pretomanid: nitroimidazopyran derived from 5-nitroimidazoles; a prodrug that requires activation by a bacterial F420-depedent glucose-6-phosphate dehydrogenase (Fgd) and nitroreductase to activate components that then inhibit bacterial mycolic acid and protein synthesis; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 456199 |
| CHEMBL ID | 227875 |
| SCHEMBL ID | 2983011 |
| MeSH ID | M0568887 |
| Synonym |
|---|
| pretomanid [usan:inn] |
| (s)-pa 824 |
| 2xoi31yc4n , |
| 2-nitro-6-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5h-imidazo(2,1-b)(1,3)oxazine |
| unii-2xoi31yc4n |
| 5h-imidazo(2,1-b)(1,3)oxazine, 6,7-dihydro-2-nitro-6-((4-(trifluoromethoxy)phenyl)methoxy)-, (6s)- |
| 187235-37-6 |
| pa 824 |
| PA-824 , |
| (6s)-2-nitro-6-[[4-(trifluoromethoxy)phenyl]methoxy]-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine |
| {4-[((3s)-6-nitro(2h,3h,4h-imidazolo[2,1-b]1,3-oxazaperhydroin-3-yloxy))methyl]phenoxy}trifluoromethane |
| pa824 |
| (6s)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine |
| CHEMBL227875 , |
| pretomanid |
| bdbm50363237 |
| NCGC00346682-02 |
| NCGC00346682-01 |
| S1162 |
| pretomanid [who-dd] |
| (3s)-3-(4-trifluoromethoxybenzyloxy)-6-nitro-2h-3,4-dihydroimidazo(2,1-b)oxazine |
| pretomanid [orange book] |
| (s)-2-nitro-6-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5h-imidazo(2,1-b)(1,3)oxazine |
| pretomanid [usan] |
| pretomanid [inn] |
| pretomanid [mi] |
| DB05154 |
| HY-10844 |
| smr004702918 |
| MLS006011141 |
| SCHEMBL2983011 |
| (s)-2-nitro-6-((4-(trifluoromethoxy)benzyl)oxy)-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine |
| D10722 |
| pretomanid (tn) |
| pretomanid (usan/inn) |
| AC-25501 |
| AKOS024464713 |
| DTXSID8041163 |
| mfcd06809939 |
| gtpl11172 |
| EX-A1749 |
| mmv688755 |
| (6s)-2-nitro-6-{[4-(trifluoromethoxy)phenyl]methoxy}-5h,6h,7h-imidazo[2,1-b][1,3]oxazine |
| SW220281-1 |
| pa-824(pretomanid) |
| A855886 |
| DS-7321 |
| Q7118312 |
| CCG-268145 |
| ZLHZLMOSPGACSZ-NSHDSACASA-N , |
| SR-05000022748-1 |
| sr-05000022748 |
| pretomanid;(6s)-6,7-dihydro-2-nitro-6-[[4-(trifluoromethoxy)phenyl]methoxy]-5h-imidazo[2,1-b][1,3]oxazine |
| CS1245 |
| pretomanidum |
| P2718 |
| Z1650127771 |
| (6s)-2-nitro-6-[[4-(trifluoromethoxy)phenyl]methoxy]-6,7-dihydro- 5h-imidazo[2,1-b][1,3]oxazine |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Five such compounds were >100-fold better than the parent drug in a mouse model of acute Mycobacterium tuberculosis infection, and two orally bioavailable pyridine analogues (3-4-fold more soluble than the parent at low pH) were superior to antitubercular drug OPC-67683 in a chronic infection model." | ( Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). Blaser, A; Denny, WA; Franzblau, SG; Kmentova, I; Ma, Z; Palmer, BD; Sutherland, HS; Thompson, AM; Wan, B; Wang, Y, 2010) | 0.36 |
| " Bioisosteric replacement of this biaryl moiety by arylpiperazine resulted in a soluble, orally bioavailable carbamate analogue providing identical activity in the acute model, comparable efficacy to OPC-67683 in a chronic infection model, favorable pharmacokinetic profiles across several species, and enhanced safety." | ( Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). Blaser, A; Denny, WA; Franzblau, SG; Kmentova, I; Ma, Z; Palmer, BD; Sutherland, HS; Thompson, AM; Wan, B; Wang, Y, 2012) | 0.38 |
| " TBA-354 (SN31354[(S)-2-nitro-6-((6-(4-trifluoromethoxy)phenyl)pyridine-3-yl)methoxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine]) is a pyridine-containing biaryl compound with exceptional efficacy against chronic murine tuberculosis and favorable bioavailability in preliminary rodent studies." | ( In vitro and in vivo activities of the nitroimidazole TBA-354 against Mycobacterium tuberculosis. Cho, S; Franzblau, SG; Kim, Y; Lu, Y; Ma, Z; Mdluli, K; Upton, AM; Wang, B; Wang, Y; Xu, J; Yang, TJ, 2015) | 0.42 |
| " The most efficacious analogue also displayed outstanding in vivo activity in the stringent chronic model (up to 24-fold better than the drug delamanid and 4-fold greater than our previous best phenylpyridine candidate), with favorable pharmacokinetics, including good oral bioavailability in the rat." | ( Synthesis and structure-activity relationships for extended side chain analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). Blaser, A; Denny, WA; Franzblau, SG; Kmentova, I; Ma, Z; Palmer, BD; Sutherland, HS; Thompson, AM; Wan, B; Wang, Y, 2015) | 0.42 |
| " The observed pretomanid plasma concentration-time profiles for all tested doses were described by a one-compartment model with first-order absorption and elimination and a sigmoidal bioavailability dependent on dose, time, and the predose fed state." | ( Modeling and Simulation of Pretomanid Pharmacokinetics in Pulmonary Tuberculosis Patients. Lyons, MA, 2018) | 0.48 |
| " Pretomanid pharmacokinetic behavior was described by a one-compartment model that at a given dose was linear in its absorption and clearance processes but where the rate of absorption and extent of bioavailability changed with dose." | ( Population Pharmacokinetics of the Antituberculosis Agent Pretomanid. Everitt, D; Nedelman, JR; Salinger, DH; Subramoney, V, 2019) | 0.51 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| " This work aimed to assess the pharmacokinetics (PK) and relative bioavailability of the DTF compared to the marketed formulation (MF) and the potential influence of dose." | ( Characterizing Absorption Properties of Dispersible Pretomanid Tablets Using Population Pharmacokinetic Modelling. Karlsson, MO; Lombardi, A; Nedelman, J; Pappas, F; Svensson, EM; Zou, Y, 2022) | 0.72 |
| " No significant difference in bioavailability was found between formulations." | ( Characterizing Absorption Properties of Dispersible Pretomanid Tablets Using Population Pharmacokinetic Modelling. Karlsson, MO; Lombardi, A; Nedelman, J; Pappas, F; Svensson, EM; Zou, Y, 2022) | 0.72 |
| "Using data from a relative bioavailability study in healthy adult volunteers, a mathematical model has been developed to inform dose selection for the investigation of pretomanid in children using the new dispersible tablet formulation." | ( Characterizing Absorption Properties of Dispersible Pretomanid Tablets Using Population Pharmacokinetic Modelling. Karlsson, MO; Lombardi, A; Nedelman, J; Pappas, F; Svensson, EM; Zou, Y, 2022) | 0.72 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 9.5221 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 6.1804 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| G | Vesicular stomatitis virus | Potency | 26.8370 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 23.9185 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 26.8370 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 26.8370 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 26.8370 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 26.8370 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 30.0000 | 0.0009 | 1.9014 | 10.0000 | AID643119 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID396475 | Ratio of Kcat to Km for Mycobacterium tuberculosis Rv3547 expressed in Escherichia coli co-transfected with maltose-binding fusion protein | 2008 | Science (New York, N.Y.), Nov-28, Volume: 322, Issue:5906 | PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. |
| AID556438 | Half life in guinea pig at 40 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID585242 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID585472 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID369305 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN2351 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID556459 | Ratio of Cmax in guinea pig at 40 mg/kg, po to MIC for Mycobacterium tuberculosis | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1368534 | Half life in CD1 mouse brain at 78 mg/kg, po after 0.25 to 24 hrs by LC-MS/MS method | 2018 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2 | Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides. |
| AID515919 | Antibacterial activity against streptomycin-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20 | Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring. |
| AID1654573 | Lipophilicity, log P of the compound | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Metabolic and Pharmaceutical Aspects of Fluorinated Compounds. |
| AID445894 | Metabolic stability in mouse liver microsomes after 1 hr at 37 degC | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. |
| AID370445 | Ratio of Kcat/Km for Mycobacterium tuberculosis F420-dependent nitroreductase by Michaelis-Menten equation | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Structure-activity relationships of antitubercular nitroimidazoles. 2. Determinants of aerobic activity and quantitative structure-activity relationships. |
| AID585471 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1224565 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | 1-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria. |
| AID556463 | Metabolic stability of the compound assessed as compound remaining in lung of guinea pig at 20 mg/kg, iv after 32 hrs | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1468877 | Cytotoxicity against human MRC5 cells after 72 hrs by resazurin dye based assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis. |
| AID683685 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives. |
| AID556447 | Mean residence time in guinea pig at 60 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1468873 | Antileishmanial activity against Leishmania donovani amastigotes expressing Luc gene infected in mouse J774A.1 cells by luciferase reporter gene assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis. |
| AID556416 | Elimination rate constant in guinea pig at 20 mg/kg, iv by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1191882 | Antimicrobial activity against isoniazid and rifampin resistant Mycobacterium tuberculosis assessed as reduction in colony forming unit after 21 days at 37 degC in presence of 1-(4-(4-(1H-pyrrol-1-yl)phenyl)piperazin-1-yl)-4-(5-(3,5-difluorobenzyl)-1-(2-f | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | A novel molecule with notable activity against multi-drug resistant tuberculosis. |
| AID585244 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID698984 | Antimycobacterial activity against Mycobacterium tuberculosis infected in human assessed as log reduction of bacterial count at 200 to 1200 mg | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID556437 | Elimination rate constant in guinea pig at 40 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1577421 | Antitubercular activity against Mycobacterium tuberculosis H37Rv | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase. |
