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Publikationer i urvalet

50 träffar

Bibliografisk träff 2016-03-08

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.

Thompson AM, O'Connor PD, Blaser A, Yardley V, Maes L, Gupta S, Launay D, Martin D, Franzblau SG, Wan B, Wang Y, Ma Z, Denny WA.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.5b01699

Bibliografisk träff 2015-12-07

Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids.

Rakesh, Bruhn DF, Scherman MS, Singh AP, Yang L, Liu J, Lenaerts AJ, Lee RE.

Bioorg Med Chem Lett · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2015.12.002

Bibliografisk träff 2015-10-14

Structure activity relationships of 4-hydroxy-2-pyridones: A novel class of antituberculosis agents.

Ng PS, Manjunatha UH, Rao SP, Camacho LR, Ma NL, Herve M, Noble CG, Goh A, Peukert S, Diagana TT, Smith PW, Kondreddi RR.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2015.10.008

Bibliografisk träff 2015-07-28

Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy.

Thompson AM, Blaser A, Palmer BD, Franzblau SG, Wan B, Wang Y, Ma Z, Denny WA.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2015.07.084

Bibliografisk träff 2015-07-02

Synthesis and anti-tubercular activity of 2-nitroimidazooxazines with modification at the C-7 position as PA-824 analogs.

Kang YG, Park CY, Shin H, Singh R, Arora G, Yu CM, Lee IY.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2015.06.060

Bibliografisk träff 2015-03-20

Design and synthesis of novel anti-tuberculosis agents from the celecoxib pharmacophore.

Salunke SB, Azad AK, Kapuriya NP, Balada-Llasat JM, Pancholi P, Schlesinger LS, Chen CS.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2015.03.041

Bibliografisk träff 2015-01-28

A novel molecule with notable activity against multi-drug resistant tuberculosis.

Nair V, Okello MO, Mangu NK, Seo BI, Gund MG.

Bioorg Med Chem Lett · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2015.01.050

Bibliografisk träff 2014-08-27

SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.

Poce G, Cocozza M, Consalvi S, Biava M.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2014.08.066

Bibliografisk träff 2014-06-02

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.

Karabanovich G, Roh J, Smutný T, Němeček J, Vicherek P, Stolaříková J, Vejsová M, Dufková I, Vávrová K, Pávek P, Klimešová V, Hrabálek A.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2014.05.069

Bibliografisk träff 2014-05-28

Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.

Moraski GC, Oliver AG, Markley LD, Cho S, Franzblau SG, Miller MJ.

Bioorg Med Chem Lett · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2014.05.062

Bibliografisk träff 2013-11-13

Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents.

Pieroni M, Wan B, Cho S, Franzblau SG, Costantino G.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2013.11.007

Bibliografisk träff 2013-10-02

Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis.

Hwang CH, Jaki BU, Klein LL, Lankin DC, McAlpine JB, Napolitano JG, Fryling NA, Franzblau SG, Cho SH, Stamets PE, Wang Y, Pauli GF.

J Nat Prod · research-article; journal article · DOI 10.1021/np400497f

Bibliografisk träff 2013-07-12

A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.

Dartois V, Barry CE.

Bioorg Med Chem Lett · research support, n.i.h., intramural; research support, non-u.s. gov't; research-article; review; journal article · DOI 10.1016/j.bmcl.2013.07.006

Bibliografisk träff 2013-07-01

Advancement of Imidazo[1,2-<i>a</i>]pyridines with Improved Pharmacokinetics and Nanomolar Activity Against <i>Mycobacterium tuberculosis.</i>

Moraski GC, Markley LD, Cramer J, Hipskind PA, Boshoff H, Bailey M, Alling T, Ollinger J, Parish T, Miller MJ.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml400088y

Bibliografisk träff 2013-05-03

Preliminary structure-activity relationships and biological evaluation of novel antitubercular indolecarboxamide derivatives against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.

Onajole OK, Pieroni M, Tipparaju SK, Lun S, Stec J, Chen G, Gunosewoyo H, Guo H, Ammerman NC, Bishai WR, Kozikowski AP.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm4003878

Bibliografisk träff 2012-09-07

The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives.

