire for the treatment of cryptococcal infections is limited. Standard treatment involves the administration of an antifungal drug derived from natural sources (i.e., amphotericin B) and two other drugs developed synthetically (i.e., flucytosine and fluconazole). Despite treatment, the mortality rates associated with fungal cryptococcosis are high. Amphotericin B and flucytosine are toxic, require intravenous administration, and are usually unavailable in low-income countries because of their high cost. However, fluconazole is cost-effective, widely available, and harmless with regard to its side effects. However, fluconazole is a fungistatic agent that has contributed considerably to the increase in fungal resistance and frequent relapses in patients with cryptococcal meningitis. Therefore, there is an unquestionable need to identify new alternatives or adjuvants to conventional drugs for the treatment of cryptococcosis. A potential antifungal agent should be able to kill cryptococci and "bypass" the virulence mechanism of the yeast. Furthermore, it should have fungicidal action, low toxicity, high selectivity, easily penetrate the central nervous system, and widely available.In this review, we describe cryptococcosis, its conventional therapy, and failures arising from the use of drugs traditionally considered to be the reference standard. Additionally, we present the approaches used for the discovery of new drugs to counteract cryptococcosis, ranging from the conventional screening of natural products to the inclusion of structural modifications to optimize anticryptococcal activity, as well as drug repositioning and combined therapies.

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Section: Structural Modificationmentioning

confidence: 99%

Searching for new antifungals for the treatment of cryptococcosis

Sousa

Almeida

Frickmann

et al. 2023

Rev. Soc. Bras. Med. Trop.

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“…[3][4][5][6] However, the methylenedioxy group frequently found in many secondary metabolities has not received much attention. At this point, it is worth mentioning the work of Barreiro et al 7 which focus on the preparation of indolecarboxylic acid analogue to the anti-inflammatory indomethacin from the methylenedioxyarene safrole.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of new indolecarboxylic acids related to the plant hormone indoleacetic acid IAA

Rosa

Rebelo

Nascimento

2003

J. Braz. Chem. Soc.

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A síntese dos ácidos 5,6-metilenodioxi-indol-3-il-metanóico 8 e 5,6-metilenodioxi-indol-3-ilacético 13 é descrita. Piperonal foi empregado como material de partida, sendo a construção do heterociclo altamente regioespecífica e está fundamentada na reação de Hemetsberger do correspondente β-azidoestireno. O composto 8 foi obtido como intermediário pivotal na preparação de 13, tendo-se conduzida a reação de Mannich para a introdução da cadeia lateral alquílica. A rota sintética empregada englobou oito etapas e conduziu a formação de 13 com rendimento total de 26%. A formação do heterociclo indólico via ciclização redutiva de o, β-dinitroestireno é também apresentada.The synthesis of 5,6-methylenedioxy-indol-3-yl-methanoic acid 8 and 5,6-methylenedioxyindol-3-yl-acetic acid 13 is described. Piperonal was employed as starting material, and the construction of the heterocyclic ring based on the Hemetsberger reaction of the corresponding β-azidostyrene was highly regiospecific. Compound 8 was obtained as a key intermediate towards 13, and a Mannich reaction was used to introduce the required alkyl side chain. The route comprised eight steps giving 13 in 26% overall yield. The formation of the indolic ring via reductive cyclisation of o, β-dinitrostyrene is also presented.

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Compositor musical e professor: uma visão comparativa

Abstract: 5. SADIE, S (ed.) Dicionário .... op. cit. p. 500. 6. SADIE, S (ed.) Dicionário .... op. cit. p. 919.

Cited by 2 publications

References 0 publications

Searching for new antifungals for the treatment of cryptococcosis

Searching for new antifungals for the treatment of cryptococcosis

Synthesis of new indolecarboxylic acids related to the plant hormone indoleacetic acid IAA

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