| AID556418 | Mean residence time in guinea pig at 20 mg/kg, iv by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID698988 | Tmax in human at 50 to 1500 mg, po | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID1179474 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in glycerol-alanine-salts medium after 7 days by Microplate Alamar Blue assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates. |
| AID1851933 | Metabolic stability in human microsomes assessed as compound remaining measured after 2 hrs | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID585461 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1659810 | Antimycobacterial activity against Mycobacterium tuberculosis drug resistant clinical isolates | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Molecule Property Analyses of Active Compounds for |
| AID683687 | Kinetic solubility of the compound at pH 7.4 | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives. |
| AID1585787 | Metabolic stability in human liver microsomes assessed as parent compound remaining at 3 uM after 2 hrs by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID1416246 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 7 days by microplate alamar blue assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant |
| AID370073 | Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35820 after 14 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID1851961 | Volume of distribution at steady state in CD-1 mouse at 10 mg/kg, iv measured upto 48 hrs by LC/MS/MS analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID585229 | Tmax in BALB/c mouse up to 1456 mg/kg, po administered as single dose | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID369308 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN3979 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID683686 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 10 days by low oxygen recovery assay | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives. |
| AID446154 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 16 to 24 hrs by microplate alamar | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development. |
| AID585464 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID585241 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID515917 | Antibacterial activity against rifampicin-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20 | Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring. |
| AID1585767 | Antiparasitic activity against Entamoeba histolytica HM-1:IMSS trophozoites after 24 to 48 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID369334 | Antimicrobial activity against log phase recombinant Mycobacterium tuberculosis H37Rv-lux with plasmid MV361 at 10 ug/ml incubated for 7 days assessed as bacterial count | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID620625 | Metabolic stability in CD1 mouse liver microsomes at 1 uM measured as compound remaining after 1 hr by LC/MS/MS analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID760163 | Antimycobacterial activity against isoniazid, rifampin, ethambutol, streptomycin, kanamycin and ofloxacin-resistant Mycobacterium tuberculosis after 14 days | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Advancement of Imidazo[1,2- |
| AID369311 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis TN576 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID1743942 | Antitubercular activity against Mycobacterium tuberculosis resistant mutants generated by plating on 7H11/0ADC agar plates in presence of 3.75 to 15 uM 2-((3,5-Dinitrobenzyl)thio)quinazolin-4(3H)-one followed by sensitivity testing | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 | 2-((3,5-Dinitrobenzyl)thio)quinazolinones: Potent Antimycobacterial Agents Activated by Deazaflavin (F |
| AID346840 | Antimycobacterial activity against wild type Mycobacterium tuberculosis H37Rv NRP-2 stage after 3 weeks under anaerobic condition | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Structure-activity relationships of antitubercular nitroimidazoles. 1. Structural features associated with aerobic and anaerobic activities of 4- and 5-nitroimidazoles. |
| AID369298 | Antimycobacterial activity against mono-rifampin-resistant Mycobacterium tuberculosis TN675 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID643092 | Antimicrobial activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as reduction in lung CFU at 100 mg/kg, po administered 11 days after post infection qd for 5 days per week for 3 weeks | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1851957 | AUC (0 to last) in CD-1 mouse at 25 mg/kg, po measured upto 48 hrs by LC/MS/MS analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID556431 | Mean residence time in guinea pig at 20 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID643095 | Antimicrobial activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as fold reduction in lung CFU at 100 mg/kg, po administered 70 days after post infection qd for 5 days per week for 3 weeks relative to OPC-67683 | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID572883 | Antibacterial activity against Mycobacterium tuberculosis H37Rv under anaerobic conditions by luciferase based low oxygen recovery assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Efficacy of quinoxaline-2-carboxylate 1,4-di-N-oxide derivatives in experimental tuberculosis. |
| AID1242700 | Anti-tubercular activity against Mycobacterium tuberculosis | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Synthesis and anti-tubercular activity of 2-nitroimidazooxazines with modification at the C-7 position as PA-824 analogs. |
| AID369312 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis TN702 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID446153 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv expressing pFCA-luxAB after 10 days by low-oxygen recovery assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development. |
| AID585254 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID643151 | Induction of mutagenesis in Salmonella Typhimurium TA98 in presence of rat liver S9 fraction by Ames test | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1585766 | Antiparasitic activity against Giardia lamblia WB trophozoites after 24 to 48 hrs by CellTiter-Glo luminescent cell viability assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID585257 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID445893 | Metabolic stability in human liver microsomes after 1 hr at 37 degC | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. |
| AID556423 | Half life in guinea pig at 40 mg/kg, po by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID541702 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by LORA method | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID765272 | Cmax/MIC in Mycobacterium tuberculosis infected mouse | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis. |
| AID585460 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1500582 | Bactericidal activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as minimum concentration required to achieve a 2-log kill measured after 21 days under hypoxic conditions | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines. |
| AID1243372 | Metabolic stability in CD1 mouse liver microsomes assessed as compound remaining after 1 hr | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy. |
| AID645533 | Cytotoxicity against african green monkey Vero cells after 72 hrs | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity. |
| AID774296 | Antimycobacterial activity against streptomycin-resistant Mycobacterium tuberculosis ATCC 35820 | 2013 | Journal of natural products, Oct-25, Volume: 76, Issue:10 | Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. |
| AID370072 | Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35837 after 14 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID564968 | Upregulation of p27 gene expression in Mycobacterium tuberculosis by microarray | 2009 | Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9 | Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth. |
| AID1179475 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in 7H12 medium after 7 days by Microplate Alamar Blue assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates. |
| AID1191878 | Antimicrobial activity against isoniazid and rifampin resistant Mycobacterium tuberculosis after 21 days at 37 degC in presence of 1-(4-(4-(1H-pyrrol-1-yl)phenyl)piperazin-1-yl)-4-(5-(3,5-difluorobenzyl)-1-(2-fluorobenzyl)-2-oxo-1,2-dihydropyridin-3-yl)-2 | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | A novel molecule with notable activity against multi-drug resistant tuberculosis. |
| AID1269341 | Clearance in CD-1 mouse at 10 mg/kg, iv after 0.02 to 48 hrs by LC-MS/MS method | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID1269348 | Antimicrobial activity against Bacillus subtilis | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID549617 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv Ddn mutant after 2 weeks | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | The effect of 5-substitution on the electrochemical behavior and antitubercular activity of PA-824. |
| AID572876 | Antibacterial activity against wild-type Mycobacterium bovis BCG by microplate Alamar Blue assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Efficacy of quinoxaline-2-carboxylate 1,4-di-N-oxide derivatives in experimental tuberculosis. |
| AID1654617 | Apparent passive permeability of the compound across apical to basolateral side in MDCK low efflux cells assessed as ratio of drug level | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Metabolic and Pharmaceutical Aspects of Fluorinated Compounds. |
| AID564971 | Downregulation of p55 gene expression Mycobacterium tuberculosis by microarray | 2009 | Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9 | Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth. |
| AID556452 | Chemical stability of the compound at 4 degC | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID620624 | Metabolic stability in human liver microsomes at 1 uM measured as compound remaining after 45 mins by LC/MS/MS analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1269329 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 7 days by microbroth dilution method | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID1679146 | Cytotoxicity against African green monkey Vero cells assessed by reduction in cell viability incubated for 72 hrs by resazurin dye fluorescence based assay | 2021 | RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1 | Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds. |
| AID760161 | Antimycobacterial activity against isoniazid, rifampin, ethambutol, kanamycin and ofloxacin-resistant Mycobacterium tuberculosis after 14 days | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Advancement of Imidazo[1,2- |
