KRM 1648: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
ID Source | ID |
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PubMed CID | 135431094 |
CHEMBL ID | 236297 |
CHEBI ID | 188526 |
SCHEMBL ID | 76007 |
MeSH ID | M0188424 |
Synonym |
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krm-1648 & mao-bushi-saishin-to |
krm-1648 & mbst |
2,7-(epoxy[1,11,13]pentadecatrienoimino)-6h-benzofuro[4,5-a]phenoxazine-1,6,15(2h)-trione, 25-(acetyloxy)-5,12,21,23-tetrahydroxy-27-methoxy-2,4,16,20,22,24,26-heptamethyl-10-[4-(2-methylpropyl)-1-piperazinyl]-, (2s,16z,18e,20s,21s,22r,23r,24r,25s,26r,27s |
krm-1648 and yokuinin |
D02550 |
rlz , |
rifalazil (usan/inn) |
benzoxazinorifamycin |
krm-1648 & scretory leukocyte protease inhibitor |
129791-92-0 |
3'-hydroxy-5'-(4-isobutylpiperazinyl)benzoxazinorifamycin |
krm 1648 |
krm-1648 |
[tetrahydroxy-(4-isobutylpiperazin-1-yl)-methoxy-heptamethyl-trioxo-[?]yl] acetate |
rifamycin viii, 1',4-didehydro-1-deoxy-1,4-dihydro-3'-hydroxy-5'-[4-(2-methylpropyl)-1-piperazinyl]-1-oxo- |
pa-1648 |
(2s,20s,21s,22r,23r,24r,25s,26r,27s)-5,12,21,23-tetrahydroxy-10-(4-isobutylpiperazin-1-yl)-27-methoxy-2,4,16,20,22,24,26-heptamethyl-1,6,15-trioxo-1,2-dihydro-6h-2,7-(epoxypentadeca[1,11,13]trienoimino)[1]benzofuro[4,5-a]phenoxazin-25-yl acetate |
rifalazil |
rifalazil [usan:inn] |
(2s,16z,18e,20s,21s,22r,23r,24r,25s,26r,27s,28e)-5,12,21,23,25-pentahydroxy-10-(4-isobutyl-1-piperazinyl)-27-methoxy-2,4,16,20,22,24,26-heptamethyl-2,7-(epoxypentadeca(1,11,13)trienimino)-6h-benzofuro(4,5-a)phenoxazine-1(2h),6,15-trione 25-acetate |
abi 1648 |
rifamycin viii, 1',4-didehydro-1-deoxy-1,4-dihydro-3'-hydroxy-5'-(4-(2-methylpropyl)-1-piperazinyl)-1-oxo- |
CHEMBL236297 |
CHEBI:188526 |
[(7s,9e,11s,12r,13s,14r,15r,16r,17s,18s,19e,21z)-2,6,15,17-tetrahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-30-[4-(2-methylpropyl)piperazin-1-yl]-23,32,37-trioxo-8,27,38-trioxa-24,34-diazahexacyclo[23.11.1.14,7.05,36.026,35.028,33]octatriaconta-1,3, |
abi1648 |
abi-1648 |
unii-s1976te8qk |
s1976te8qk , |
3'-hydroxy-5'-(4-isobutyl-1-piperazinyl)benzoxazinorifamycin |
DB04934 |
SCHEMBL76007 |
rifalazil [mi] |
1',4-didehydro-1-deoxy-1,4-dihydro-3'-hydroxy-5'-(4-(2-methylpropyl)-1-piperazinyl)-1-oxorifamycin viii |
rifalazil [usan] |
rifalazil [inn] |
(7s,9e,11s,12r,13s,14r,15r,16r,17s,18s,19e,21z)-2,15,17,32-tetrahydroxy-30-(4-isobutyl-1-piperazinyl)-11-methoxy-3,7,12,14,16,18,22-heptamethyl-6,23,37-trioxo-8,27,38-trioxa-24,34-diazahexacyclo[23.11;.1.14,7.05,36.026,35.028,33]octatriaconta-1(36),2,4,9, |
HY-105099 |
bdbm50491559 |
Q7333206 |
CS-0024983 |
Excerpt | Reference |
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" The overall treatment-emergent adverse event (TEAE) and treatment-related TEAE rates were lower in the rifalazil group (68% and 55%) than in the azithromycin group (71% and 62%), respectively." | ( Randomized, double-blind, multicenter safety and efficacy study of rifalazil compared with azithromycin for treatment of uncomplicated genital Chlamydia trachomatis infection in women. Batteiger, BE; Geisler, WM; Hurwitz, SJ; Koltun, WD; Mathew, J; Mayes, A; Morgan, F; Pascual, ML; Sayada, C; Schinazi, RF; Tao, S, 2014) |
Excerpt | Reference |
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" We investigated the activity of three doses of the semisynthetic benzoxazinorifamycin KRM 1648, alone or in combination with ethambutol or clarithromycin, in beige mice challenged with the MAC strain 101." | ( Activity of KRM 1648 alone or in combination with ethambutol or clarithromycin against Mycobacterium avium in beige mouse model of disseminated infection. Bermudez, LE; Inderlied, CB; Kolonoski, P; Young, LS, 1994) |
"In this study, the in vitro and in vivo anti-Mycobacterium leprae activity of the newly developed benzoxazinorifamycin, KRM-1648, in combination with clofazimine (CFZ) or dapsone (DDS) was evaluated." | ( Therapeutic efficacy of benzoxazinorifamycin, KRM-1648, in combination with other antimicrobials against Mycobacterium leprae infection induced in nude mice. Dekio, S; Saito, H; Sato, K; Tomioka, H, 1994) |
"A study was performed on the therapeutic efficacy of KRM-1648 combined with LC9018 in beige mice infected with Mycobacterium intracellulare." | ( [Therapeutic efficacy of a benzoxazinorifamycin, KRM-1648, combined with a immunopotentiator, LC9018, in Mycobacterium intracellulare infection induced in beige mice]. Hidaka, T; Saito, H; Sato, K; Tomioka, H, 1993) |
"The activity of KRM-1648, alone and in combination with isoniazid, was compared with those of isoniazid, rifampin, and the combination of rifampin plus isoniazid in a murine model of tuberculosis." | ( Activity of KRM-1648 in combination with isoniazid against Mycobacterium tuberculosis in a murine model. Cynamon, MH; Klemens, SP, 1996) |
