OPC-67683: an antitubercular agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 6480466 |
| CHEMBL ID | 218650 |
| CHEBI ID | 134742 |
| SCHEMBL ID | 57791 |
| MeSH ID | M0505349 |
| Synonym |
|---|
| delamanid |
| opc-67683 |
| 2-methyl-6-nitro-2-[(4-{4-[4-(trifluoromethoxy)phenoxy]piperidin-1-yl}phenoxy)methyl]-2,3-dihydroimidazo[2,1-b]oxazole, (2r)- |
| 681492-22-8 |
| (2r)-2-methyl-6-nitro-2-[[4-[4-[4-(trifluoromethoxy)phenoxy]-1-piperidyl]phenoxy]methyl]-3h-imidazo[2,1-b]oxazole |
| CHEBI:134742 |
| CHEMBL218650 |
| opc 67683 |
| deltyba (tn) |
| delamanid (jan/usan) |
| D09785 |
| delamanid [usan:inn:jan] |
| (2r)-2-methyl-6-nitro-2-((4-(4-(4-(trifluoromethoxy)phenoxy)piperidin-1- yl)phenoxy)methyl)-2,3-dihydroimidazo(2,1-b)oxazole |
| 8oot6m1pc7 , |
| unii-8oot6m1pc7 |
| imidazo(2,1-b)oxazole, 2,3-dihydro-2-methyl-6-nitro-2-((4-(4-(4-(trifluoromethoxy)phenoxy)-1-piperidinyl)phenoxy)methyl)-, (2r)- |
| NCGC00348214-01 |
| SCHEMBL57791 |
| (r)-2-methyl-6-nitro-2-(4-[4-(4-trifluoromethoxyphenoxy)piperidin-1-yl]phenoxymethyl}-2,3-dihydroimidazo[2,1-b]oxazole |
| (r)-2-methyl-6-nitro-2-{4-[4-(4-trifluoromethoxyphenoxy)piperidin-1-yl]phenoxymethyl}-2,3-dihydroimidazo[2,1-b]oxazole |
| delamanid [inn] |
| deltyba |
| delamanid [who-dd] |
| opc67683 |
| (2r)-2-methyl-6-nitro-2-((4-(4-(4-(trifluoromethoxy)phenoxy)piperidin-1-yl)phenoxy)methyl)-2,3-dihydroimidazo(2,1-b)(1,3)oxazole |
| delamanid [mi] |
| delamanid [jan] |
| delamanid [usan] |
| HY-10846 |
| CS-5866 |
| AKOS025289781 |
| [(2r)-2-methyl-2-[[4-[4-[4-(trifluoromethoxy)phenoxy]-1-piperidyl]phenoxy]methyl]-3h-imidazo[2,1-b]oxazol-6-yl]azinic acid |
| DTXSID60218326 |
| (2r)-2,3-dihydro-2-methyl-6-nitro-2-[[4-[4-[4-(trifluoromethoxy)phenoxy]-1-piperidinyl]phenoxy]methyl]imidazo[2,1-b]oxazole |
| s5007 , |
| (r)-2-methyl-6-nitro-2-((4-(4-(4-(trifluoromethoxy)phenoxy)piperidin-1-yl)phenoxy)methyl)-2,3-dihydroimidazo[2,1-b]oxazole |
| mfcd18251539 |
| mmv688262 |
| delamanid (opc-67683) |
| BCP07838 |
| delamanid; opc 67683; opc67683 |
| opc-67683; delamanid |
| EX-A2414 |
| DB11637 |
| Q15408413 |
| SB14863 |
| CCG-269934 |
| nsc794689 |
| nsc-794689 |
| (2r)-2-methyl-6-nitro-2-[(4-{4-[4-(trifluoromethoxy)phenoxy]-1-piperidinyl}phenoxy)methyl]-2,3-dihydroimidazo[2,1-b][1,3]oxazole |
| A856044 |
| AS-56105 |
| AC-35849 |
| bdbm50592580 |
| 1-(4-{[(2r)-2-methyl-6-nitro-2h,3h-imidazo[2,1-b][1,3]oxazol-2-yl]methoxy}phenyl)-4-[4-(trifluoromethoxy)phenoxy]piperidine |
| EN300-20602812 |
Five such compounds were >100-fold better than the parent drug in a mouse model of acute Mycobacterium tuberculosis infection. Two orally bioavailable pyridine analogues were superior to antitubercular drug OPC-67683 in a chronic infection model.
