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Items: 1 to 20 of 157

1.

4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.

Naik M, Humnabadkar V, Tantry SJ, Panda M, Narayan A, Guptha S, Panduga V, Manjrekar P, Jena LK, Koushik K, Shanbhag G, Jatheendranath S, Manjunatha MR, Gorai G, Bathula C, Rudrapatna S, Achar V, Sharma S, Ambady A, Hegde N, Mahadevaswamy J, Kaur P, Sambandamurthy VK, Awasthy D, Narayan C, Ravishankar S, Madhavapeddi P, Reddy J, Prabhakar K, Saralaya R, Chatterji M, Whiteaker J, McLaughlin B, Chiarelli LR, Riccardi G, Pasca MR, Binda C, Neres J, Dhar N, Signorino-Gelo F, McKinney JD, Ramachandran V, Shandil R, Tommasi R, Iyer PS, Narayanan S, Hosagrahara V, Kavanagh S, Dinesh N, Ghorpade SR.

J Med Chem. 2014 Jun 26;57(12):5419-34. doi: 10.1021/jm5005978. Epub 2014 Jun 11.

PMID:
24871036
2.

Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.

Panda M, Ramachandran S, Ramachandran V, Shirude PS, Humnabadkar V, Nagalapur K, Sharma S, Kaur P, Guptha S, Narayan A, Mahadevaswamy J, Ambady A, Hegde N, Rudrapatna SS, Hosagrahara VP, Sambandamurthy VK, Raichurkar A.

J Med Chem. 2014 Jun 12;57(11):4761-71. doi: 10.1021/jm5002937. Epub 2014 May 22.

PMID:
24818517
3.

Characterization of DprE1-Mediated Benzothiazinone Resistance in Mycobacterium tuberculosis.

Foo CS, Lechartier B, Kolly GS, Boy-Röttger S, Neres J, Rybniker J, Lupien A, Sala C, Piton J, Cole ST.

Antimicrob Agents Chemother. 2016 Oct 21;60(11):6451-6459. doi: 10.1128/AAC.01523-16. Print 2016 Nov.

4.

Lead optimization of 1,4-azaindoles as antimycobacterial agents.

Shirude PS, Shandil RK, Manjunatha MR, Sadler C, Panda M, Panduga V, Reddy J, Saralaya R, Nanduri R, Ambady A, Ravishankar S, Sambandamurthy VK, Humnabadkar V, Jena LK, Suresh RS, Srivastava A, Prabhakar KR, Whiteaker J, McLaughlin RE, Sharma S, Cooper CB, Mdluli K, Butler S, Iyer PS, Narayanan S, Chatterji M.

J Med Chem. 2014 Jul 10;57(13):5728-37. doi: 10.1021/jm500571f. Epub 2014 Jun 20.

PMID:
24874895
5.

Azaindoles: noncovalent DprE1 inhibitors from scaffold morphing efforts, kill Mycobacterium tuberculosis and are efficacious in vivo.

Shirude PS, Shandil R, Sadler C, Naik M, Hosagrahara V, Hameed S, Shinde V, Bathula C, Humnabadkar V, Kumar N, Reddy J, Panduga V, Sharma S, Ambady A, Hegde N, Whiteaker J, McLaughlin RE, Gardner H, Madhavapeddi P, Ramachandran V, Kaur P, Narayan A, Guptha S, Awasthy D, Narayan C, Mahadevaswamy J, Vishwas KG, Ahuja V, Srivastava A, Prabhakar KR, Bharath S, Kale R, Ramaiah M, Choudhury NR, Sambandamurthy VK, Solapure S, Iyer PS, Narayanan S, Chatterji M.

J Med Chem. 2013 Dec 12;56(23):9701-8. doi: 10.1021/jm401382v. Epub 2013 Nov 21.

PMID:
24215368
6.

2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1.

