In present investigation, a series of substituted phenyl-5,6-dimethoxy-1-oxo-2,5-dihydro-1H-2-indenylmethanone analogues were synthesized and were evaluated for antimycobacterial activity against Mycobacterium tuberculosis H(37)Rv and INH resistant M. tuberculosis. All the newly synthesized compounds were showing moderate to high inhibitory activities. The compound 5,6-dimethoxy-1-oxo-2,5-dihydro-1H-2-indenyl-4-fluorophenylmethanone (5g) was found to be the most promising compounds active against M. tuberculosis H(37)Rv and isoniazid (INH) resistant M. tuberculosis with Minimum inhibitory concentration 0.10 and 0.10 microM.
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http://dx.doi.org/10.1016/j.bmcl.2009.10.034 | DOI Listing |
Arch Microbiol
January 2025
Clinical Microbiology and PK-PD Division, CSIR-Indian Institute of Integrative Medicine, Sanatnagar, Srinagar, J&K, 190005, India.
Tuberculosis (TB) remains a major global threat, with 10 million new cases and 1.5 million deaths each year. In multidrug-resistant tuberculosis (MDR-TB), resistance is most commonly observed against isoniazid (INH) and rifampicin (RIF), the two frontline drugs.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, S. Kovalevskoy Street, 22, Ekaterinburg 620137, Russia.
The synthetic approach based on a sequence of Buchwald-Hartwig cross-coupling and annulation through intramolecular oxidative cyclodehydrogenation has been used for the construction of novel 4-alkyl-4-thieno[2',3':4,5]pyrrolo[2,3-]quinoxaline derivatives. For the first time, these polycyclic compounds were evaluated for antimycobacterial activity, including extensively drug-resistant strains. A reasonable bacteriostatic effect against HRv was demonstrated.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
School of Laboratory Medicine and Medical Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa.
Coding and non-coding RNAs (ncRNAs) are potential novel markers that can be exploited for TB diagnostics in the fight against . The current study investigated the mechanisms of transcript regulation and ncRNA signatures through Total RNA Seq and small (smRNA) RNA Seq followed by Bioinformatics analysis in Beijing and F15/LAM4/KZN (KZN) clinical strains compared to the laboratory strain. Total RNA Seq revealed differential regulation of RNA transcripts in Beijing (n = 1095) and KZN (n = 856) strains compared to the laboratory H37Rv strain.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of Medical Chemistry, Institute of Chemistry, Saint Petersburg State University, Saint Petersburg 199034, Russia.
The use of the concept of privileged structures significantly accelerates the search for new leads and their optimization. 6-(methylsulfonyl)-8-(4-methyl-4-1,2,4-triazol-3-yl)-2-(5-nitro-2-furoyl)-2,6-diazaspiro[3.4]octane has been identified as a lead, with MICs of 0.
View Article and Find Full Text PDFMicroorganisms
November 2024
Department of Microbiology, Instituto Nacional de Enfermedades Respiratorias Ismael Cosío Villegas, Mexico City 14080, Mexico.
Tuberculosis (TB) is one of the most common respiratory infections worldwide, and it is caused by (). employs immune evasion mechanisms that allow the disease to become chronic. Despite extensive research, the host-pathogen interaction remains incompletely understood.
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