| 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) | 0.54 |
| " 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) | 0.57 |
| " 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 |
| " Delamanid PK was adequately described for all observed dosing regimens and subpopulations by a two-compartment model with first-order elimination and absorption, an absorption lag time, and decreased relative bioavailability with increasing dose." | ( Population Pharmacokinetic Analysis of Delamanid in Patients with Pulmonary Multidrug-Resistant Tuberculosis. Gibiansky, E; Mallikaarjun, S; Wang, X, 2020) | 0.56 |
| " The covariates included in the model were body weight on the apparent volume of distribution and apparent clearance (for both delamanid and DM-6705); formulation (dispersible versus film-coated tablet) on the mean absorption time; age, formulation, and dose on the bioavailability of delamanid; and age on the fraction of delamanid metabolized to DM-6705." | ( Population Pharmacokinetic and Concentration-QTc Analysis of Delamanid in Pediatric Participants with Multidrug-Resistant Tuberculosis. Hafkin, J; Karlsson, MO; Mallikaarjun, S; Sasaki, T; Svensson, EM; Wang, X; Wang, Y, 2022) | 0.72 |
| "Poor solubility is a major challenge that can limit the oral bioavailability of many drugs, including delamanid, a weakly basic nitro-dihydro-imidazooxazole derivative used to treat tuberculosis." | ( Combining enabling formulation strategies to generate supersaturated solutions of delamanid: In situ salt formation during amorphous solid dispersion fabrication for more robust release profiles. Duong, TV; Nguyen, HT; Taylor, LS, 2022) | 0.72 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Regimens should contain at least one new class of drug; be broadly applicable for use against MDR and extensively drug-resistant Mycobacterium tuberculosis complex strains; contain three to five effective drugs, each from a different drug class; be delivered orally; have a simple dosing schedule; have a good side-effect profile that allows limited monitoring; last a maximum of 6 months; and have minimal interaction with antiretrovirals." | ( Principles for designing future regimens for multidrug-resistant tuberculosis. Balasegaram, M; Brigden, G; du Cros, P; Horsburgh, CR; Hughes, J; McIlleron, H; Mitnick, CD; Nuermberger, E; Nyang'wa, BT; Phillips, PP; Rich, M; Varaine, F, 2014) | 0.4 |
| " Its superior potency and pharmacokinetic profile that predicts suitability for once-daily oral dosing suggest that TBA-354 be studied further for its potential as a next-generation nitroimidazole." | ( 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 |
| " M1 had the highest exposure among the eight metabolites after repeated oral dosing in humans, which indicated that M1 was the major metabolite." | ( Pharmacokinetics and Metabolism of Delamanid, a Novel Anti-Tuberculosis Drug, in Animals and Humans: Importance of Albumin Metabolism In Vivo. Hirao, Y; Kitano, K; Koyama, N; Sasahara, K; Shibata, M; Shimokawa, Y; Umehara, K, 2015) | 0.42 |
| " Twice-daily oral dosing of delamanid at 30 mg kg(-1) for 5 days resulted in sterile cures in a mouse model of VL." | ( The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis. Auer, JL; Fairlamb, AH; Norval, S; Osuna-Cabello, M; Patterson, S; Read, KD; Simeons, FR; Stojanovski, L; Wyllie, S, 2016) | 0.43 |
| " Coadministration of Kaletra (lopinavir/ritonavir) with delamanid resulted in an approximately 25% higher delamanid area under the concentration-time curve from time 0 to the end of the dosing interval (AUCτ)." | ( Delamanid Coadministered with Antiretroviral Drugs or Antituberculosis Drugs Shows No Clinically Relevant Drug-Drug Interactions in Healthy Subjects. Geiter, L; Mallikaarjun, S; Paccaly, A; Patil, S; Petersen, C; Shoaf, SE; Wells, C, 2016) | 0.43 |
| " Combinations of optimal dose and release rates were simulated such that plasma concentrations were maintained over the epidemiological cut-off or minimum inhibitory concentration for the dosing interval." | ( Modelling the long-acting administration of anti-tuberculosis agents using PBPK: a proof of concept study. Flexner, C; Moss, DM; Owen, A; Podany, AT; Rajoli, RKR; Siccardi, M; Swindells, S, 2018) | 0.48 |
| " Studies of explanted lungs from patients with drug-resistant tuberculosis have shown substantial drug-specific gradients across pulmonary cavities, suggesting that alternative dosing and drug delivery strategies are needed to reduce functional monotherapy at the site of disease." | ( The Lancet Respiratory Medicine Commission: 2019 update: epidemiology, pathogenesis, transmission, diagnosis, and management of multidrug-resistant and incurable tuberculosis. Dheda, K; Dooley, KE; Furin, J; Gumbo, T; Maartens, G; Murray, M; Nardell, EA; Warren, RM, 2019) | 0.51 |
| " The high frequency of dosing leads to poor adherence for patients who live in lower economic and nomadic populations." | ( Sustained absorption of delamanid from lipid-based formulations as a path to reduced frequency of administration. Boyd, BJ; Clulow, AJ; Hawley, A; Pham, AC; Ramirez, G; Salim, M, 2021) | 0.62 |
| " Delamanid PK was adequately described for all observed dosing regimens and subpopulations by a two-compartment model with first-order elimination and absorption, an absorption lag time, and decreased relative bioavailability with increasing dose." | ( Population Pharmacokinetic Analysis of Delamanid in Patients with Pulmonary Multidrug-Resistant Tuberculosis. Gibiansky, E; Mallikaarjun, S; Wang, X, 2020) | 0.56 |
| "We found a strong association of weight with bedaquiline and clofazimine exposure parameters, suggesting the need for weight-based dosing for those agents." | ( Pharmacokinetics of bedaquiline, delamanid and clofazimine in patients with multidrug-resistant tuberculosis. Al-Shaer, MH; Alghamdi, WA; Barbakadze, K; Kempker, RR; Kipiani, M; Mikiashvili, L; Peloquin, CA, 2021) | 0.62 |