Tukulula M, Little S, Gut J, Rosenthal PJ, Wan B, Franzblau SG, Chibale K.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2012.08.047

Bibliografisk träff 2012-04-05

Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.

Gill SK, Xu H, Kirchhoff PD, Cierpicki T, Turbiak AJ, Wan B, Zhang N, Peng KW, Franzblau SG, Garcia GA, Showalter HD.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm201716n

Bibliografisk träff 2012-02-25

Tuberculosis: the drug development pipeline at a glance.

Villemagne B, Crauste C, Flipo M, Baulard AR, Déprez B, Willand N.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2012.02.033

Bibliografisk träff 2012-02-16

Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds.

Moraski GC, Markley LD, Chang M, Cho S, Franzblau SG, Hwang CH, Boshoff H, Miller MJ.

Bioorg Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmc.2012.02.025

Bibliografisk träff 2012-01-12

Synthesis and evaluation of anti-tubercular and antibacterial activities of new 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives. Part 2.

Lu X, Liu X, Wan B, Franzblau SG, Chen L, Zhou C, You Q.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2012.01.007

Bibliografisk träff 2011-12-29

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, Palmer BD, Sutherland HS, Kmentova I, Franzblau SG, Wan B, Wang Y, Ma Z, Thompson AM, Denny WA.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm2012276

Bibliografisk träff 2011-09-01

Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824).

Thompson AM, Sutherland HS, Palmer BD, Kmentova I, Blaser A, Franzblau SG, Wan B, Wang Y, Ma Z, Denny WA.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm200377r

Bibliografisk träff 2011-08-19

Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.

Jin Y, Gill SK, Kirchhoff PD, Wan B, Franzblau SG, Garcia GA, Showalter HD.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2011.08.054

Bibliografisk träff 2011-07-26

Structure-activity relationships of antitubercular nitroimidazoles. 3. Exploration of the linker and lipophilic tail of ((s)-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)-(4-trifluoromethoxybenzyl)amine (6-amino PA-824).

Cherian J, Choi I, Nayyar A, Manjunatha UH, Mukherjee T, Lee YS, Boshoff HI, Singh R, Ha YH, Goodwin M, Lakshminarayana SB, Niyomrattanakit P, Jiricek J, Ravindran S, Dick T, Keller TH, Dartois V, Barry CE.

J Med Chem · research support, n.i.h., intramural; research support, non-u.s. gov't; research-article; journal article · DOI 10.1021/jm1010644

Bibliografisk träff 2011-06-01

Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.

Moraski GC, Markley LD, Hipskind PA, Boshoff H, Cho S, Franzblau SG, Miller MJ.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml200036r

Bibliografisk träff 2011-04-20

Synthesis and antimycobacterial activities of non-purine analogs of 6-aryl-9-benzylpurines: Imidazopyridines, pyrrolopyridines, benzimidazoles, and indoles.

Khoje AD, Charnock C, Wan B, Franzblau S, Gundersen LL.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2011.04.023

Bibliografisk träff 2011-03-15

Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity.

Singh K, Singh K, Wan B, Franzblau S, Chibale K, Balzarini J.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2011.03.010

Bibliografisk träff 2011-03-02

Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents.

Hans RH, Wiid IJ, van Helden PD, Wan B, Franzblau SG, Gut J, Rosenthal PJ, Chibale K.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2011.02.008

Bibliografisk träff 2011-01-05

Synthesis and antitubercular activity of monocyclic nitroimidazoles: insights from econazole.

Lee SH, Kim S, Yun MH, Lee YS, Cho SN, Oh T, Kim P.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2010.12.128

Bibliografisk träff 2010-11-25

The effect of 5-substitution on the electrochemical behavior and antitubercular activity of PA-824.

Bollo S, Núñez-Vergara LJ, Kang S, Zhang L, Boshoff HI, Barry CE, Squella JA, Dowd CS.

Bioorg Med Chem Lett · research support, n.i.h., intramural; research support, non-u.s. gov't; research-article; journal article · DOI 10.1016/j.bmcl.2010.11.093