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Showing 25 to 36 of 87 entries
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Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents.

ACS medicinal chemistry letters

Lv K, You X, Wang B, Wei Z, Chai Y, Wang B, Wang A, Huang G, Liu M, Lu Y.
PMID: 28626525
ACS Med Chem Lett. 2017 May 10;8(6):636-641. doi: 10.1021/acsmedchemlett.7b00106. eCollection 2017 Jun 08.

A series of new 8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one(BTZ) derivatives containing a C-2 nitrogen spiro-heterocycle moiety based on the structures of BTZ candidates BTZ043 and PBTZ169 were designed and synthesized as new antitubercular agents. Many of them were found to have excellent

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Lv K, You X, Wang B, et al. Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents. ACS Med Chem Lett. 2017;8(6):636-641doi: 10.1021/acsmedchemlett.7b00106.
Lv, K., You, X., Wang, B., Wei, Z., Chai, Y., Wang, B., Wang, A., Huang, G., Liu, M., & Lu, Y. (2017). Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents. ACS medicinal chemistry letters, 8(6), 636-641. https://doi.org/10.1021/acsmedchemlett.7b00106
Lv, Kai, et al. "Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents." ACS medicinal chemistry letters vol. 8,6 (2017): 636-641. doi: https://doi.org/10.1021/acsmedchemlett.7b00106
Lv K, You X, Wang B, Wei Z, Chai Y, Wang B, Wang A, Huang G, Liu M, Lu Y. Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents. ACS Med Chem Lett. 2017 May 10;8(6):636-641. doi: 10.1021/acsmedchemlett.7b00106. eCollection 2017 Jun 08. PMID: 28626525; PMCID: PMC5467196.
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The conserved Lysine69 residue plays a catalytic role in Mycobacterium tuberculosis shikimate dehydrogenase.

BMC research notes

Rodrigues VS, Breda A, Santos DS, Basso LA.
PMID: 19917104
BMC Res Notes. 2009 Nov 16;2:227. doi: 10.1186/1756-0500-2-227.

BACKGROUND: The shikimate pathway is an attractive target for the development of antitubercular agents because it is essential in Mycobacterium tuberculosis, the causative agent of tuberculosis, but absent in humans. M. tuberculosis aroE-encoded shikimate dehydrogenase catalyzes the forth reaction...

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Rodrigues VS, Breda A, Santos DS, et al. The conserved Lysine69 residue plays a catalytic role in Mycobacterium tuberculosis shikimate dehydrogenase. BMC Res Notes. 2009;2:227doi: 10.1186/1756-0500-2-227.
Rodrigues, V. S., Breda, A., Santos, D. S., & Basso, L. A. (2009). The conserved Lysine69 residue plays a catalytic role in Mycobacterium tuberculosis shikimate dehydrogenase. BMC research notes, 2227. https://doi.org/10.1186/1756-0500-2-227
Rodrigues, Valnês S, et al. "The conserved Lysine69 residue plays a catalytic role in Mycobacterium tuberculosis shikimate dehydrogenase." BMC research notes vol. 2 (2009): 227. doi: https://doi.org/10.1186/1756-0500-2-227
Rodrigues VS, Breda A, Santos DS, Basso LA. The conserved Lysine69 residue plays a catalytic role in Mycobacterium tuberculosis shikimate dehydrogenase. BMC Res Notes. 2009 Nov 16;2:227. doi: 10.1186/1756-0500-2-227. PMID: 19917104; PMCID: PMC2789096.
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Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis.

ACS medicinal chemistry letters

Zhao H, Lu Y, Sheng L, Yuan Z, Wang B, Wang W, Li Y, Ma C, Wang X, Zhang D, Huang H.
PMID: 28523106
ACS Med Chem Lett. 2017 Apr 12;8(5):533-537. doi: 10.1021/acsmedchemlett.7b00068. eCollection 2017 May 11.

A novel series of fluorine-containing benzoxazinyl-oxazolidinones were designed and synthesized as antidrug-resistant tuberculosis agents possessing good activity and improved pharmacokinetic profiles. Compound

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Zhao H, Lu Y, Sheng L, et al. Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis. ACS Med Chem Lett. 2017;8(5):533-537doi: 10.1021/acsmedchemlett.7b00068.
Zhao, H., Lu, Y., Sheng, L., Yuan, Z., Wang, B., Wang, W., Li, Y., Ma, C., Wang, X., Zhang, D., & Huang, H. (2017). Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis. ACS medicinal chemistry letters, 8(5), 533-537. https://doi.org/10.1021/acsmedchemlett.7b00068
Zhao, Hongyi, et al. "Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis." ACS medicinal chemistry letters vol. 8,5 (2017): 533-537. doi: https://doi.org/10.1021/acsmedchemlett.7b00068
Zhao H, Lu Y, Sheng L, Yuan Z, Wang B, Wang W, Li Y, Ma C, Wang X, Zhang D, Huang H. Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis. ACS Med Chem Lett. 2017 Apr 12;8(5):533-537. doi: 10.1021/acsmedchemlett.7b00068. eCollection 2017 May 11. PMID: 28523106; PMCID: PMC5430409.
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Respiratory review of 2014: tuberculosis and nontuberculous mycobacterial pulmonary disease.

Tuberculosis and respiratory diseases

Park CK, Kwon YS.
PMID: 25368661
Tuberc Respir Dis (Seoul). 2014 Oct;77(4):161-6. doi: 10.4046/trd.2014.77.4.161. Epub 2014 Oct 31.