| AID556422 | Elimination rate constant in guinea pig at 40 mg/kg, po by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID556433 | Tmax in guinea pig at 20 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID369320 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis TN2557 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID1851920 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as bacterial growth inhibition incubated for 5 days under normoxic condition by resazurin microtiter assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID515921 | Antibacterial activity against clofazimine-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20 | Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring. |
| AID1243373 | Cytotoxicity against African green monkey Vero cells after 72 hrs | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy. |
| AID1269353 | Antimicrobial activity against Acinetobacter baumannii | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID572879 | Antibacterial activity against Mycobacterium bovis BCG harboring fbiC gene by microplate Alamar Blue assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Efficacy of quinoxaline-2-carboxylate 1,4-di-N-oxide derivatives in experimental tuberculosis. |
| AID1483197 | Antitubercular activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as reduction in bacterial burden at 100 mg/kg, po qd administered every 5 days a week for 3 weeks | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | 7-Substituted 2-Nitro-5,6-dihydroimidazo[2,1-b][1,3]oxazines: Novel Antitubercular Agents Lead to a New Preclinical Candidate for Visceral Leishmaniasis. |
| AID585227 | Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in po dosed BALB/c mouse assessed as reduction in log10 CFU count by single dose study | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID369309 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN4259 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID585478 | Cmax in mouse at 100 or 50 mg/kg, po administered as single dose | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID572882 | Antibacterial activity against Mycobacterium tuberculosis H37Rv under aerobic conditions | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Efficacy of quinoxaline-2-carboxylate 1,4-di-N-oxide derivatives in experimental tuberculosis. |
| AID774293 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS-PMS assay | 2013 | Journal of natural products, Oct-25, Volume: 76, Issue:10 | Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. |
| AID556450 | Bioavailability (0 to infinity) in guinea pig at 60 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1194570 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv expressing Lux assessed as reduction in growth measured after 3 weeks by bioluminescence assay | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9 | Design and synthesis of novel anti-tuberculosis agents from the celecoxib pharmacophore. |
| AID556417 | Half life in guinea pig at 20 mg/kg, iv by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID556446 | Half life in guinea pig at 60 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1585788 | Metabolic stability in CD-1 mouse liver microsomes assessed as parent compound remaining at 3 uM after 2 hrs by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID585473 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1243371 | Metabolic stability in human liver microsomes assessed as compound remaining after 1 hr | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy. |
| AID572878 | Antibacterial activity against Mycobacterium bovis BCG harboring moaA gene by microplate Alamar Blue assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Efficacy of quinoxaline-2-carboxylate 1,4-di-N-oxide derivatives in experimental tuberculosis. |
| AID315121 | Antitubercular activity against Mycobacterium tuberculosis H37Rv T2 nitroreductase mutant | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824. |
| AID370069 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 14 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID1585789 | Metabolic stability in human plasma assessed as parent compound remaining at 3 uM after 2 hrs by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID581005 | Drug excretion in feces of healthy human | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development. |
| AID689235 | Antimycobacterial activity against isoniazid-,rifampin-,ethambutol-,pyrazinamide-,streptomycin-,kanamycin-,paraaminosalicylic acid-resistant Mycobacterium tuberculosis after 14 days | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds. |
| AID774292 | Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC90 for Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate Alamar blue assay | 2013 | Journal of natural products, Oct-25, Volume: 76, Issue:10 | Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. |
| AID1269335 | Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID548281 | Antimicrobial activity against Trypanosoma brucei NfxR1 | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis. |
| AID585480 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse assessed as bacteriostatic effect at 12.5 mg/kg, po administered as single dose | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1851928 | Substrate activity at Mycobacterium tuberculosis Ddn expressed in Escherichia coli BL21 (DE3) assessed as oxidation of F420H2 by measuring Kcat/Km by spectrophotometric analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID445272 | Antitubercular activity against Mycobacterium tuberculosis H37Rv in anaerobic condition after 7 days by low oxygen recovery assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID689237 | Antimycobacterial activity against isoniazid-,rifampin-,ethambutol-,rifabutin-resistant Mycobacterium tuberculosis after 14 days | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds. |
| AID585247 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID370250 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 1.25 mg/kg, po administered once daily measured after 28 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID369310 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis TN565 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID581002 | Antimicrobial activity against compound-susceptible Mycobacterium tuberculosis | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development. |
| AID556415 | AUC (0 to infinity) in guinea pig at 20 mg/kg, iv by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1468874 | Antileishmanial activity against Leishmania infantum amastigotes infected in mouse primary peritoneal macrophages after 5 days by Giemsa staining based microscopic method | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis. |
| AID572881 | Antibacterial activity against Mycobacterium bovis BCG harboring pil8 gene by microplate Alamar Blue assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Efficacy of quinoxaline-2-carboxylate 1,4-di-N-oxide derivatives in experimental tuberculosis. |
| AID369314 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis TN768 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID548283 | Selectivity ratio of EC50 for Trypanosoma brucei NfxR1 to EC50 for Trypanosoma brucei | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis. |
| AID370254 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 20 mg/kg, po administered once daily measured after 28 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID585455 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID698987 | AUC in human at 50 to 1500 mg, po | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID585238 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID556443 | Bioavailability in guinea pig at 40 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID556464 | Metabolic stability of the compound assessed as compound remaining in lung of guinea pig at 40 mg/kg, po after 32 hrs | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID396476 | Binding affinity to Mycobacterium tuberculosis Rv3547 expressed in Escherichia coli co-transfected with maltose-binding fusion protein assessed as reoxidation of deazaflavin cofactor F420 by UV spectrophotometry | 2008 | Science (New York, N.Y.), Nov-28, Volume: 322, Issue:5906 | PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. |
| AID585479 | AUC (0 to t) in mouse at 100 or 50 mg/kg, po administered as single dose | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1179477 | Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by CellTiter 96 assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates. |
| AID369303 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN1051 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID346842 | Antimycobacterial activity against Mycobacterium tuberculosis with deazaflavin-dependent nitroreductase mutant | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Structure-activity relationships of antitubercular nitroimidazoles. 1. Structural features associated with aerobic and anaerobic activities of 4- and 5-nitroimidazoles. |
| AID556461 | Ratio of Cmax in mouse at 100 mg/kg, po to MIC for Mycobacterium tuberculosis | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID548280 | Antimicrobial activity against Trypanosoma brucei | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis. |
| AID370252 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 5 mg/kg, po administered once daily measured after 28 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID541941 | Metabolic stability in human liver microsomes assessed as compound remaining after 1 hr | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1654619 | Protein binding in human plasma | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Metabolic and Pharmaceutical Aspects of Fluorinated Compounds. |
| AID585239 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID556414 | Chemical stability of the compound after 12 months | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID585468 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID369304 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN1082 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID585250 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID445896 | Antitubercular effect in Mycobacterium tuberculosis infected BALB/c mouse assessed as CFU reduction at 100 mg/kg, po administered 5 days a week for 3 weeks | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. |
| AID396482 | Induction of nitrous acid production in NRP2 phase Mycobacterium bovis BCG assessed as ratio of Vmax to Km under hypoxic non replicating condition | 2008 | Science (New York, N.Y.), Nov-28, Volume: 322, Issue:5906 | PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. |
| AID1063301 | Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 16 to 24 hrs by microplate-Alamar Blue assay | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents. |
