Antituberculosis activity

The increase in new cases of drug resistance to first-line drugs such as ethambutol (ETB) makes it necessary to develop improvements for antituberculosis drugs. A new method for improving the bioavailability of active pharmaceutical ingredient (API) was investigated for preventing drug resistance and side-effects of antituberculosis drugs. In this study, an antituberculosis drug delivery system using β-cyclodextrin (β-CD) as the supramolecular carrier of ETB was prepared using the kneading method.

10p lyhuyenthu 31-01-2023 3 1   Download

The new compounds 7a–k, 8a–k, and 9a–k were synthesized from flavonones 4–6, which can be considered new precursors for quinoline synthesis through a one-step reaction. All the target compounds (7a–k, 8a–k, and 9a–k) were evaluated for their in vitro antimicrobial activity against nine test microorganisms. They showed the most activity against Mycobacterium smegmatis with minimum inhibitory concentrations (MIC) of 62.5–500 µg/mL, indicating their potential uses as antituberculosis agents. Among them 8a–k (m-fluoride) were the most active compounds against M. smegmatis (MIC, 62.5–125 µg/mL).

17p langthannam 29-12-2021 11 0   Download

A series of 5-substituted-1,3,4-thiadiazole-based fluoroquinolone derivatives were designed as potential antibacterial and anticancer agents using a molecular hybridization approach. The target compounds 16–25 were synthesized by reacting the corresponding N-(5-substituted-1,3,4-thiadiazol-2-yl)-2-chloroacetamides with ciprofloxacin or norfloxacin. The purity and identity of the synthesized compounds were determined by the use of chromatographic and spectral techniques (NMR, IR, MS, etc.) besides elemental analysis.

20p tudichquannguyet 29-11-2021 8 2   Download

Finding novel cholinesterase inhibitors that would be able to cross the blood–brain barrier, have favorable pharmacokinetic parameters, and reduce hepatotoxicity along with other side effects has been the main focus of investigations dealing with Alzheimer disease. In this study we evaluated cholinesterase inhibitory and antioxidant activity of seven oxazole derivatives. These compounds have been efficiently and sustainably prepared by photochemical electrocyclization reaction.

7p tudichquannguyet 29-11-2021 10 2   Download

A series of 3-mercapto-1,2,4-triazole–pyrrole hybrids was designed as antimycobacterial agents by employing 5- (4-(1H -pyrrol-1-yl)phenyl)-4H -1,2,4-triazole-3-thiol as the scaffold onto which several types of moieties were introduced in the triazole ring at N-4 and N-2 and as substituents of the mercapto function. The aforementioned moieties are an allyl or a phenyl moiety at N-4; an aminomethyl group at N-2; or methyl, substituted benzyl, ethoxycarbonylmethyl, or substituted phenacyl at sulfur.

16p tudichquannguyet 29-11-2021 8 1   Download

The nicotinamidase⁄pyrazinamidase (PncA) ofMycobacterium tuberculosis is involved in the activation of the important front-line antituberculosis drug pyrazinamide by converting it into the active form, pyrazinoic acid. Mutations in thepncA gene cause pyrazinamide resistance in M. tuber-culosis.

10p media19 05-03-2013 31 1   Download

We included studies that evaluated the performance of the most recent generation of commercial, RD1 antigen-based IGRAs (QFT-GIT and T-SPOT) among adults (age $15 years) with suspected active pulmonary tuberculosis or confirmed tuberculosis in low- and middle-income countries [22]; the World Bank Country Classification was considered as a surrogate for national tuberculosis incidence. HIV infection was established either by documented serological testing or self-report.

10p taisaocothedung 12-01-2013 39 1   Download