| " Predictions with the final model suggested a similar QT prolonging potential with simplified, once-daily dosing regimens compared with the approved regimens, with a maximum median change from baseline QTcF increase of 20 milliseconds in both regimens." | ( Assessing Prolongation of the Corrected QT Interval with Bedaquiline and Delamanid Coadministration to Predict the Cardiac Safety of Simplified Dosing Regimens. Cramer, YS; Diacon, AH; Dooley, KE; Karlsson, MO; Maartens, G; Morganroth, J; Rosenkranz, SL; Shenje, J; Svensson, EM; Tanneau, L; Upton, CM, 2022) | 0.72 |
| Class | Description |
|---|---|
| piperidines | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0001 | 1.7740 | 10.0000 | AID1862192 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0001 | 1.7536 | 10.0000 | AID1862198 |
| Cytochrome P450 2C8 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0008 | 1.8848 | 7.9000 | AID1862194 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0000 | 2.0151 | 10.0000 | AID1862197 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0000 | 2.8005 | 10.0000 | AID1862195 |
| Cytochrome P450 2B6 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0011 | 3.4186 | 10.0000 | AID1862193 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.0000 | 2.3983 | 10.0000 | AID1862196 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 30.0000 | 0.0009 | 1.9014 | 10.0000 | AID1862199 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID698981 | Tmax in Mycobacterium tuberculosis infected mouse at 2.5 mg/kg | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID1862199 | Inhibition of human ERG | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID370286 | Effect on CYP2C19 in human liver assessed as S-mephenytoin 49 hydroxylation at 30 uM relative to control | 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. |
| AID370295 | Effect on CYP3A4 in human liver assessed as testosterone 6-beta-hydroxylation at 30 uM relative to control | 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. |
| AID1557274 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 35837 | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Drug-resistance in |
| AID1862182 | Aqueous solubility of compound at pH 7.4 | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID1290492 | Antileishmanial activity against amastigote stage of Leishmania infantum in early curative golden hamster chronic visceral leishmaniasis model assessed as reduction in parasite load in spleen at 50 mg/kg, po qd administered for 5 days by Giemsa staining-b | 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. |
| AID1557276 | Antitubercular activity against Mycobacterium tuberculosis Kurono ATCC 35812 | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Drug-resistance in |
| 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. |
| AID1862173 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition incubated for 10 days under hypoxic condition followed by 28 hrs incubation under normoxic condition by Low-Oxygen-Recovery Assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID1290458 | Kinetic aqueous solubility of compound at pH 7 at 20 degC by HPLC analysis | 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. |
| AID1290452 | Antileishmanial activity against amastigote stage of Leishmania infantum infected in mouse primary peritoneal macrophages assessed as parasite growth inhibition incubated for 5 days by Giemsa staining-based microscopic analysis | 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. |
| AID699005 | Inhibition of methoxy-mycolic acid biosynthesis in Mycobacterium tuberculosis | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID1456712 | Antileishmanial activity against Leishmania donovani LV9 amastigotes infected in po dosed BALB/c mouse assessed as reduction in parasite burden dosed on day 7 post-infection administered bid for 5 to 10 days | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Nitroimidazoles: Molecular Fireworks That Combat a Broad Spectrum of Infectious Diseases. |
| AID370274 | Effect on CYP1A1/CYP1A2 in human liver assessed as 7-ethoxyresorufin O-deethylation at 10 uM relative to control | 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. |
| AID1659809 | Antimycobacterial activity against Mycobacterium tuberculosis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Molecule Property Analyses of Active Compounds for |
| AID370090 | Drug metabolism in OPC-67683 resistant Mycobacterium bovis BCG Tokyo assessed as cell pellet [14C]OPC-67683 metabolite level after 48 hrs by scintillation counting | 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. |
| AID370282 | Effect on CYP2C8/CYP2C9 in human liver assessed as tolubutamide methylhydroxylation at 10 uM relative to control | 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. |
| AID370303 | Stability in dog liver microsomes | 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. |
| AID1552797 | Apparent permeability across basolateral to apical side in MDCK cells at 100 mM incubated for 60 mins by HPLC analysis | 2019 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17 | Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents. |
| AID370247 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 0.156 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. |
| AID370098 | Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 2.5 mg/kg, po after 12 hrs | 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. |
| AID370078 | Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis isolates | 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. |
| 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. |
| AID1264496 | Selectivity index, ratio of CC50 for human HepG2 cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 27294 | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10 | Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents. |
| AID1862187 | Plasma protein binding in rat assessed as bound fraction | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID1862188 | Plasma protein binding in dog assessed as bound fraction | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID1264491 | Aqueous solubility of compound at pH7 for 4 hrs by HPLC analysis | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10 | Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents. |