| AID461171 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate Alamar blue assay | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3 | Synthesis, antimalarial and antitubercular activity of acetylenic chalcones. |
| AID643079 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring pFCA-lux AB gene measured under anaerobic condition after 11 days by luminescence analysis | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1063299 | Antitubercular activity against capreomycin-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 16 to 24 hrs by microplate-Alamar Blue assay | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents. |
| AID585259 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID556430 | Half life in guinea pig at 20 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID346844 | Ratio of Kcat/Km for Mycobacterium tuberculosis F420-dependent nitroreductase by Michaelis-Menten equation | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Structure-activity relationships of antitubercular nitroimidazoles. 1. Structural features associated with aerobic and anaerobic activities of 4- and 5-nitroimidazoles. |
| AID585231 | Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as reduction in CFU count by agar proportion method | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID643093 | Antimicrobial activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as fold reduction in lung CFU at 100 mg/kg, po administered 11 days after post infection qd for 5 days per week for 3 weeks relative to PA-824 | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID549615 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv assessed as minimum anaerobicidal cancentration after 3 weeks | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | The effect of 5-substitution on the electrochemical behavior and antitubercular activity of PA-824. |
| AID541699 | Solubility of the compound in water at pH 7.0 by HPLC | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID585458 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID369299 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN913 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID585251 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1269347 | Antimicrobial activity against Bacillus anthracis | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID620622 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv under anaerobic conditions by fluorescence based low-oxygen-recovery assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1063305 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 16 to 24 hrs by microplate-Alamar Blue assay | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents. |
| AID556424 | Mean residence time in guinea pig at 40 mg/kg, po by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| 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. |
| AID556426 | Tmax in guinea pig at 40 mg/kg, po by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID643082 | Antimicrobial activity against Mycobacterium bovis | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID564969 | Upregulation of p55 gene expression Mycobacterium tuberculosis by microarray | 2009 | Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9 | Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth. |
| AID369331 | Inhibition of lipid synthesis in log phase Mycobacterium bovis BCG assessed as [14C] acetate incorporation after 3 hrs by chromatography | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID590141 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by LORA assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7 | Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents. |
| AID614924 | Ratio of Kcat to Km for Mycobacterium tuberculosis deazaflavin-dependent nitroreductase | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16 | Structure-activity relationships of antitubercular nitroimidazoles. 3. Exploration of the linker and lipophilic tail of ((s)-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)-(4-trifluoromethoxybenzyl)amine (6-amino PA-824). |
| AID1585795 | Apparent permeability across basolateral to apical side in human Caco2 cells assessed as mean drug recovery at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID556455 | Half life in po dosed dog | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID585477 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in single po dosed BALB/c mouse assessed as reduction in lung CFU count | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID643115 | Octanol-water partition coefficient, log P of the compound by shake-flask method | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1269351 | Antimicrobial activity against Streptococcus pyogenes | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID610801 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 4 days by MABA assay | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Synthesis and antimycobacterial activities of non-purine analogs of 6-aryl-9-benzylpurines: Imidazopyridines, pyrrolopyridines, benzimidazoles, and indoles. |
| AID556428 | AUC (0 to infinity) in guinea pig at 20 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID446152 | Cytotoxicity against african green monkey Vero cells after 72 hrs | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development. |
| AID369301 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN1008 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID577831 | Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis H37Rv under anaerobic condition after 7 days by GFP reporter gene assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5 | Synthesis and antitubercular activity of monocyclic nitroimidazoles: insights from econazole. |
| AID369302 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN1040 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID698989 | Antimycobacterial activity against Mycobacterium tuberculosis infected in mouse administered as qd | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID369328 | Acute toxicity in Mycobacterium tuberculosis H37Rv infected BALB/c mouse at >1000 mg/kg, po single dose | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID643117 | Thermodynamic solubility of the compound at pH 7.4 | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID515920 | Antibacterial activity against kanamycin-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20 | Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring. |
| AID556453 | Chemical stability of the compound at 25 degC | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID614923 | Antitubercular activity against Mycobacterium tuberculosis | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16 | Structure-activity relationships of antitubercular nitroimidazoles. 3. Exploration of the linker and lipophilic tail of ((s)-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)-(4-trifluoromethoxybenzyl)amine (6-amino PA-824). |
| AID765270 | AUC/MIC in Mycobacterium tuberculosis infected mouse | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis. |
| AID315122 | Aqueous solubility of the compound | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824. |
| AID1269332 | Half life in mouse liver microsomes | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID590140 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7 | Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents. |
| AID585467 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID689238 | Antimycobacterial activity against isoniazid-,rifampin-,ethambutol-,streptomycin-,kanamycin-,ofloxacin-resistant Mycobacterium tuberculosis after 14 days | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds. |
| AID369333 | Antimicrobial activity against log phase recombinant Mycobacterium tuberculosis H37Rv-lux with plasmid MV361 at 10 ug/ml incubated for 7 days assessed as bacterial count after 4 days | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID285160 | Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed as bacterial density after 7 days | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis. |
| AID1269333 | Apparent permeability from apical to basolateral side in human Caco2 cells | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID369327 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in Hartley guinea pig assessed as reduction in mycobacterial burden in spleen at 40 mg/kg, po daily after 30 days of infection for 30 days relative to isoniazid | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID620620 | Aqueous solubility of the compound in water at pH 7 by HPLC analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID585249 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1851938 | Stability in mouse plasma assessed as compound remaining measured after 2 hrs | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID1269354 | Antimicrobial activity against Escherichia coli | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID643119 | Inhibition of human Erg expressed in HEK293 cells by FAST patch clamp analysis | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID765273 | fCmax/MIC in Mycobacterium tuberculosis infected mouse | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis. |
| AID585246 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID585255 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID445271 | Antitubercular activity against Mycobacterium tuberculosis H37Rv in aerobic condition after 7 days by microplate alamar blue assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID541943 | Thermodynamic solubility in aqueous buffer at pH 1 at 20 degC by HPLC | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1851960 | Oral bioavailability in CD-1 mouse at 25 mg/kg measured upto 48 hrs by LC/MS/MS analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID689236 | Antimycobacterial activity against isoniazid-,rifampin-,ethambutol-,kanamycin-,paraaminosalicylic acid-resistant Mycobacterium tuberculosis after 14 days | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds. |
| AID643080 | Kinetic solubility of the compound in water at pH 7 by HPLC analysis | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID585465 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1585769 | Antibacterial activity against Mycobacterium tuberculosis H37Rv after 5 days under normoxic condition by resazurin dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID626867 | Antimicrobial activity against replicating Mycobacterium tuberculosis after 8 days by micro plate alamar blue assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin. |
| AID556435 | Bioavailability in guinea pig at 20 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID548282 | Antimicrobial activity against Trypanosoma brucei NfxR2 | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis. |
| AID585235 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID585248 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1468870 | Kinetic solubility in pH 7 water by HPLC analysis | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis. |