Neres J, Hartkoorn RC, Chiarelli LR, Gadupudi R, Pasca MR, Mori G, Venturelli A, Savina S, Makarov V, Kolly GS, Molteni E, Binda C, Dhar N, Ferrari S, Brodin P, Delorme V, Landry V, de Jesus Lopes Ribeiro AL, Farina D, Saxena P, Pojer F, Carta A, Luciani R, Porta A, Zanoni G, De Rossi E, Costi MP, Riccardi G, Cole ST.

ACS Chem Biol. 2015 Mar 20;10(3):705-14. doi: 10.1021/cb5007163. Epub 2014 Dec 9.

PMID:
25427196
7.

Identification and development of 2-methylimidazo[1,2-a]pyridine-3-carboxamides as Mycobacterium tuberculosis pantothenate synthetase inhibitors.

Samala G, Nallangi R, Devi PB, Saxena S, Yadav R, Sridevi JP, Yogeeswari P, Sriram D.

Bioorg Med Chem. 2014 Aug 1;22(15):4223-32. doi: 10.1016/j.bmc.2014.05.038. Epub 2014 May 23.

PMID:
24953948
8.

Investigating the structural basis of arylamides to improve potency against M. tuberculosis strain through molecular dynamics simulations.

Punkvang A, Saparpakorn P, Hannongbua S, Wolschann P, Beyer A, Pungpo P.

Eur J Med Chem. 2010 Dec;45(12):5585-93. doi: 10.1016/j.ejmech.2010.09.008. Epub 2010 Sep 17.

PMID:
20888672
9.

Discovery of benzothiazoles as antimycobacterial agents: Synthesis, structure-activity relationships and binding studies with Mycobacterium tuberculosis decaprenylphosphoryl-β-D-ribose 2'-oxidase.

Landge S, Mullick AB, Nagalapur K, Neres J, Subbulakshmi V, Murugan K, Ghosh A, Sadler C, Fellows MD, Humnabadkar V, Mahadevaswamy J, Vachaspati P, Sharma S, Kaur P, Mallya M, Rudrapatna S, Awasthy D, Sambandamurthy VK, Pojer F, Cole ST, Balganesh TS, Ugarkar BG, Balasubramanian V, Bandodkar BS, Panda M, Ramachandran V.

Bioorg Med Chem. 2015 Dec 15;23(24):7694-710. doi: 10.1016/j.bmc.2015.11.017. Epub 2015 Nov 18.

PMID:
26643218
10.

Benzothiazinones are suicide inhibitors of mycobacterial decaprenylphosphoryl-β-D-ribofuranose 2'-oxidase DprE1.

Trefzer C, Škovierová H, Buroni S, Bobovská A, Nenci S, Molteni E, Pojer F, Pasca MR, Makarov V, Cole ST, Riccardi G, Mikušová K, Johnsson K.

J Am Chem Soc. 2012 Jan 18;134(2):912-5. doi: 10.1021/ja211042r. Epub 2011 Dec 21.

PMID:
22188377
11.

The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis.

Makarov V, Neres J, Hartkoorn RC, Ryabova OB, Kazakova E, Šarkan M, Huszár S, Piton J, Kolly GS, Vocat A, Conroy TM, Mikušová K, Cole ST.

Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52. doi: 10.1128/AAC.00778-15. Epub 2015 May 18.

12.

Development of selective DprE1 inhibitors: Design, synthesis, crystal structure and antitubercular activity of benzothiazolylpyrimidine-5-carboxamides.

Chikhale R, Menghani S, Babu R, Bansode R, Bhargavi G, Karodia N, Rajasekharan MV, Paradkar A, Khedekar P.

Eur J Med Chem. 2015;96:30-46. doi: 10.1016/j.ejmech.2015.04.011. Epub 2015 Apr 7.

PMID:
25874329
13.

Development of benzo[d]oxazol-2(3H)-ones derivatives as novel inhibitors of Mycobacterium tuberculosis InhA.

Pedgaonkar GS, Sridevi JP, Jeankumar VU, Saxena S, Devi PB, Renuka J, Yogeeswari P, Sriram D.