"The in vivo activities of KRM-1648 alone or in combination with both ethambutol (EB) and kanamycin (KM) or clarithromycin (CAM) were tested against Mycobacterium intracellulare infections in beige mice." | ( Activity of KRM-1648 alone or in combination with both ethambutol and kanamycin or clarithromycin against Mycobacterium intracellulare infections in beige mice. Amitani, R; Kuze, F; Murayama, T; Suzuki, K; Tanaka, E; Yamamoto, T, 1996) |
"In the present study, we evaluated the in vivo anti-Mycobacterium leprae activities of KRM-1648 (KRM) given at long intervals in combination with ofloxacin (OFLX), clofazimine (CFZ), and dapsone (DDS)." | ( Studies on therapeutic activity of benzoxazinorifamycin KRM-1648 in combination with other antimicrobial agents and biological response modifiers interferon-gamma and granulocyte-macrophage colony-stimulating factor against M. leprae infection in athymic Maw, WW; Saito, H; Sato, K; Tomioka, H, 1997) |
"The activity of KRM 1648 (KRM), a new benzoxazinorifamycin, and rifabutin (RBT), alone or in combination with clarithromycin (CLA), was evaluated against Mycobacterium avium complex (MAC) that multiplied in human alveolar macrophages (AM)." | ( Activity of KRM 1648 or rifabutin alone or in combination with clarithromycin against Mycobacterium avium complex in human alveolar macrophages. Amitani, R; Hashimoto, T; Kuze, F; Matsumoto, H; Suzuki, K; Tanaka, E; Tsuyuguchi, K; Yamamoto, T, 1997) |
"According to this human alveolar macrophage model of MAC infection, KRM and RBT in combination with CLA was found to be a promising candidate against human pulmonary MAC infection, and deserves clinical evaluation." | ( Activity of KRM 1648 or rifabutin alone or in combination with clarithromycin against Mycobacterium avium complex in human alveolar macrophages. Amitani, R; Hashimoto, T; Kuze, F; Matsumoto, H; Suzuki, K; Tanaka, E; Tsuyuguchi, K; Yamamoto, T, 1997) |
"The effects of half-sized secretory leukocyte protease inhibitor or diclofenac sodium administered alone or in combination with the benzoxazinorifamycin KRM-1648 on the therapeutic efficacy of KRM-1648 against Mycobacterium avium complex (MAC) in mice were studied." | ( Therapeutic effects of benzoxazinorifamycin KRM-1648 administered alone or in combination with a half-sized secretory leukocyte protease inhibitor or the nonsteroidal anti-inflammatory drug diclofenac sodium against Mycobacterium avium complex infection i Kawahara, S; Kawauchi, H; Sano, C; Sato, K; Shimizu, T; Tomioka, H, 1999) |
"Rifalazil (formerly known as KRM-1648) in combination with isoniazid has been found to be more active than rifampin/isoniazid." | ( Durable cure for tuberculosis: rifalazil in combination with isoniazid in a murine model of Mycobacterium tuberculosis infection. Cynamon, MH; DeStefano, MS; Shoen, CM, 2000) |
"The antimicrobial effect of a benzoxazinorifamycin, KRM-1648, either alone or in combination with ofloxacin, was evaluated in vitro against two type strains and six clinical isolates of Mycobacterium ulcerans." | ( In vitro activity of KRM-1648, either singly or in combination with ofloxacin, against Mycobacterium ulcerans. Dhople, AM, 2001) |
" Similar to ofloxacin and levofloxacin, sitafloxacin also exhibited synergistic activity when combined with either rifabutin or KRM-1648, but not with rifampin." | ( In-vitro activity of sitafloxacin (DU-6859a), either singly or in combination with rifampin analogs, against Mycobacterium leprae. Dhople, AM; Namba, K, 2003) |
" To address the high-frequency resistance seen with rifamycins, we assessed the ability of rifalazil, alone and in combination with vancomycin, to both kill cells and to suppress the appearance of resistant mutants in log and stationary phase Staphylococcus aureus cultures, using high cell densities in an in vitro kill curve model." | ( In vitro time-kill activities of rifalazil, alone and in combination with vancomycin, against logarithmic and stationary cultures of Staphylococcus aureus. Farquhar, R; Murphy, CK; Osburne, MS; Rothstein, DM, 2006) |
" To explore strategies to overcome resistance development, we studied the effects of rifalazil in combination with several different antibiotics in an in vitro time-kill model, against both log phase and stationary phase Staphylococcus aureus cells." | ( Enhanced activity of rifalazil in combination with levofloxacin, linezolid, or mupirocin against Staphylococcus aureus in vitro. Murphy, CK; Osburne, MS; Rothstein, DM, 2006) |
Excerpt | Reference |
