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Items: 22

1.

Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.

Sutherland HS, Tong AST, Choi PJ, Blaser A, Franzblau SG, Cooper CB, Upton AM, Lotlikar M, Denny WA, Palmer BD.

Bioorg Med Chem. 2020 Jan 1;28(1):115213. doi: 10.1016/j.bmc.2019.115213. Epub 2019 Nov 26.

PMID:
31810890
2.

TBAJ-876 Displays Bedaquiline-Like Mycobactericidal Potency without Retaining the Parental Drug's Uncoupler Activity.

Sarathy JP, Ragunathan P, Cooper CB, Upton AM, Grüber G, Dick T.

Antimicrob Agents Chemother. 2020 Jan 27;64(2). pii: e01540-19. doi: 10.1128/AAC.01540-19. Print 2020 Jan 27.

3.

TBAJ-876 Retains Bedaquiline's Activity against Subunits c and ε of Mycobacterium tuberculosis F-ATP Synthase.

Sarathy JP, Ragunathan P, Shin J, Cooper CB, Upton AM, Grüber G, Dick T.

Antimicrob Agents Chemother. 2019 Sep 23;63(10). pii: e01191-19. doi: 10.1128/AAC.01191-19. Print 2019 Oct.

4.

Contribution of Pretomanid to Novel Regimens Containing Bedaquiline with either Linezolid or Moxifloxacin and Pyrazinamide in Murine Models of Tuberculosis.

Xu J, Li SY, Almeida DV, Tasneen R, Barnes-Boyle K, Converse PJ, Upton AM, Mdluli K, Fotouhi N, Nuermberger EL.

Antimicrob Agents Chemother. 2019 Apr 25;63(5). pii: e00021-19. doi: 10.1128/AAC.00021-19. Print 2019 May.

5.

3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.

Sutherland HS, Tong AST, Choi PJ, Blaser A, Conole D, Franzblau SG, Lotlikar MU, Cooper CB, Upton AM, Denny WA, Palmer BD.

Bioorg Med Chem. 2019 Apr 1;27(7):1292-1307. doi: 10.1016/j.bmc.2019.02.026. Epub 2019 Feb 15.

6.

Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.

Blaser A, Sutherland HS, Tong AST, Choi PJ, Conole D, Franzblau SG, Cooper CB, Upton AM, Lotlikar M, Denny WA, Palmer BD.

Bioorg Med Chem. 2019 Apr 1;27(7):1283-1291. doi: 10.1016/j.bmc.2019.02.025. Epub 2019 Feb 15.

7.

Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.

Sutherland HS, Tong AST, Choi PJ, Conole D, Blaser A, Franzblau SG, Cooper CB, Upton AM, Lotlikar MU, Denny WA, Palmer BD.

Bioorg Med Chem. 2018 May 1;26(8):1797-1809. doi: 10.1016/j.bmc.2018.02.026. Epub 2018 Feb 20.

8.

Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.

Choi PJ, Sutherland HS, Tong AST, Blaser A, Franzblau SG, Cooper CB, Lotlikar MU, Upton AM, Guillemont J, Motte M, Queguiner L, Andries K, Van den Broeck W, Denny WA, Palmer BD.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5190-5196. doi: 10.1016/j.bmcl.2017.10.042. Epub 2017 Oct 20.

9.

6-Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis.

Tong AST, Choi PJ, Blaser A, Sutherland HS, Tsang SKY, Guillemont J, Motte M, Cooper CB, Andries K, Van den Broeck W, Franzblau SG, Upton AM, Denny WA, Palmer BD, Conole D.

ACS Med Chem Lett. 2017 Sep 22;8(10):1019-1024. doi: 10.1021/acsmedchemlett.7b00196. eCollection 2017 Oct 12.

10.

Contribution of the nitroimidazoles PA-824 and TBA-354 to the activity of novel regimens in murine models of tuberculosis.

Tasneen R, Williams K, Amoabeng O, Minkowski A, Mdluli KE, Upton AM, Nuermberger EL.

Antimicrob Agents Chemother. 2015 Jan;59(1):129-35. doi: 10.1128/AAC.03822-14. Epub 2014 Oct 20.

11.