| AID644238 | Antitubercular activity against Mycobacterium tuberculosis H37Rv after 16 to 24 hrs by microplate alamar blue assay | 2012 | European journal of medicinal chemistry, Mar, Volume: 49 | Synthesis and evaluation of anti-tubercular and antibacterial activities of new 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives. Part 2. |
| AID556458 | Antimicrobial activity against Mycobacterium tuberculosis | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID585234 | Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse assessed as reduction in log10 CFU count at 96 mg/kg, po bid | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID370253 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 10 mg/kg, po administered once daily measured after 28 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID585462 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1269339 | AUC(infinity) in CD-1 mouse at 10 mg/kg, iv after 0.02 to 48 hrs by LC-MS/MS method | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID556451 | Bioavailability in guinea pig at 60 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID369325 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv with plasmid MH102 infected in BALB/c mouse assessed as reduction in mycobacterial burden in lung at 100 mg/kg, po daily after 4 days of infection for 7 to 60 days relative to isoniazid | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID541935 | Antitubercular activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as reduction in lung microbial load at 100 mg/kg, po qd for 5 days per week for 3 weeks administered 70 days post infection relative to untreated control | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1191876 | Antimicrobial activity against isoniazid and rifampin resistant Mycobacterium tuberculosis after 21 days at 37 degC by agar dilution drug susceptibility assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | A novel molecule with notable activity against multi-drug resistant tuberculosis. |
| AID396477 | Binding affinity to Mycobacterium tuberculosis Rv3547 assessed as nitrous acid production by Griess method in presence of cofactor F420H2 | 2008 | Science (New York, N.Y.), Nov-28, Volume: 322, Issue:5906 | PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. |
| AID369306 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN2524 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID549616 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv F420 mutant after 2 weeks | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | The effect of 5-substitution on the electrochemical behavior and antitubercular activity of PA-824. |
| AID585466 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1269352 | Antimicrobial activity against Streptococcus pneumoniae | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID585256 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID564973 | Antimicrobial activity against Mycobacterium bovis BCG by resazurine microtiter assay | 2009 | Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9 | Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth. |
| AID760170 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv expressing pCHERRY3 after 4 days by plate format assay | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Advancement of Imidazo[1,2- |
| AID645529 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in GAST medium after 1 week by microplate alamar blue assay | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity. |
| AID581001 | Antimicrobial activity against multiple drug-resistant Mycobacterium tuberculosis | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development. |
| AID369313 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis TN715 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID1290501 | Antitubercular activity against Mycobacterium tuberculosis in acute tuberculosis infection BALB/c mouse model assessed as reduction in parasite burden at 100 mg/kg, po administered 5 days per week for 3 weeks started on day 11 post infection | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Repositioning Antitubercular 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]oxazoles for Neglected Tropical Diseases: Structure-Activity Studies on a Preclinical Candidate for Visceral Leishmaniasis. |
| AID774297 | Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis ATCC 35822 | 2013 | Journal of natural products, Oct-25, Volume: 76, Issue:10 | Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. |
| AID369322 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv with plasmid MH102 infected in BALB/c mouse assessed as reduction in mycobacterial burden in spleen at 25 mg/kg, po daily after 4 days of infection for 10 days relative to isoniazid | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID396479 | Induction of nitrous acid production in NRP2 phase Mycobacterium bovis BCG at 1.85 uM to 100 uM after 2 days under hypoxic non replicating condition in presence of DAF-FM diacetate | 2008 | Science (New York, N.Y.), Nov-28, Volume: 322, Issue:5906 | PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. |
| AID1851934 | Metabolic stability in mouse microsomes assessed as compound remaining measured after 2 hrs | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID556456 | Tmax in po dosed monkey | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID774298 | Antimycobacterial activity against rifampin-resistant Mycobacterium tuberculosis ATCC 35838 | 2013 | Journal of natural products, Oct-25, Volume: 76, Issue:10 | Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. |
| AID556441 | Tmax in guinea pig at 40 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1269340 | Half life in CD-1 mouse at 10 mg/kg, iv after 0.02 to 48 hrs by LC-MS/MS method | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID556439 | Mean residence time in guinea pig at 40 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID315118 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by oxygen depletion assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824. |
| AID698995 | Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID577832 | Antifungal activity against Candida albicans ATCC 90027 after 48 hrs by broth microdilution method | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5 | Synthesis and antitubercular activity of monocyclic nitroimidazoles: insights from econazole. |
| AID1851963 | Half life in CD-1 mouse at 10 mg/kg, iv measured upto 48 hrs by LC/MS/MS analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID564970 | Downregulation of p27 gene expression Mycobacterium tuberculosis by microarray | 2009 | Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9 | Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth. |
| AID369329 | Chronic toxicity in Mycobacterium tuberculosis H37Rv infected BALB/c mouse at >500 mg/kg, po for 28 days | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID689234 | Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis isolate 2 after 14 days | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds. |
| AID1851932 | Plasma protein binding in mouse | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID369300 | Antimycobacterial activity against mono-rifampin-resistant Mycobacterium tuberculosis TN994 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID396478 | Induction of nitrous acid production in NRP2 phase Mycobacterium bovis BCG under aerobic condition in presence of DAF-FM diacetate | 2008 | Science (New York, N.Y.), Nov-28, Volume: 322, Issue:5906 | PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. |
| AID1679147 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in 7H12 media assessed as reduction in bacterial growth incubated for 7 days by resazurin dye fluorescence based assay | 2021 | RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1 | Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds. |
| AID369317 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis TN1314 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID1851959 | Half life in CD-1 mouse at 25 mg/kg, po measured upto 48 hrs by LC/MS/MS analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID610802 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv transfected with pFPCA-luxAB grown under anaerobic condition for 10 days followed by 24 hrs incubation under aerobic condition by LORA assay | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11 | Synthesis and antimycobacterial activities of non-purine analogs of 6-aryl-9-benzylpurines: Imidazopyridines, pyrrolopyridines, benzimidazoles, and indoles. |
| AID1585774 | Antiparasitic activity against bloodstream form of Trypanosoma brucei brucei strain 427 after 48 hrs by resazurin dye-based assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID1179476 | Antitubercular activity against Mycobacterium tuberculosis H37Rv transfected with pFCA-luxAB in 7H12 medium after 10 days by low-oxygen recovery assay | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15 | Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates. |
| AID689233 | Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis isolate 1 after 14 days | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds. |
| AID556421 | AUC (0 to infinity) in guinea pig at 40 mg/kg, po by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID572877 | Antibacterial activity against Mycobacterium bovis BCG harboring fgd gene by microplate Alamar Blue assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Efficacy of quinoxaline-2-carboxylate 1,4-di-N-oxide derivatives in experimental tuberculosis. |
| AID1468886 | Metabolic stability in CD-1 mouse liver microsomes assessed as parent compound remaining at 1 uM after 1 hr | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis. |
| AID585233 | Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse assessed as reduction in log10 CFU count at 96 mg/kg, po for 5 days relative to control | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID760167 | Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis clinical isolate 1 after 14 days | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Advancement of Imidazo[1,2- |
| AID556436 | AUC (0 to infinity) in guinea pig at 40 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1851922 | Antimycobacterial activity against Mycobacterium avium ATCC 25291 assessed as bacterial growth inhibition incubated for 6 days under normoxic condition by resazurin microtiter assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID370074 | Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35812 after 14 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID396481 | Mycobactericidal activity against Mycobacterium tuberculosis H37Rv assessed as minimum anaerobicidal concentration required for 1 log reduction in bacterial numbers after 1 week under hypoxic non replicating condition | 2008 | Science (New York, N.Y.), Nov-28, Volume: 322, Issue:5906 | PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. |
