Clinical considerations and pharmacokinetic interactions between HIV and tuberculosis therapeutics

Maranchick, Nicole F.; Kwara, Awewura; Peloquin, Charles A.

doi:10.1080/17512433.2024.2317954

Expert Review of Clinical Pharmacology

2024

DOI: 10.1080/17512433.2024.2317954

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Clinical considerations and pharmacokinetic interactions between HIV and tuberculosis therapeutics

Nicole F. Maranchick,

Awewura Kwara,

Charles A. Peloquin

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2024

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Synthesis of 6-dialkylaminopyrimidine carboxamide analogues and their anti-tubercular properties

Tshinavhe,

Peton,

Simelane

et al. 2024

Med Chem Res

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Tuberculosis (TB) continues to be a threat to global health stability. Pyrimidine carboxamides have demonstrated potent anti-tubercular properties against clinical Mycobacterium tuberculosis, the causative agent of TB. Herein, we report a follow-up study on the synthesis of pyrimidine carboxamide molecular analogues and their anti-TB evaluation. In total, a library consisting of 37 new compounds is reported. Seven compounds (7b, 7d, 7m, 7p, 7q, 7aa, and 7ah) demonstrated excellent in vitro activities with MIC90 values below 1.00 µM. Apart from compound 7ah, compounds with improved aqueous solubility properties had lower anti-TB potency. Preliminary mode of action studies using bioluminescence assays indicate that the active compounds do not affect the integrity of mycobacterial DNA or the cell wall. The active compounds were also found to be bactericidal against replicating H37Rv Mtb strain.

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Synthesis of 6-dialkylaminopyrimidine carboxamide analogues and their anti-tubercular properties

Tshinavhe,

Peton,

Simelane

et al. 2024

Med Chem Res

View full text Add to dashboard Cite

show abstract

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Clinical considerations and pharmacokinetic interactions between HIV and tuberculosis therapeutics

Cited by 1 publication

References 115 publications

Synthesis of 6-dialkylaminopyrimidine carboxamide analogues and their anti-tubercular properties

Synthesis of 6-dialkylaminopyrimidine carboxamide analogues and their anti-tubercular properties

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