In vitro and in vivo activities of the nitroimidazole TBA-354 against Mycobacterium tuberculosis.

Upton AM, Cho S, Yang TJ, Kim Y, Wang Y, Lu Y, Wang B, Xu J, Mdluli K, Ma Z, Franzblau SG.

Antimicrob Agents Chemother. 2015 Jan;59(1):136-44. doi: 10.1128/AAC.03823-14. Epub 2014 Oct 20.

12.

Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents.

Hwang JM, Oh T, Kaneko T, Upton AM, Franzblau SG, Ma Z, Cho SN, Kim P.

J Nat Prod. 2013 Mar 22;76(3):354-67. doi: 10.1021/np3007167. Epub 2013 Jan 29.

PMID:
23360475
13.

Identification of less lipophilic riminophenazine derivatives for the treatment of drug-resistant tuberculosis.

Zhang D, Lu Y, Liu K, Liu B, Wang J, Zhang G, Zhang H, Liu Y, Wang B, Zheng M, Fu L, Hou Y, Gong N, Lv Y, Li C, Cooper CB, Upton AM, Yin D, Ma Z, Huang H.

J Med Chem. 2012 Oct 11;55(19):8409-17. doi: 10.1021/jm300828h. Epub 2012 Sep 20.

PMID:
22931472
14.

In vitro and in vivo activity of clofazimine against Mycobacterium tuberculosis persisters.

Xu J, Lu Y, Fu L, Zhu H, Wang B, Mdluli K, Upton AM, Jin H, Zheng M, Zhao W, Li P.

Int J Tuberc Lung Dis. 2012 Aug;16(8):1119-25. doi: 10.5588/ijtld.11.0752. Epub 2012 Jun 12.

PMID:
22691726
15.

Clofazimine analogs with efficacy against experimental tuberculosis and reduced potential for accumulation.

Lu Y, Zheng M, Wang B, Fu L, Zhao W, Li P, Xu J, Zhu H, Jin H, Yin D, Huang H, Upton AM, Ma Z.

Antimicrob Agents Chemother. 2011 Nov;55(11):5185-93. doi: 10.1128/AAC.00699-11. Epub 2011 Aug 15.

16.

Meta-analysis of randomized trials on first line and adjunctive levetiracetam.

Lo BW, Kyu HH, Jichici D, Upton AM, Akl EA, Meade MO.

Can J Neurol Sci. 2011 May;38(3):475-86. Review.

PMID:
21515509
17.

Role of the methylcitrate cycle in propionate metabolism and detoxification in Mycobacterium smegmatis.

Upton AM, McKinney JD.

Microbiology. 2007 Dec;153(Pt 12):3973-3982. doi: 10.1099/mic.0.2007/011726-0.

PMID:
18048912
18.

'Soothing the ring of fire': Australian women's and midwives' experiences of using perineal warm packs in the second stage of labour.

Dahlen HG, Homer CS, Cooke M, Upton AM, Nunn RA, Brodrick BS.

Midwifery. 2009 Apr;25(2):e39-48. Epub 2007 Nov 26.

PMID:
18031878
19.
20.

Role of the methylcitrate cycle in Mycobacterium tuberculosis metabolism, intracellular growth, and virulence.

Muñoz-Elías EJ, Upton AM, Cherian J, McKinney JD.

Mol Microbiol. 2006 Jun;60(5):1109-22.

21.

Arylamine N-acetyltransferase is required for synthesis of mycolic acids and complex lipids in Mycobacterium bovis BCG and represents a novel drug target.

Bhakta S, Besra GS, Upton AM, Parish T, Sholto-Douglas-Vernon C, Gibson KJ, Knutton S, Gordon S, DaSilva RP, Anderton MC, Sim E.

J Exp Med. 2004 May 3;199(9):1191-9. Epub 2004 Apr 26.

22.

Arylamine N-acetyltransferase of Mycobacterium tuberculosis is a polymorphic enzyme and a site of isoniazid metabolism.

Upton AM, Mushtaq A, Victor TC, Sampson SL, Sandy J, Smith DM, van Helden PV, Sim E.

Mol Microbiol. 2001 Oct;42(2):309-17.

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