| AID1191880 | Antimicrobial activity against isoniazid and rifampin resistant Mycobacterium tuberculosis assessed as ratio of MIC combination/MIC compound alone after 21 days at 37 degC in presence of 1-(4-(4-(1H-pyrrol-1-yl)phenyl)piperazin-1-yl)-4-(5-(3,5-difluoroben | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | A novel molecule with notable activity against multi-drug resistant tuberculosis. |
| AID445890 | Cytotoxicity against african green monkey Vero cells after 72 hrs by tetrazolium dye assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. |
| AID1851958 | Tmax in CD-1 mouse at 25 mg/kg, po measured upto 48 hrs by LC/MS/MS analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID643118 | Plasma protein binding in human at 10 uM | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1585796 | Efflux ratio of apparent permeability in human Caco2 cells at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID1063300 | Antitubercular activity against moxifloxacin-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 16 to 24 hrs by microplate-Alamar Blue assay | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents. |
| AID643153 | Induction of mutagenesis in Salmonella Typhimurium TA100 in presence of rat liver S9 fraction by Ames test | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID445889 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv expressing pFCA-luxAB after 10 days by luminescence-based low-oxygen recovery assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. |
| AID689239 | Antimycobacterial activity against isoniazid-,rifampin-,ethambutol-,kanamycin-,ofloxacin-resistant Mycobacterium tuberculosis after 14 days | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds. |
| AID396480 | Bactericidal activity against Mycobacterium tuberculosis H37Rv under aerobic condition by broth dilution method | 2008 | Science (New York, N.Y.), Nov-28, Volume: 322, Issue:5906 | PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. |
| AID765269 | fT>MIC in Mycobacterium tuberculosis infected mouse | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis. |
| AID1851921 | Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as bacterial growth inhibition incubated for 6 days under normoxic condition by resazurin microtiter assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID346841 | Antimycobacterial activity against Mycobacterium tuberculosis with cofactor F420 mutant | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Structure-activity relationships of antitubercular nitroimidazoles. 1. Structural features associated with aerobic and anaerobic activities of 4- and 5-nitroimidazoles. |
| AID548284 | Selectivity ratio of EC50 for Trypanosoma brucei NfxR2 to EC50 for Trypanosoma brucei | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis. |
| AID643152 | Induction of mutagenesis in Salmonella Typhimurium TA100 in absence of rat liver S9 fraction by Ames test | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1851962 | Clearance in CD-1 mouse at 10 mg/kg, iv measured upto 48 hrs by LC/MS/MS analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID556425 | Cmax in guinea pig at 40 mg/kg, po by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID285161 | Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as relative light unit after 11 days by LORA assay | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis. |
| AID585476 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1468884 | Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM after 1 hr | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis. |
| AID556460 | Ratio of Cmax in guinea pig at 40 mg/kg, administered via intratracheal insufflation to MIC for Mycobacterium tuberculosis | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1243370 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 11 days by LORA assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy. |
| AID585253 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID515918 | Antibacterial activity against isoniazid-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20 | Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring. |
| AID765271 | fAUC/MIC in Mycobacterium tuberculosis infected mouse | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis. |
| AID1585794 | Apparent permeability across apical to basolateral side in human Caco2 cells assessed as mean drug recovery at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID620623 | Metabolic stability in human liver microsomes at 1 uM measured as compound remaining after 1 hr by LC/MS/MS analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID698985 | Half life in human at 50 to 1500 mg, po | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID445276 | Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse assessed as ratio of lung CFU for compound to lung CFU for PA-824 at 100 mg/kg, po daily for 5 days a week for 3 weeks | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID585463 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID556449 | Tmax in guinea pig at 60 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID774294 | Antimycobacterial activity against cycloserine-resistant Mycobacterium tuberculosis ATCC 35826 | 2013 | Journal of natural products, Oct-25, Volume: 76, Issue:10 | Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. |
| AID370070 | Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35838 after 14 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID541937 | Antitubercular activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as reduction in lung microbial load at 100 mg/kg, po qd for 5 days per week for 3 weeks administered 70 days post infection relative to OPC-67683 | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID396483 | Induction of nitrous acid production in NRP2 phase Mycobacterium bovis BCG at 20 uM by fluorescence quenching measurement in presence of C-PTIO | 2008 | Science (New York, N.Y.), Nov-28, Volume: 322, Issue:5906 | PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. |
| AID620621 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv under aerobic conditions by microplate alamar blue assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID346839 | Antimycobacterial activity against wild type Mycobacterium tuberculosis H37Rv ATCC 27294 after 2 weeks | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Structure-activity relationships of antitubercular nitroimidazoles. 1. Structural features associated with aerobic and anaerobic activities of 4- and 5-nitroimidazoles. |
| AID577830 | Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis H37Rv after 7 days by alamar blue assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5 | Synthesis and antitubercular activity of monocyclic nitroimidazoles: insights from econazole. |
| AID1242702 | Anti-tubercular activity against Mycobacterium tuberculosis H37Rv incubated at 37 degC by microscopy | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Synthesis and anti-tubercular activity of 2-nitroimidazooxazines with modification at the C-7 position as PA-824 analogs. |
| AID581006 | Drug excretion in urine of healthy human | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development. |
| AID585243 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID541944 | Thermodynamic solubility in aqueous buffer at pH 7.4 at 20 degC by HPLC | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID585230 | Elimination half life in BALB/c mouse up to 1456 mg/kg, po administered as single dose | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID645531 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in 7H12 medium after 1 week by microplate alamar blue assay | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity. |
| AID369307 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN3183 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID1679148 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in GAS media assessed as reduction in bacterial growth incubated for 7 days by resazurin dye fluorescence based assay | 2021 | RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1 | Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds. |
| AID369318 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis TN1618 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| 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. |
| AID1265239 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days | 2015 | European journal of medicinal chemistry, Dec-01, Volume: 106 | Structure activity relationships of 4-hydroxy-2-pyridones: A novel class of antituberculosis agents. |
| AID369297 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis H37Rv | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID370251 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 2.5 mg/kg, po administered once daily measured after 28 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID369316 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis TN1195 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID585252 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID699004 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID1851919 | Solubility of compound in water by LC-UV analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID698986 | Cmax in human at 50 to 1500 mg, po | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID445275 | Metabolic stability in pooled CD1 mouse liver microsomes assessed as compound remaining after 1 hr by LC-MS-MS | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1851924 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as bacterial growth inhibition incubated for 5 days under hypoxic condition by resazurin microtiter assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID369332 | Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis TN1037 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID585228 | Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse at 12.5 mg/kg, po for 5 days relative to control | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1851927 | Substrate activity at Mycobacterium tuberculosis Ddn expressed in Escherichia coli BL21 (DE3) assessed as oxidation of F420H2 by measuring Km by spectrophotometric analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID585240 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID370444 | Antimycobacterial activity against wild type Mycobacterium tuberculosis H37Rv NRP-2 stage after 3 weeks under anaerobic condition | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Structure-activity relationships of antitubercular nitroimidazoles. 2. Determinants of aerobic activity and quantitative structure-activity relationships. |
