ArticleAntimicrobial agents and chemotherapy1991
In vitro antimycobacterial activities of newly synthesized benzoxazinorifamycins.
Article in Antimicrobial agents and chemotherapy, 1991. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 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
27 citing papers in PubMed, 125 citations in OpenAlex.
- Late-Stage Functionalization of the Rifamycin Core via Click Chemistry Toward New Antibacterial Derivatives.Molecules (Basel, Switzerland) · 2026Article
- Recent Biochemical Advances in Antitubercular Drugs: Challenges and Future.Current topics in medicinal chemistry · 2024Review
- Therapeutic efficacy of rifalazil (KRM-1648) in a M. ulcerans-induced Buruli ulcer mouse model.PloS one · 2022Article
- A Semisynthetic Kanglemycin Shows In Vivo Efficacy against High-Burden Rifampicin Resistant Pathogens.ACS infectious diseases · 2020Article
- Preclinical Models of Nontuberculous Mycobacteria Infection for Early Drug Discovery and Vaccine Research.Pathogens (Basel, Switzerland) · 2020Review
- In vitro anti-Helicobacter pylori activities of new rifamycin derivatives, KRM-1648 and KRM-1657.Antimicrobial agents and chemotherapy · 1999Article
- Effects of the Chinese traditional medicine mao-bushi-saishin-to on therapeutic efficacy of a new benzoxazinorifamycin, KRM-1648, against Mycobacterium avium infection in mice.Antimicrobial agents and chemotherapy · 1999Article
- Effects of benzoxazinorifamycin KRM-1648 on cytokine production at sites of Mycobacterium avium complex infection induced in mice.Antimicrobial agents and chemotherapy · 1997Article
- Pharmacokinetics of KRM-1648, a new benzoxazinorifamycin, in rats and dogs.Antimicrobial agents and chemotherapy · 1996Article
- Luciferase in vivo expression technology: use of recombinant mycobacterial reporter strains to evaluate antimycobacterial activity in mice.Antimicrobial agents and chemotherapy · 1996Article
- Activity of KRM-1648 in combination with isoniazid against Mycobacterium tuberculosis in a murine model.Antimicrobial agents and chemotherapy · 1996Article
- In vitro bactericidal and in vivo therapeutic activities of a new rifamycin derivative, KRM-1648, against Mycobacterium tuberculosis.Antimicrobial agents and chemotherapy · 1996Article
- Activity of KRM-1648 alone or in combination with both ethambutol and kanamycin or clarithromycin against Mycobacterium intracellulare infections in beige mice.Antimicrobial agents and chemotherapy · 1996Article
- How effective is KRM-1648 in treatment of disseminated Mycobacterium avium complex infections in beige mice?Antimicrobial agents and chemotherapy · 1996Article
- Anticytomegaloviral activity of methotrexate associated with preferential accumulation of drug by cytomegalovirus-infected cells.Antimicrobial agents and chemotherapy · 1996Article
- In vitro and in vivo activities of the benzoxazinorifamycin KRM-1648 against Mycobacterium tuberculosis.Antimicrobial agents and chemotherapy · 1995Article
- Antimycobacterial activity of a new rifamycin derivative, 3-(4-cinnamylpiperazinyl iminomethyl) rifamycin SV (T9).Antimicrobial agents and chemotherapy · 1995Article
- Mechanism of action of antimycobacterial activity of the new benzoxazinorifamycin KRM-1648.Antimicrobial agents and chemotherapy · 1995Article
- In vitro activity of the benzoxazinorifamycin KRM-1648 against drug-susceptible and multidrug-resistant tubercle bacilli.Antimicrobial agents and chemotherapy · 1995Article
- In vitro and in vivo antimycobacterial activities of a new quinolone, DU-6859a.Antimicrobial agents and chemotherapy · 1994Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Newly synthesized rifamycin derivatives, KRM-1648, KRM-1657, KRM-1668, KRM-1686, and KRM-1687, having the chemical structures of 3'-hydroxy-5'-(4-alkylpiperazinyl)-benzoxazinorifamycins (alkyl residues: isobutyl, propyl, sec-butyl, sec-butyl [R configuration], and sec-butyl [S configuration], respectively), were studied for their in vitro antimycobacterial activities. Representative (KRM-1648) MICs for 90% of the strains tested, determined by the agar dilution method on 7H11 medium, of various pathogenic mycobacteria (9 species, 174 strains) were as follows (in micrograms per milliliter): Mycobacterium tuberculosis (rifampin [RMP]-susceptible strains), less than or equal to 0.0125; M. tuberculosis (RMP-resistant strains), 12.5; M. kansasii, 0.05; M. marinum, less than or equal to 0.0125; M. scrofulaceum, 0.1; M. avium, 1.56; M. intracellulare, 0.1; M. fortuitum, greater than 100; and M. chelonae subsp. abscessus and M. chelonae subsp. chelonae, greater than 100. These values are more than 64 times lower than those of RMP, except for the values against RMP-resistant M. tuberculosis (8 times lower) and those against rapid growers, including M. fortuitum and M. chelonae (the same as those of RMP). The other derivatives had similar levels of in vitro activity against these mycobacteria. When murine peritoneal macrophages in which M. intracellulare was phagocytosed in vitro were cultured in the presence of the benzoxazinorifamycins (1 microgram/ml), much more rapid killing of the organisms ingested in the macrophages was seen compared with when the same amount of RMP was added to the medium. The addition of benzoxazinorifamycins at the concentration of 0.05 micrograms/ml caused more marked suppression of intracellular growth of the organisms compared with addition of RMP. KRM-1648 and KRM-1657 inhibited intracellular growth of M. tuberculosis, and their efficacies were much greater than that of RMP.
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