| AID370279 | Effect on CYP2B6 in human liver assessed as 7-benzyloxyresorufin O-debenzylation at 10 uM relative to control | 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. |
| 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. |
| AID698980 | Cmax in Mycobacterium tuberculosis infected mouse at 2.5 mg/kg | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID541936 | 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 PA-824 | 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). |
| AID370248 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 0.313 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. |
| AID1766395 | Antileishmanial activity against wild type Leishmania donovani promastigotes incubated for 72 hrs by resazurin dye based assay | 2021 | ACS medicinal chemistry letters, Sep-09, Volume: 12, Issue:9 | Monocyclic Nitro-heteroaryl Nitrones with Dual Mechanism of Activation: Synthesis and Antileishmanial Activity. |
| AID370082 | Antimycobacterial activity against streptomycin-resistant Mycobacterium tuberculosis isolates | 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. |
| AID1435708 | Antimycobacterial activity against Mycobacterium tuberculosis after 14 days | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents. |
| AID1862200 | Antimycobacterial activity against clinical isolate multidrug resistant Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID1290453 | Antitrypanosomal activity against Trypanosoma cruzi infected in human MRC5 cells assessed as parasite growth inhibition incubated for 7 days by chlorophenol red alpha-D-galactopyranoside-based assay | 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. |
| AID541938 | Antitubercular activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as reduction in lung microbial load at 30 mg/kg, po qd for 5 days per week for 8 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). |
| AID1862189 | Plasma protein binding in human assessed as bound fraction | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID274946 | Reduction in log CFU of Mycobacterium tuberculosis Kurono infected in mouse lung at 0.5 mg/kg, po after 10 days | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis and antituberculosis activity of a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles. |
| 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). |
| AID1766403 | Antileishmanial activity against Leishmania donovani LdBOB derived from MHOM/SD/62/1 S-CL2D promastigotes overexpressing NTR2 incubated for 72 hrs by resazurin dye based assay | 2021 | ACS medicinal chemistry letters, Sep-09, Volume: 12, Issue:9 | Monocyclic Nitro-heteroaryl Nitrones with Dual Mechanism of Activation: Synthesis and Antileishmanial Activity. |
| AID1862202 | Antimycobacterial activity against Mycobacterium tuberculosis Erdman assessed as bacterial growth inhibition | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID370096 | Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 2.5 mg/kg, po after 6 hrs | 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. |
| AID1290456 | Antitubercular activity against Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay | 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. |
| AID370065 | Toxic mutagenic effect in Salmonella Typhimurium TA100 in presence of rat liver microsomes after 48 hrs by bacterial reverse mutation test | 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. |
| AID370067 | Toxic mutagenic effect in Salmonella Typhimurium TA1537 in presence of rat liver microsomes after 48 hrs by bacterial reverse mutation test | 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. |
| 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. |
| AID370088 | Drug metabolism in OPC-67683 resistant Mycobacterium bovis BCG Tokyo assessed as cell supernatant [14C]OPC-67683 metabolite level after 48 hrs by scintillation counting | 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. |
| AID370298 | Effect on CYP3A4 in human liver assessed as nifedipine oxidation at 30 uM relative to control | 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. |
| AID370294 | Effect on CYP3A4 in human liver assessed as testosterone 6-beta-hydroxylation at 10 uM relative to control | 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. |
| AID1475123 | Stability in pooled human liver microsomes assessed as compound remaining measured after 1 hr | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]thiazoles: Facile synthesis and comparative appraisal against tuberculosis and neglected tropical diseases. |
| AID1264494 | Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis by resazurin microtiter assay | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10 | Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents. |
| AID370292 | Effect on CYP2E1 in human liver assessed as chlorzoxazone 6-hydroxylation at 30 uM relative to control | 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. |
| AID1290455 | Cytotoxicity against human MRC5 cells assessed as cell viability incubated for 72 hrs by fluorimetric assay | 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. |
| AID1475125 | Anti-tubercular activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as reduction in lung colony forming units at 100 mg/kg, po administered via gavage for 5 days each week for 3 weeks measured after 1 day post last dose relative | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]thiazoles: Facile synthesis and comparative appraisal against tuberculosis and neglected tropical diseases. |
| AID1862183 | Apparent permeability across apical to basolateral side in dog MDCK cells | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID370086 | Inhibition of keto-mycolic acid synthesis in Mycobacterium bovis BCG after 60 mins | 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. |
| 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. |
| AID370068 | Toxic mutagenic effect in Escherichia coli WP2 uvrA in presence of rat liver microsomes after 48 hrs by bacterial reverse mutation test | 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. |