| AID585454 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID585236 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID760162 | Antimycobacterial activity against isoniazid, rifampin, ethambutol, kanamycin and rifabutin-resistant Mycobacterium tuberculosis after 14 days | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Advancement of Imidazo[1,2- |
| AID556427 | Bioavailability (0 to infinity) in guinea pig at 40 mg/kg, po by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID445273 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS assay | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID556454 | Half life in po dosed monkey | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID564978 | Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring inactivated p55 gene by resazurine microtiter assay | 2009 | Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9 | Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth. |
| AID581003 | Half life in healthy human | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development. |
| AID556448 | Cmax in guinea pig at 60 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1585793 | Apparent permeability across basolateral to apical side in human Caco2 cells at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID370071 | Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35822 after 14 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID445892 | Thermodynamic solubility in water at pH 7.4 at | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. |
| AID643078 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring pFCA-lux AB gene measured under aerobic condition after 8 days by luminescence analysis | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1585790 | Metabolic stability in CD-1 mouse plasma assessed as parent compound remaining at 3 uM after 2 hrs by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID645530 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in GAS medium after 1 week by microplate alamar blue assay | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity. |
| AID698994 | Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID585474 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID760164 | Antimycobacterial activity against isoniazid, rifampin, ethambutol, kanamycin and p-aminosalicylic acid-resistant Mycobacterium tuberculosis after 14 days | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Advancement of Imidazo[1,2- |
| AID369315 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis TN772 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID765268 | T>MIC in Mycobacterium tuberculosis infected mouse | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17 | A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis. |
| AID556434 | Bioavailability (0 to infinity) in guinea pig at 20 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID585459 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 10% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID585258 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.06250 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID369324 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv with plasmid MH102 infected in BALB/c mouse assessed as reduction in mycobacterial burden in lung at 50 mg/kg, po daily after 4 days of infection for 7 to 60 days relative to isoniazid | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID585470 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1063302 | Antitubercular activity against rifampin-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 16 to 24 hrs by microplate-Alamar Blue assay | 2014 | European journal of medicinal chemistry, Jan-24, Volume: 72 | Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents. |
| AID774295 | Antimycobacterial activity against kanamycin-resistant Mycobacterium tuberculosis ATCC 35827 | 2013 | Journal of natural products, Oct-25, Volume: 76, Issue:10 | Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. |
| AID556432 | Cmax in guinea pig at 20 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1851956 | Cmax in CD-1 mouse at 25 mg/kg, po measured upto 48 hrs by LC/MS/MS analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID556440 | Cmax in guinea pig at 40 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID585457 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID461172 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by low-oxygen-recovery assay | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3 | Synthesis, antimalarial and antitubercular activity of acetylenic chalcones. |
| AID643083 | Metabolic stability of the compound in human liver microsomes assessed as compound remaining after 1 hr | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1851937 | Stability in human plasma assessed as compound remaining measured after 2 hrs | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID585237 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 400 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 5% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID599556 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity. |
| AID556419 | Cmax in guinea pig at 20 mg/kg, iv by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1654616 | Aqueous solubility of the compound in pH 6.8 buffer | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Metabolic and Pharmaceutical Aspects of Fluorinated Compounds. |
| AID1654618 | Intrinsic clearance in human liver microsome | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Metabolic and Pharmaceutical Aspects of Fluorinated Compounds. |
| AID369330 | Inhibition of protein synthesis in log phase Mycobacterium bovis BCG assessed as [35S] incorporation after 3 hrs | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID774299 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 10 days under low oxygen condition followed by normoxic environment for 28 hrs by low oxygen recovery assay | 2013 | Journal of natural products, Oct-25, Volume: 76, Issue:10 | Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. |
| AID585232 | Toxicity in BALB/c mouse assessed as adverse effect up to 1456 mg/kg, po administered as single dose | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID285162 | Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as bacterial density after 10 days | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis. |
| AID645532 | Antitubercular activity against non-replicating Mycobacterium tuberculosis H37Rv expressing vibrio harveyii luciferase gene incubated 10 days under anaerobic condition measured after 28 hrs of recovery in aerobic condition by luciferase based low oxygen r | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity. |
| AID315119 | Antitubercular activity against Mycobacterium tuberculosis H37Rv T3 nitroreductase mutant | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824. |
| AID1269349 | Antimicrobial activity against Enterococcus faecalis | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID1269336 | Plasma protein binding in human | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID760166 | Antimycobacterial activity against isoniazid, rifampin, ethambutol, pyrazinamide, streptomycin, kanamycin and p-aminosalicylic acid-resistant Mycobacterium tuberculosis after 14 days | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Advancement of Imidazo[1,2- |
| AID1585771 | Antibacterial activity against non-replicating Mycobacterium tuberculosis H37Rv after 5 days under hypoxic condition by resazurin dye-based fluorescence assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID315117 | Antitubercular activity against Mycobacterium tuberculosis H37Rv under aerobic conditions | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824. |
| AID1269350 | Antimicrobial activity against Staphylococcus aureus | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID445274 | Metabolic stability in pooled human liver microsomes assessed as compound remaining after 1 hr by LC-MS-MS | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1 | Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID620627 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse chronic infection model assessed as fold reduction in bacterial CFU in lungs at 100 mg/kg, po administered for 5 days a week for 3 weeks beginning on day 70 postin | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID369323 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv with plasmid MH102 infected in BALB/c mouse assessed as reduction in mycobacterial burden in lung at 25 mg/kg, po daily after 4 days of infection for 10 days relative to isoniazid | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID626868 | Antimicrobial activity against non-replicating Mycobacterium tuberculosis after 11 days by luminescence based low oxygen recovery assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin. |
| AID369326 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in Hartley guinea pig assessed as reduction in mycobacterial burden in lung at 40 mg/kg, po daily after 30 days of infection for 30 days relative to isoniazid | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID556457 | Tmax in po dosed rat | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| 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. |
| AID445891 | Solubility in water at pH 7 at 20 degC | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. |
| AID564983 | Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring pPAZ23 carrying p27-p55 operon by resazurine microtiter assay | 2009 | Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9 | Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth. |
| AID556462 | Metabolic stability of the compound assessed as compound remaining in lung of guinea pig administered via intratracheal insufflation | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID556444 | AUC (0 to infinity) in guinea pig at 60 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID564988 | Antimicrobial activity against Mycobacterium bovis BCG harboring pPAZ23 carrying p27-p55 operon by resazurine microtiter assay | 2009 | Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9 | Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth. |
| AID445897 | Protein binding in human plasma | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. |
| AID572880 | Antibacterial activity against Mycobacterium bovis BCG harboring moaD gene by microplate Alamar Blue assay | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Efficacy of quinoxaline-2-carboxylate 1,4-di-N-oxide derivatives in experimental tuberculosis. |
| AID1162166 | Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development. |
| AID1269356 | Antimicrobial activity against Pseudomonas aeruginosa | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID346843 | Antimycobacterial activity against Mycobacterium tuberculosis with deazaflavin-dependent nitroreductase mutant under anaerobic condition | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Structure-activity relationships of antitubercular nitroimidazoles. 1. Structural features associated with aerobic and anaerobic activities of 4- and 5-nitroimidazoles. |
| AID370443 | Antimycobacterial activity against wild type Mycobacterium tuberculosis H37Rv ATCC 27294 after 2 weeks | 2009 | Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5 | Structure-activity relationships of antitubercular nitroimidazoles. 2. Determinants of aerobic activity and quantitative structure-activity relationships. |
| AID1851926 | Substrate activity at Mycobacterium tuberculosis Ddn expressed in Escherichia coli BL21 (DE3) assessed as oxidation of F420H2 by measuring Kcat by spectrophotometric analysis | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID643120 | Induction of mutagenesis in Salmonella Typhimurium TA98 in absence of rat liver S9 fraction by Ames test | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1871985 | Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Tuberculosis drug discovery: Progression and future interventions in the wake of emerging resistance. |
| AID370255 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 40 mg/kg, po administered once daily measured after 28 days | 2006 | PLoS medicine, Nov, Volume: 3, Issue:11 | OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. |
| AID541701 | Antitubercular activity against Mycobacterium tuberculosis H37Rv by MABA method | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID556412 | Chemical stability of the compound at 40 degC | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID556420 | Tmax in guinea pig at 20 mg/kg, iv by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID396484 | Bactericidal activity against Mycobacterium tuberculosis prcAB/tetR mutant after 3 days under anaerobic condition by serial dilution method | 2008 | Science (New York, N.Y.), Nov-28, Volume: 322, Issue:5906 | PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. |
| AID369321 | Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate IS6110 infected in mouse at 25 mg/kg, po | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID1585768 | Antibacterial activity against Clostridium difficile 630 ATCC BAA-1382 by broth microdilution assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID370056 | Antimycobacterial activity against Mycobacterium tuberculosis | 2005 | Antimicrobial agents and chemotherapy, Jun, Volume: 49, Issue:6 | New small-molecule synthetic antimycobacterials. |
| AID1851923 | Antimycobacterial activity against Mycobacterium smegmatis mc2155 ATCC 700084 assessed as bacterial growth inhibition incubated for 24 hrs under normoxic condition by resazurin microtiter assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID1243375 | Antimycobacterial activity against Mycobacterium tuberculosis infected in mouse assessed as fold reduction of colony forming units in lungs at 100 mg/kg, po administered for 5 days a week for 3 weeks beginning on day 70 post-infection relative to control | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy. |
| AID369335 | Inhibition of nucleic acid synthesis in Mycobacterium bovis BCG | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID315120 | Antitubercular activity against Mycobacterium tuberculosis H37Rv 5A1 nitroreductase mutant | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7 | Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824. |
| AID585475 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1269355 | Antimicrobial activity against Klebsiella pneumoniae | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID549614 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv after 2 weeks | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2 | The effect of 5-substitution on the electrochemical behavior and antitubercular activity of PA-824. |
| AID643116 | Thermodynamic solubility of the compound at pH 1 | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID369319 | Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis TN1811 | 2000 | Nature, Jun-22, Volume: 405, Issue:6789 | A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. |
| AID445888 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 16 to 24 hrs by microplate alamar blue assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. |
| AID1243369 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 8 days by MABA assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy. |
| 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. |
| AID1243383 | Ratio of pretomanid MIC90 to compound MIC90 for Mycobacterium tuberculosis H37Rv after 8 days by MABA assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18 | Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy. |
| AID556429 | Elimination rate constant in guinea pig at 20 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID774300 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate Alamar blue assay | 2013 | Journal of natural products, Oct-25, Volume: 76, Issue:10 | Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. |
| AID1585791 | Protein binding in human plasma at 5 uM after 30 mins by LC-MS/MS analysis based ultrafiltration method | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID285159 | Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed by relative light units after 7 days | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4 | Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis. |
| AID556445 | Elimination rate constant in guinea pig at 60 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID614928 | Bactericidal activity against Mycobacterium tuberculosis assessed as minimum concentration required for anaerobicidal activity | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16 | Structure-activity relationships of antitubercular nitroimidazoles. 3. Exploration of the linker and lipophilic tail of ((s)-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)-(4-trifluoromethoxybenzyl)amine (6-amino PA-824). |
| AID643094 | Antimicrobial activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as fold reduction in lung CFU at 100 mg/kg, po administered 70 days after post infection qd for 5 days per week for 3 weeks | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1269334 | Apparent permeability from basolateral to apical side in human Caco2 cells | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID1585792 | Apparent permeability across apical to basolateral side in human Caco2 cells at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
| AID585469 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.25000 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1468875 | Antitrypanosomal activity against Trypanosoma cruzi infected in human MRC5 cells after 7 days by alpha-galactosidase reporter gene assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis. |
| AID643084 | Metabolic stability of the compound in CD-1 mouse liver microsomes assessed as compound remaining after 1 hr | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID541940 | Antitubercular activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as reduction in lung microbial load at 100 mg/kg, po qd for 5 days per week for 3 weeks administered 11 days post infection relative to OPC-67683 | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID1269342 | Volume of distribution at steady state in CD-1 mouse at 10 mg/kg, iv after 0.02 to 48 hrs by LC-MS/MS method | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID739411 | Antitubercular activity against Mycobacterium tuberculosis H37Rv after 21 days by spectrophotometric analysis | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10 | Preliminary structure-activity relationships and biological evaluation of novel antitubercular indolecarboxamide derivatives against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains. |
| AID585245 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 200 mg assessed as time during compound concentration exceeds MIC of 0.03125 ug/ml assuming 15% unbound compound concentration by one compartment | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID1468876 | Antitrypanosomal activity against Trypanosoma brucei bloodstream forms after 72 hrs by resazurin dye based assay | 2018 | Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6 | Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis. |
| AID1659809 | Antimycobacterial activity against Mycobacterium tuberculosis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Molecule Property Analyses of Active Compounds for |
| AID760165 | Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis clinical isolate 2 after 14 days | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7 | Advancement of Imidazo[1,2- |
| AID1851931 | Plasma protein binding in human | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection. |
| AID1557270 | Antitubercular activity against Mycobacterium tuberculosis by radiometric analysis | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Drug-resistance in |
| AID556442 | Bioavailability (0 to infinity) in guinea pig at 40 mg/kg, administered via intratracheal insufflation by HPLC method | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1871984 | Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Tuberculosis drug discovery: Progression and future interventions in the wake of emerging resistance. |
| AID1269330 | Cytotoxicity against African green monkey Vero cells by cell titer glo assay | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids. |
| AID541942 | Metabolic stability in CD1 mouse liver microsomes assessed as compound remaining after 1 hr | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23 | Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). |
| AID581004 | Tmax in healthy human | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development. |
| AID585456 | fT>MIC for >= 1 log reduction in CFU count in Mycobacterium tuberculosis H37Rv in using simulated dose of at 100 mg assessed as time during compound concentration exceeds MIC of 0.12500 ug/ml assuming 7% unbound compound concentration by one compartment h | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | PA-824 exhibits time-dependent activity in a murine model of tuberculosis. |
| AID556413 | Chemical stability of the compound after 6 months | 2009 | Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4 | Dry powder nitroimidazopyran antibiotic PA-824 aerosol for inhalation. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| [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 | 0 (0.00) | 18.2507 |
| 2000's | 39 (15.60) | 29.6817 |
| 2010's | 133 (53.20) | 24.3611 |
| 2020's | 78 (31.20) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (31.65) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 22 (8.76%) | 5.53% |
| Reviews | 30 (11.95%) | 6.00% |
| Case Studies | 1 (0.40%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 198 (78.88%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||