Bioorg Med Chem. 2014 Nov 1;22(21):6134-45. doi: 10.1016/j.bmc.2014.08.031. Epub 2014 Sep 4.

PMID:
25282650
14.

Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.

Hameed P S, Patil V, Solapure S, Sharma U, Madhavapeddi P, Raichurkar A, Chinnapattu M, Manjrekar P, Shanbhag G, Puttur J, Shinde V, Menasinakai S, Rudrapatana S, Achar V, Awasthy D, Nandishaiah R, Humnabadkar V, Ghosh A, Narayan C, Ramya VK, Kaur P, Sharma S, Werngren J, Hoffner S, Panduga V, Kumar CN, Reddy J, Kumar K N M, Ganguly S, Bharath S, Bheemarao U, Mukherjee K, Arora U, Gaonkar S, Coulson M, Waterson D, Sambandamurthy VK, de Sousa SM.

J Med Chem. 2014 Jun 12;57(11):4889-905. doi: 10.1021/jm500432n. Epub 2014 May 23.

PMID:
24809953
15.

Identification of a novel inhibitor of isocitrate lyase as a potent antitubercular agent against both active and non-replicating Mycobacterium tuberculosis.

Liu Y, Zhou S, Deng Q, Li X, Meng J, Guan Y, Li C, Xiao C.

Tuberculosis (Edinb). 2016 Mar;97:38-46. doi: 10.1016/j.tube.2015.12.003. Epub 2016 Jan 6.

PMID:
26980494
16.

Biological evaluation of potent triclosan-derived inhibitors of the enoyl-acyl carrier protein reductase InhA in drug-sensitive and drug-resistant strains of Mycobacterium tuberculosis.

Stec J, Vilchèze C, Lun S, Perryman AL, Wang X, Freundlich JS, Bishai W, Jacobs WR Jr, Kozikowski AP.

ChemMedChem. 2014 Nov;9(11):2528-37. doi: 10.1002/cmdc.201402255. Epub 2014 Aug 27.

17.

Development of ssDNA aptamers as potent inhibitors of Mycobacterium tuberculosis acetohydroxyacid synthase.

Baig IA, Moon JY, Lee SC, Ryoo SW, Yoon MY.

Biochim Biophys Acta. 2015 Oct;1854(10 Pt A):1338-50. doi: 10.1016/j.bbapap.2015.05.003. Epub 2015 May 16.

PMID:
25988243
18.

Novel amide and sulphonamide derivatives of 6-(piperazin-1-yl)phenanthridine as potent Mycobacterium tuberculosis H37Rv inhibitors.

Naidu KM, Nagesh HN, Singh M, Sriram D, Yogeeswari P, Gowri Chandra Sekhar KV.

Eur J Med Chem. 2015 Mar 6;92:415-26. doi: 10.1016/j.ejmech.2015.01.013. Epub 2015 Jan 9.

PMID:
25590862
19.

DprE1--from the discovery to the promising tuberculosis drug target.

Mikusová K, Makarov V, Neres J.

Curr Pharm Des. 2014;20(27):4379-403. Review.

PMID:
24245764
20.

Whole cell screen based identification of spiropiperidines with potent antitubercular properties.

Tantry SJ, Degiacomi G, Sharma S, Jena LK, Narayan A, Guptha S, Shanbhag G, Menasinakai S, Mallya M, Awasthy D, Balakrishnan G, Kaur P, Bhattacharjee D, Narayan C, Reddy J, Naveen Kumar CN, Shandil R, Boldrin F, Ventura M, Manganelli R, Hartkoorn RC, Cole ST, Panda M, Markad SD, Ramachandran V, Ghorpade SR, Dinesh N.

Bioorg Med Chem Lett. 2015 Aug 15;25(16):3234-45. doi: 10.1016/j.bmcl.2015.05.087. Epub 2015 Jun 3.

PMID:
26087937

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