ArticleOrganic & biomolecular chemistry2016
Synthesis and evaluation of new 2-aminothiophenes against Mycobacterium tuberculosis.
Article in Organic & biomolecular chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 45 citations in OpenAlex.
- Synthesis and evaluation of Trehalose-Pks13 inhibitor conjugates targeting mycobacteria.Carbohydrate research · 2025Article
- Synthesis and biological studies of 2-aminothiophene derivatives as positive allosteric modulators of glucagon-like peptide 1 receptor.Bioorganic & medicinal chemistry · 2024Article
- Inhibitors of the Thioesterase Activity ofACS infectious diseases · 2024Article
- Green methodologies for the synthesis of 2-aminothiophene.Environmental chemistry letters · 2023Review
- Synthesis and Anti-Inflammatory Activity of 2-Amino-4,5,6,7-tetrahydrobenzo[b]thiophene-Derived NRF2 Activators.ChemistryOpen · 2022Article
- OvercomingActa pharmaceutica Sinica. B · 2022Review
- 2-Aminothiophene derivatives as a new class of positive allosteric modulators of glucagon-like peptide 1 receptor.Chemical biology & drug design · 2022Article
- Catalyst-Free Site Selective Hydroxyalkylation of 5-Phenylthiophen-2-amine with α-Trifluoromethyl Ketones through Electrophilic Aromatic Substitution.Molecules (Basel, Switzerland) · 2022Article
- Article
- Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.European journal of medicinal chemistry · 2021Article
- 2-((3,5-Dinitrobenzyl)thio)quinazolinones: Potent Antimycobacterial Agents Activated by Deazaflavin (FJournal of medicinal chemistry · 2021Article
- Multicomponent Petasis Reaction for the Synthesis of Functionalized 2-Aminothiophenes and Thienodiazepines.ACS combinatorial science · 2020Article
- Screening of the Pathogen Box reveals new starting points for anti-trypanosomal drug discovery.MedChemComm · 2018Article
- Mycobacterial cell wall biosynthesis: a multifaceted antibiotic target.Parasitology · 2018Review
- An Antibacterial β-Lactone Kills Mycobacterium tuberculosis by Disrupting Mycolic Acid Biosynthesis.Angewandte Chemie (International ed. in English) · 2018Article
- Crystallization and structure analysis of the core motif of the Pks13 acyltransferase domain fromPeerJ · 2018Article
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Authors and funding
9 authors at 3 institutions in 3 countries.
Funding
Abstract
Tuberculosis (TB) and its drug resistant forms kills more people than any other infectious disease. This fact emphasizes the need to identify new drugs to treat TB. 2-Aminothiophenes (2AT) have been reported to inhibit Pks13, a validated anti-TB drug target. We synthesized a library of 42 2AT compounds. Among these, compound 33 showed remarkable potency against Mycobacterium tuberculosis (Mtb) H37RV (MIC = 0.23 μM) and showed an impressive potency (MIC = 0.20-0.44 μM) against Mtb strains resistant to isoniazid, rifampicin and fluoroquinolones. The site of action for the compound 33 is presumed to be Pks13 or an earlier enzyme in the mycolic acid biosynthetic pathway. This inference is based on structural similarity of the compound 33 with known Pks13 inhibitors, which is corroborated by mycolic acid biosynthesis studies showing that the compound strongly inhibits the biosynthesis of all forms of mycolic acid in Mtb. In summary, these studies suggest 33 represents a promising anti-TB lead that exhibits activity well below toxicity to human monocytic cells.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.