| AID370265 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected po dosed BALB/c mouse assessed as reduction in viable lung bacterial count administered once daily | 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. |
| AID370089 | Drug metabolism in Mycobacterium bovis BCG Tokyo assessed as cell pellet [14C]OPC-67683 metabolite level after 48 hrs by scintillation counting | 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. |
| AID370304 | Stability in rabbit liver microsomes | 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. |
| AID370302 | Stability in mouse liver microsomes | 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. |
| AID370276 | Effect on CYP1A1/CYP1A2 in human liver assessed as 7-ethoxyresorufin O-deethylation at 100 uM relative to control | 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. |
| AID1290459 | Kinetic solubility of compound in 0.1 M HCl at pH 1 at 20 degC by HPLC analysis | 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. |
| AID1290494 | Antileishmanial activity against amastigote stage of Leishmania infantum in early curative golden hamster chronic visceral leishmaniasis model assessed as reduction in parasite load in spleen at 12.5 mg/kg, po qd administered for 5 days by Giemsa staining | 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. |
| 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. |
| AID370066 | Toxic mutagenic effect in Salmonella Typhimurium TA1535 in presence of rat liver microsomes after 48 hrs by bacterial reverse mutation test | 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. |
| AID370092 | Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 2.5 mg/kg, po after 2 hrs | 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. |
| AID370275 | Effect on CYP1A1/CYP1A2 in human liver assessed as 7-ethoxyresorufin O-deethylation at 30 uM relative to control | 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. |
| AID370123 | Half life in Mycobacterium bovis BCG infected tuberculosis mouse model at 2.5 mg/kg, po | 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. |
| 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. |
| AID370280 | Effect on CYP2B6 in human liver assessed as 7-benzyloxyresorufin O-debenzylation at 30 uM relative to control | 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. |
| AID370080 | Antimycobacterial activity against ethambutol-resistant Mycobacterium tuberculosis isolates | 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. |
| AID370079 | Antimycobacterial activity against ethambutol-susceptible Mycobacterium tuberculosis isolates | 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. |
| AID274943 | Antituberculosis activity against INH resistant Mycobacterium tuberculosis H37Rv | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis and antituberculosis activity of a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles. |
| AID1862172 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition incubated for 7 days by MABA assay | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID1862171 | Metabolic stability in mouse liver microsomes assessed as half life | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID274949 | Decrease in Mycobacterium tuberculosis count in mouse pulmonary | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis and antituberculosis activity of a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles. |
| AID698979 | Half life in Mycobacterium tuberculosis infected mouse at 2.5 mg/kg | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID370306 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as reduction in viable lung bacterial count at 0.313 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. |
| AID1552792 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial cell growth incubated for 8 days measured under aerobic MABA conditions by alamar blue staining based assay | 2019 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17 | Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents. |
| AID1290488 | Antileishmanial activity against amastigote stage of Leishmania infantum in early curative golden hamster chronic visceral leishmaniasis model assessed as reduction in parasite load in liver at 50 mg/kg, po qd administered for 5 days by Giemsa staining-ba | 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. |
| AID1862192 | Inhibition of CYP1A2 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| 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. |
| AID370095 | Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 2.5 mg/kg, po after 4 hrs | 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. |
| AID274945 | Reduction in log CFU of Mycobacterium tuberculosis Kurono infected in mouse lung at 50 mg/kg, po relative to control | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis and antituberculosis activity of a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles. |
| 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. |
| AID370266 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected po dosed immunocompromized BALB/c mouse assessed as reduction in viable lung bacterial count administered once daily | 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. |
| AID370278 | Effect on CYP2A6 in human liver assessed as coumarin 7-hydroxylation at 100 uM relative to control | 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. |
| AID1862193 | Inhibition of CYP2B6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID698818 | Antimycobacterial activity against Mycobacterium tuberculosis infected in human assessed as log reduction of bacterial count at 100 to 400 mg, qd for 14 days | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID1862206 | In vivo antimycobacterial activity against Mycobacterium tuberculosis Erdman infected mouse chronic tuberculosis infection model assessed as reduction log10 CFU at 10 to 100 mg/kg for 4 weeks at 5 days/week administered after 31 days post infection relati | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID370305 | Stability in monkey liver microsomes | 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. |