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"Macrocycles are ideal in efforts to tackle "difficult" targets, but our understanding of what makes them cell permeable and orally bioavailable is limited." | ( Macrocyclic drugs and clinical candidates: what can medicinal chemists learn from their properties? Giordanetto, F; Kihlberg, J, 2014) |
Excerpt | Reference |
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" bovis Ravenel infection, three rifamycin derivatives gave "distinctive dose-response curves" in the correlation of dose sizes with the mean survival times or "log10CFU/lungs reductions"." | ( [Therapeutic efficacy of benzoxazinorifamycin KRM-1648 against experimental murine tuberculosis: (1). A study on the efficacy of short course treatment with the intratracheal and intravenous infection model]. Doi, N, 1998) |
Class | Description |
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phenoxazine | |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
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[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1653515 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.1 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID669186 | Antitubercular activity against Mycobacterium tuberculosis H37Rv in aerobic conditions after 7 days by microplate-based alamar blue assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID1879496 | Antibacterial activity against Clostridioides difficile ATCC 9689 | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens. |
AID669178 | Inhibition of Mycobacterium tuberculosis wild type RNA polymerase by rolling circle transcription assay in the presence of sigmaA factor | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID1653513 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.025 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID1653516 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.2 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID1653394 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.05 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID1879497 | Antibacterial activity against Helicobacter pylori ATCC 700392 | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens. |
AID669180 | Inhibition of Mycobacterium tuberculosis RNA polymerase S450L mutant by rolling circle transcription assay in the presence of sigmaA factor | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID1653397 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.05 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID669197 | Metabolic stability in mouse microsomes assessed as compound remaining after 30 mins | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID301526 | Antibacterial activity against rifamycin-sensitive Staphylococcus aureus CB190 ATCC 29213 | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Preparation and in vitro anti-staphylococcal activity of novel 11-deoxy-11-hydroxyiminorifamycins. |
AID1879495 | Antibacterial activity against Staphylococcus aureus ATCC 29213 | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens. |
AID1653514 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.05 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID1065392 | Half life in human at 25 mg, po administered through fat rich diet | 2014 | Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2 | Macrocyclic drugs and clinical candidates: what can medicinal chemists learn from their properties? |
AID669191 | Activation of PXR in human DPX2 cells at 100 uM after 24 hrs by luciferase reporter gene assay relative to control | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID1653396 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.1 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID341089 | Antimicrobial activity against Clostridium difficile clinical isolates by agar dilution method | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8 | In vitro activities of 15 antimicrobial agents against 110 toxigenic clostridium difficile clinical isolates collected from 1983 to 2004. |
AID1653510 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.2 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID669190 | Activation of PXR in human DPX2 cells at <100 uM after 24 hrs by luciferase reporter gene assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID1653509 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.1 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID1653522 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.2 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID748179 | Inhibition of rifamycin-resistant Escherichia coli RNA polymerase D516V mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC45 | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins. |
