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Start Over Author "da Silva PA" Journal bioorganic medicinal chemistry
2 results on '"da Silva PA"'

1. Synthesis and antimycobacterial activity of isoniazid derivatives from renewable fatty acids.

Author

Rodrigues MO, Cantos JB, D'Oca CR, Soares KL, Coelho TS, Piovesan LA, Russowsky D, da Silva PA, and D'Oca MG

Subjects
Antitubercular Agents chemistry, Drug Resistance, Bacterial drug effects, Isoniazid chemical synthesis, Microbial Sensitivity Tests, Rifampin pharmacology, Antitubercular Agents chemical synthesis, Antitubercular Agents pharmacology, Fatty Acids chemistry, Isoniazid analogs & derivatives, Isoniazid pharmacology, Mycobacterium tuberculosis drug effects
Abstract

This work describes the synthesis of a series of fatty acid hydrazide derivatives of isoniazid (INH). The compounds were tested against Mycobacterium tuberculosis H37Rv (ATCC 27294) as well as INH-resistant (ATCC 35822 and 1896 HF) and rifampicin-resistant (ATCC 35338) M. tuberculosis strains. The fatty acid derivatives of INH showed high antimycobacterial potency against the studied strains, which is desirable for a pharmaceutical compound, suggesting that the increased lipophilicity of isoniazid plays an important role in its antimycobacterial activity., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Published
2013
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2. Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.

Author

Figueiredo R, Moiteiro C, Medeiros MA, da Silva PA, Ramos D, Spies F, Ribeiro MO, Lourenço MC, Júnior IN, Gaspar MM, Cruz ME, Curto MJ, Franzblau SG, Orozco H, Aguilar D, Hernandez-Pando R, and Costa MC

Subjects
Animals, Antitubercular Agents chemistry, Antitubercular Agents pharmacology, Drug Resistance, Bacterial, Mice, Mice, Inbred BALB C, Rifabutin pharmacology, Structure-Activity Relationship, Mycobacterium avium drug effects, Mycobacterium tuberculosis drug effects, Rifabutin analogs & derivatives, Tuberculosis drug therapy
Abstract

Clinical utility of rifabutin 1 (RBT), a potent antibiotic used in multidrug regimens for tuberculosis (TB) as well as for infections caused by Mycobacterium avium complex (MAC), has been hampered due to dose-limiting toxicity. RBT analogs 2-11 were synthesized and evaluated against M. avium 1581 and Mycobacterium tuberculosis susceptible and resistant strains in vitro. A selection of candidates were also assayed against non-replicating persistent (NRP) M. tuberculosis. Subsequent in vivo studies with the best preclinical candidate drugs 5 and 8, in a model of progressive pulmonary tuberculosis of Balb/C mice infected either with H(37)Rv drug-sensible strain or with multidrug resistant (MDR) clinical isolates, resistant to all primary antibiotics including rifampicin, were performed. The results disclosed here suggest that 5 and 8 have potential for clinical application.

Published
2009
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