| AID1862181 | Aqueous solubility of compound at pH 2.0 | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID1290493 | Antileishmanial activity against amastigote stage of Leishmania infantum in early curative golden hamster chronic visceral leishmaniasis model assessed as reduction in parasite load in spleen at 25 mg/kg, po qd administered for 5 days by Giemsa staining-b | 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. |
| AID1557273 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 35822 | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Drug-resistance in |
| AID1475124 | Stability in CD-1 mouse liver microsomes assessed as compound remaining measured after 1 hr | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]thiazoles: Facile synthesis and comparative appraisal against tuberculosis and neglected tropical diseases. |
| AID370077 | Antimycobacterial activity against isoniazid-susceptible Mycobacterium tuberculosis isolates | 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. |
| 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). |
| AID1862169 | Metabolic stability in human liver microsomes assessed as half life | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID370299 | Effect on CYP3A4 in human liver assessed as nifedipine oxidation at 100 uM relative to control | 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. |
| AID1862201 | Antimycobacterial activity against clinical isolate drug susceptible Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID370081 | Antimycobacterial activity against streptomycin-susceptible Mycobacterium tuberculosis isolates | 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. |
| AID1552798 | Efflux ratio of apparent permeability across basolateral to apical over apical to basolateral side in MDCK cells at 100 mM incubated for 60 mins by HPLC analysis | 2019 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17 | Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents. |
| 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. |
| 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. |
| AID1290497 | Antileishmanial activity against amastigote stage of Leishmania infantum in early curative golden hamster chronic visceral leishmaniasis model assessed as reduction in parasite load in bone marrow at 25 mg/kg, po qd administered for 5 days by Giemsa stain | 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. |
| AID370091 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in human THP1 cells after 4 hrs | 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. |
| AID370099 | Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 2.5 mg/kg, po after 24 hrs | 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. |
| AID581007 | Antimicrobial activity against compound-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. |
| AID370122 | Tmax in Mycobacterium bovis BCG infected tuberculosis mouse model at 2.5 mg/kg, po | 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. |
| AID1552791 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17 | Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents. |
| AID1264490 | Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by resazurin microtiter assay | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10 | Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents. |
| AID1862186 | Plasma protein binding in mouse assessed as bound fraction | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID1862197 | Inhibition of CYP2D6 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID370277 | Effect on CYP2A6 in human liver assessed as coumarin 7-hydroxylation at 30 uM relative to control | 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. |
| AID370097 | Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 2.5 mg/kg, po after 8 hrs | 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. |
| AID1862196 | Inhibition of CYP2C19 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID370121 | AUC (0 to t) in Mycobacterium bovis BCG infected tuberculosis mouse model at 2.5 mg/kg, po | 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. |
| AID698977 | Tmax in smear positive tuberculosis patient | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID698982 | Inhibition of keto-mycolic acid biosynthesis in Mycobacterium tuberculosis | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| 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. |
| AID1290457 | Antitubercular activity against Mycobacterium tuberculosis preincubated for 7 days under anaeorobic conditions followed by recovery for 28 hrs by Low-Oxygen-Recovery Assay | 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. |
| 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. |
| AID1557275 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 35820 | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Drug-resistance in |
| AID1552796 | Apparent permeability across apical to basolateral side in MDCK cells at 100 mM incubated for 60 mins by HPLC analysis | 2019 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17 | Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents. |
| AID698978 | AUC in Mycobacterium tuberculosis infected mouse at 2.5 mg/kg | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID370075 | Antimycobacterial activity against rifampicin-susceptible Mycobacterium tuberculosis isolates | 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. |
| AID370094 | Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 2.5 mg/kg, po after 1 hr | 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. |
| AID1552793 | Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial cell growth incubated for 11 days measured under anaerobic LORA condition by luminescence assay | 2019 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17 | Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents. |