AID748180 | Inhibition of wild type Escherichia coli RNA polymerase after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC45 | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins. |
AID669198 | Metabolic stability in human microsomes assessed as compound remaining after 30 mins | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID669608 | Half life in human | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID669199 | Half life in mouse microsomes | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID748178 | Inhibition of rifamycin-resistant Escherichia coli RNA polymerase H526Y mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC45 | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins. |
AID1653395 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.025 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID669179 | Inhibition of Mycobacterium tuberculosis RNA polymerase D435V mutant by rolling circle transcription assay in the presence of sigmaA factor | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID520287 | Antimicrobial activity against Chlamydia pneumoniae AR39 infected in C57BL/6J mouse at 1 mg/kg, ip assessed as bacterial load measured on day 10 post infection relative to control | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Efficacy of benzoxazinorifamycins in a mouse model of Chlamydia pneumoniae lung infection. |
AID1653393 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.025 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID669187 | Antitubercular activity against Mycobacterium tuberculosis H37Rv in anaerobic conditions after 11 days by luminescnece-based low-oxygen recovery assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID1653521 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.1 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID1653519 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.025 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID669192 | Cytotoxicity against human DPX2 cells expressing PXR assessed as decrease in cell viability at 100 uM after 24 hrs relative to control | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID301527 | Antibacterial activity against rifamycin-resistance Staphylococcus aureus CB372 | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Preparation and in vitro anti-staphylococcal activity of novel 11-deoxy-11-hydroxyiminorifamycins. |
AID301528 | Antibacterial activity against rifamycin-resistance Staphylococcus aureus CB370 | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Preparation and in vitro anti-staphylococcal activity of novel 11-deoxy-11-hydroxyiminorifamycins. |
AID1653390 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.2 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID748177 | Inhibition of rifamycin-resistant Escherichia coli RNA polymerase S531L mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC45 | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins. |
AID669176 | Inhibition of Mycobacterium tuberculosis wild type RNA polymerase by rolling circle transcription assay in the absence of sigmaA factor | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID520288 | Antimicrobial activity against Chlamydia pneumoniae AR39 infected in C57BL/6J mouse at 3 mg/kg, ip assessed as bacterial load measured on day 10 post infection relative to control | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Efficacy of benzoxazinorifamycins in a mouse model of Chlamydia pneumoniae lung infection. |
AID1653520 | Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.05 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol) | 2019 | Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13 | Insights of synthetic analogues of anti-leprosy agents. |
AID520286 | Antimicrobial activity against Chlamydia pneumoniae TW-183 after 72 hrs by twofold dilution method | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5 | Efficacy of benzoxazinorifamycins in a mouse model of Chlamydia pneumoniae lung infection. |
AID669177 | Inhibition of Mycobacterium tuberculosis RNA polymerase H445Y mutant by rolling circle transcription assay in the presence of sigmaA factor | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
AID669200 | Half life in human microsomes | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8 | Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 65 (53.28) | 18.2507 |
2000's | 46 (37.70) | 29.6817 |
2010's | 6 (4.92) | 24.3611 |
2020's | 5 (4.10) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 9 (7.32%) | 5.53% |
Reviews | 14 (11.38%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 100 (81.30%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |