ArticleAntimicrobial agents and chemotherapy2005
In vitro and in vivo activities of macrolide derivatives against Mycobacterium tuberculosis.
Article in Antimicrobial agents and chemotherapy, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 65 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
65 citing papers in PubMed, 208 citations in OpenAlex.
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- Discovery of natural-product-derived sequanamycins as potent oral anti-tuberculosis agents.Cell · 2023Article
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- Syntheses and studies of deuterated Imdiazo[1,2-a]pyridine-3-carboxamides with potent anti-tuberculosis activity and improved metabolic properties.Bioorganic chemistry · 2022Article
- Synthesis and Structure-Activity Relationships for the Anti-Mycobacterial Activity of 3-Phenyl-Pharmaceuticals (Basel, Switzerland) · 2022Article
- Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis.European journal of medicinal chemistry · 2022Article
- Synthetic studies towards isomeric pyrazolopyrimidines as potential ATP synthesis inhibitors ofTetrahedron letters · 2022Article
- "Upcycling" known molecules and targets for drug-resistant TB.Frontiers in cellular and infection microbiology · 2022Article
- Biosynthetic Interrogation of Soil Metagenomes Reveals Metamarin, an Uncommon Cyclomarin Congener with Activity againstJournal of natural products · 2021Article
- Recent Progress in the Discovery and Development of 2-Nitroimidazooxazines and 6-Nitroimidazooxazoles to Treat Tuberculosis and Neglected Tropical Diseases.Molecules (Basel, Switzerland) · 2020Review
- A review of medicinal plant of Middle East and North Africa (MENA) region as source in tuberculosis drug discovery.Saudi journal of biological sciences · 2020Review
- A Preclinical Candidate Targeting Mycobacterium tuberculosis KasA.Cell chemical biology · 2020Article
- Intracellular and in vivo evaluation of imidazo[2,1-b]thiazole-5-carboxamide anti-tuberculosis compounds.PloS one · 2020Article
- Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.Bioorganic & medicinal chemistry · 2019Article
- Rufomycin Targets ClpC1 Proteolysis in Mycobacterium tuberculosis and M. abscessus.Antimicrobial agents and chemotherapy · 2019Article
- An antimycobacterial pleuromutilin analogue effective against dormant bacilli.Bioorganic & medicinal chemistry · 2018Article
- Synthesis and Activity againstMolecules (Basel, Switzerland) · 2018Article
5 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Existing macrolides have never shown definitive clinical efficacy in tuberculosis. Recent reports suggest that ribosome methylation is involved in macrolide resistance in Mycobacterium tuberculosis, a mechanism that newer macrolides have been designed to overcome in gram-positive bacteria. Therefore, selected macrolides and ketolides (descladinose) with substitutions at positions 9, 11,12, and 6 were assessed for activity against M. tuberculosis, and those with MICs of < or = 4 microM were evaluated for cytotoxicity to Vero cells and J774A.1 macrophages. Several compounds with 9-oxime substitutions or aryl substitutions at position 6 or on 11,12 carbamates or carbazates demonstrated submicromolar MICs. For the three macrolide-ketolide pairs, macrolides demonstrated superior activity. Four compounds with low MICs and low cytotoxicity also effected significant reductions in CFU in infected macrophages. Active compounds were assessed for tolerance and the ability to reduce CFU in the lungs of BALB/c mice in an aerosol infection model. A substituted 11,12 carbazate macrolide demonstrated significant dose-dependent inhibition of M. tuberculosis growth in mice, with a 10- to 20-fold reduction of CFU in lung tissue. Structure-activity relationships, some of which are unique to M. tuberculosis, suggest several synthetic directions for further improvement of antituberculosis activity. This class appears promising for yielding a clinically useful agent for tuberculosis.
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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.