| AID1862203 | In vivo antimycobacterial activity against Mycobacterium tuberculosis Erdman infected mouse acute tuberculosis infection model assessed as reduction lung bacterial loads by measuring CFU at 10 to 100 mg/kg for 3 weeks at 5 days/week | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID370296 | Effect on CYP3A4 in human liver assessed as testosterone 6-beta-hydroxylation at 100 uM relative to control | 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. |
| AID1475122 | Solubility in HCl at pH 1 after 15 mins by HPLC method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]thiazoles: Facile synthesis and comparative appraisal against tuberculosis and neglected tropical diseases. |
| AID370087 | Drug metabolism in Mycobacterium bovis BCG Tokyo assessed as cell supernatant [14C]OPC-67683 metabolite level after 48 hrs by scintillation counting | 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. |
| AID370291 | Effect on CYP2E1 in human liver assessed as chlorzoxazone 6-hydroxylation at 10 uM relative to control | 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. |
| AID1862170 | Metabolic stability in rat liver microsomes assessed as half life | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID698983 | Antimycobacterial activity against Mycobacterium tuberculosis infected in mouse assessed as reduction of CFU at 0.625 mg/kg | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Tuberculosis: the drug development pipeline at a glance. |
| AID1290489 | Antileishmanial activity against amastigote stage of Leishmania infantum in early curative golden hamster chronic visceral leishmaniasis model assessed as reduction in parasite load in liver at 25 mg/kg, po qd administered for 5 days by Giemsa staining-ba | 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. |
| 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. |
| AID1456711 | Antileishmanial activity against Leishmania donovani LV9 amastigotes infected in mouse peritoneal macrophages after 72 hrs | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Nitroimidazoles: Molecular Fireworks That Combat a Broad Spectrum of Infectious Diseases. |
| AID1290454 | Antitrypanosomal activity against trypomastigote stage of Trypanosoma brucei incubated for 72 hrs by resazurin staining-based fluorescence analysis | 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. |
| AID1862184 | Apparent permeability across basolateral to apical side in dog MDCK cells | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID1862194 | Inhibition of CYP2C8 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| 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. |
| AID370083 | Inhibition of fatty acid synthesis in Mycobacterium bovis BCG after 60 mins | 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. |
| AID370093 | Effect on CYP2A6 in human liver assessed as coumarin 7-hydroxylation at 10 uM relative to control | 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. |
| AID370260 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as reduction in viable lung bacterial count at 0.625 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. |
| AID1552794 | Solubility of the compound in water at pH 2 by HPLC analysis | 2019 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17 | Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents. |
| 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. |
| 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. |
| AID1862195 | Inhibition of CYP2C9 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID370281 | Effect on CYP2B6 in human liver assessed as 7-benzyloxyresorufin O-debenzylation at 100 uM relative to control | 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. |
| AID370288 | Effect on CYP2D6 in human liver assessed as bufuralol 19-hydroxylation at 10 uM relative to control | 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. |
| AID370249 | Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 0.625 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. |
| AID1552790 | Antimycobacterial activity against Mycobacterium bovis ATCC 35737 assessed as reduction in bacterial cell growth incubated for 8 days by alamar blue staining based assay | 2019 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17 | Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents. |
| AID1557271 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 25618 | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Drug-resistance in |
| AID370293 | Effect on CYP2E1 in human liver assessed as chlorzoxazone 6-hydroxylation at 100 uM relative to control | 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. |
| AID370120 | Cmax in Mycobacterium bovis BCG infected tuberculosis mouse model at 2.5 mg/kg, po | 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. |
| AID1290465 | Metabolic stability in hamster liver microsomes assessed as parent compound remaining at 1 uM after 1 hr by LC-MS/MS analysis | 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. |
| 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 |
| AID370287 | Effect on CYP2C19 in human liver assessed as S-mephenytoin 49 hydroxylation at 100 uM relative to control | 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. |
| AID370064 | Toxic mutagenic effect in Salmonella Typhimurium TA98 in presence of rat liver microsomes after 48 hrs by bacterial reverse mutation test | 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. |
| AID1862185 | Efflux ratio of apparent permeability across basolateral to apical over apical to basolateral membrane in dog MDCK cells | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID1264495 | Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10 | Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents. |
| AID370084 | Inhibition of alpha-mycolic acid synthesis in Mycobacterium bovis BCG after 60 mins | 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. |
| AID274944 | Antituberculosis activity against rifampicin resistant Mycobacterium tuberculosis H37Rv | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis and antituberculosis activity of a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles. |
| AID1766404 | Selectivity index, ratio of IC50 for antileishmanial activity against wild type Leishmania donovani promastigotes to IC50 for antileishmanial activity against Leishmania donovani LdBOB derived from MHOM/SD/62/1 S-CL2D promastigotes overexpressing NTR2 | 2021 | ACS medicinal chemistry letters, Sep-09, Volume: 12, Issue:9 | Monocyclic Nitro-heteroaryl Nitrones with Dual Mechanism of Activation: Synthesis and Antileishmanial Activity. |
| AID370300 | Stability in human liver microsomes | 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. |
| AID1264492 | Antimicrobial activity against nonreplicating Mycobacterium tuberculosis 18b by resazurin microtiter assay | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10 | Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents. |
| 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 |
| AID370076 | Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis isolates | 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. |
| AID1264493 | Antimicrobial activity against rifamycin-resistant Mycobacterium tuberculosis by resazurin microtiter assay | 2015 | ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10 | Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents. |
| AID370301 | Stability in rat liver microsomes | 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. |
| AID1475121 | Solubility in water at pH 7 after 15 mins by HPLC method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]thiazoles: Facile synthesis and comparative appraisal against tuberculosis and neglected tropical diseases. |
| AID274947 | Reduction in log CFU of Mycobacterium tuberculosis Kurono infected in mouse lung at 10 mg/kg, po after 10 days | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis and antituberculosis activity of a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles. |
| AID370285 | Effect on CYP2C19 in human liver assessed as S-mephenytoin 4'-hydroxylation at 10 uM relative to control | 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. |
| AID643097 | Antimicrobial activity against Mycobacterium tuberculosis infected in chronic BALB/c mouse infection model assessed as fold reduction in lung CFU at 100 mg/kg, po dministered 50 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). |
| 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. |
| AID370297 | Effect on CYP3A4 in human liver assessed as nifedipine oxidation at 10 uM relative to control | 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. |
| AID1290490 | Antileishmanial activity against amastigote stage of Leishmania infantum in early curative golden hamster chronic visceral leishmaniasis model assessed as reduction in parasite load in liver at 12.5 mg/kg, po qd administered for 5 days by Giemsa staining- | 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. |
| AID370283 | Effect on CYP2C8/CYP2C9 in human liver assessed as tolubutamide methylhydroxylation at 30 uM relative to control | 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. |
| AID1557272 | Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 35838 | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8 | Drug-resistance in |
| AID1862198 | Inhibition of CYP3A4 (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID370290 | Effect on CYP2D6 in human liver assessed as bufuralol 19-hydroxylation at 100 uM relative to control | 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. |
| 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. |
| AID1290496 | Antileishmanial activity against amastigote stage of Leishmania infantum in early curative golden hamster chronic visceral leishmaniasis model assessed as reduction in parasite load in bone marrow at 50 mg/kg, po qd administered for 5 days by Giemsa stain | 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. |
| AID1290498 | Antileishmanial activity against amastigote stage of Leishmania infantum in early curative golden hamster chronic visceral leishmaniasis model assessed as reduction in parasite load in bone marrow at 12.5 mg/kg, po qd administered for 5 days by Giemsa sta | 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. |
| AID370284 | Effect on CYP2C8/CYP2C9 in human liver assessed as tolubutamide methylhydroxylation at 100 uM relative to control | 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. |
| AID370289 | Effect on CYP2D6 in human liver assessed as bufuralol 19-hydroxylation at 30 uM relative to control | 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. |
| AID274942 | Antituberculosis activity against Mycobacterium tuberculosis H37Rv | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Synthesis and antituberculosis activity of a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles. |
| AID370085 | Inhibition of methoxy-mycolic acid synthesis in Mycobacterium bovis BCG after 60 mins | 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. |
| 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. |
| AID1871987 | Antimycobacterial activity against drug-susceptible Mycobacterium tuberculosis H37Rv | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Tuberculosis drug discovery: Progression and future interventions in the wake of emerging resistance. |
| AID1862174 | Cytotoxicity against African green monkey vero cells assessed as reduction in cell viability | 2022 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 72 | Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent. |
| AID1552795 | Solubility of the compound in water at pH 6.5 by HPLC analysis | 2019 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17 | Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents. |
| [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 | 11 (4.64) | 29.6817 |
| 2010's | 151 (63.71) | 24.3611 |
| 2020's | 75 (31.65) | 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 (18.07) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 17 (7.08%) | 5.53% |
| Reviews | 50 (20.83%) | 6.00% |
| Case Studies | 16 (6.67%) | 4.05% |
| Observational | 9 (3.75%) | 0.25% |
| Other | 148 (61.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||