Combination drug delivery approaches for tuberculosis

Santos, Filipa; Duarte, Ana Rita C.

doi:10.1016/b978-0-323-85873-1.00006-x

Cited by 1 publication

(1 citation statement)

References 164 publications

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“…In order to prevent this unfavorable phenomenon, the rules of pharmacotherapy should be scrupulously followed [6,7]. Due to the fact that tuberculosis is still one of the diseases leading to death and is a threat mainly due to the constantly developing chemotherapeutic and antibiotic resistant strains of Mycobacterium tuberculosis, new, effective anti-tuberculosis Materials 2022, 15, 5513 2 of 16 agents are being sought [8,9], especially given that the most effective anti-tuberculosis drug is still isoniazid, which was introduced into medical treatment in 1952 [10].…”

Section: Introductionmentioning

confidence: 99%

N′-Substituted 4-Phenylpicolinohydrazonamides with Thiosemicarbazone Moiety as New Potential Antitubercular Agents: Synthesis, Structure and Evaluation of Antimicrobial Activity

et al. 2022

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Three new 4-phenylpicolin derivatives with a thiosemicarbazone structure were synthesized and evaluated for tuberculostatic activity. The compounds were obtained by the condensation of methyl 4-phenylpicolonimidate with the corresponding cycloalkylamino-1-carbothiohydrazides. The 1H NMR temperature spectra obtained showed proton lability at the nitrogen atom N2, and X-ray crystallography confirmed the zwitterionic structure of all products. ADME calculations indicate that the compounds can be tested as future drugs. All compounds were absorbed in the gastrointestinal tract. All compounds also showed very good tuberculostatic activity (MIC 3.1–12.5 µg/mL). Derivative 1b showed the best selectivity for M. tuberculosis compared to the other pathogenic species tested. The study has allowed the emergence of imine derivative 1b as a good structure for further optimization in the search for antitubercular drugs.

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