Since tuberculosis (TB) remains a major global health concern and the incidence of multi-drug resistant (MDR)-TB is increasing globally, new modalities for the detection of TB and drug resistant TB are needed to improve TB control. The Xpert MTB/RIF...

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Park CK, Kwon YS. Respiratory review of 2014: tuberculosis and nontuberculous mycobacterial pulmonary disease. Tuberc Respir Dis (Seoul). 2014;77(4):161-6doi: 10.4046/trd.2014.77.4.161.
Park, C. K., & Kwon, Y. S. (2014). Respiratory review of 2014: tuberculosis and nontuberculous mycobacterial pulmonary disease. Tuberculosis and respiratory diseases, 77(4), 161-6. https://doi.org/10.4046/trd.2014.77.4.161
Park, Cheol Kyu, and Kwon, Yong Soo. "Respiratory review of 2014: tuberculosis and nontuberculous mycobacterial pulmonary disease." Tuberculosis and respiratory diseases vol. 77,4 (2014): 161-6. doi: https://doi.org/10.4046/trd.2014.77.4.161
Park CK, Kwon YS. Respiratory review of 2014: tuberculosis and nontuberculous mycobacterial pulmonary disease. Tuberc Respir Dis (Seoul). 2014 Oct;77(4):161-6. doi: 10.4046/trd.2014.77.4.161. Epub 2014 Oct 31. PMID: 25368661; PMCID: PMC4217031.
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Treatment of Drug Susceptible Pulmonary Tuberculosis.

Tuberculosis and respiratory diseases

Shin HJ, Kwon YS.
PMID: 26175767
Tuberc Respir Dis (Seoul). 2015 Jul;78(3):161-7. doi: 10.4046/trd.2015.78.3.161. Epub 2015 Jun 30.

Tuberculosis (TB) remains a major global health problem, and the incidence of TB cases has not significantly decreased over the past decade in Korea. The standard short course regimen is highly effective against TB, but requires multiple TB-specific drugs...

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Shin HJ, Kwon YS. Treatment of Drug Susceptible Pulmonary Tuberculosis. Tuberc Respir Dis (Seoul). 2015;78(3):161-7doi: 10.4046/trd.2015.78.3.161.
Shin, H. J., & Kwon, Y. S. (2015). Treatment of Drug Susceptible Pulmonary Tuberculosis. Tuberculosis and respiratory diseases, 78(3), 161-7. https://doi.org/10.4046/trd.2015.78.3.161
Shin, Hong-Joon, and Kwon, Yong-Soo. "Treatment of Drug Susceptible Pulmonary Tuberculosis." Tuberculosis and respiratory diseases vol. 78,3 (2015): 161-7. doi: https://doi.org/10.4046/trd.2015.78.3.161
Shin HJ, Kwon YS. Treatment of Drug Susceptible Pulmonary Tuberculosis. Tuberc Respir Dis (Seoul). 2015 Jul;78(3):161-7. doi: 10.4046/trd.2015.78.3.161. Epub 2015 Jun 30. PMID: 26175767; PMCID: PMC4499581.
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Selective Mycobacterium tuberculosis Shikimate Kinase Inhibitors as Potential Antibacterials.

Perspectives in medicinal chemistry

Gordon S, Simithy J, Goodwin DC, Calderón AI.
PMID: 25861218
Perspect Medicin Chem. 2015 Mar 15;7:9-20. doi: 10.4137/PMC.S13212. eCollection 2015.

Owing to the persistence of tuberculosis (TB) as well as the emergence of multidrug-resistant and extensively drug-resistant (XDR) forms of the disease, the development of new antitubercular drugs is crucial. Developing inhibitors of shikimate kinase (SK) in the shikimate...

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Gordon S, Simithy J, Goodwin DC, et al. Selective Mycobacterium tuberculosis Shikimate Kinase Inhibitors as Potential Antibacterials. Perspect Medicin Chem. 2015;7:9-20doi: 10.4137/PMC.S13212.
Gordon, S., Simithy, J., Goodwin, D. C., & Calderón, A. I. (2015). Selective Mycobacterium tuberculosis Shikimate Kinase Inhibitors as Potential Antibacterials. Perspectives in medicinal chemistry, 79-20. https://doi.org/10.4137/PMC.S13212
Gordon, Sara, et al. "Selective Mycobacterium tuberculosis Shikimate Kinase Inhibitors as Potential Antibacterials." Perspectives in medicinal chemistry vol. 7 (2015): 9-20. doi: https://doi.org/10.4137/PMC.S13212
Gordon S, Simithy J, Goodwin DC, Calderón AI. Selective Mycobacterium tuberculosis Shikimate Kinase Inhibitors as Potential Antibacterials. Perspect Medicin Chem. 2015 Mar 15;7:9-20. doi: 10.4137/PMC.S13212. eCollection 2015. PMID: 25861218; PMCID: PMC4362912.
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Structure-activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting .

RSC medicinal chemistry

Haranahalli K, Tong S, Kim S, Awwa M, Chen L, Knudson SE, Slayden RA, Singleton E, Russo R, Connell N, Ojima I.
PMID: 34046600
RSC Med Chem. 2020 Oct 16;12(1):78-94. doi: 10.1039/d0md00256a. eCollection 2021 Jan 01.

Filamenting temperature sensitive protein Z (FtsZ) is an essential bacterial cell division protein and a promising target for the development of new antibacterial therapeutics. As a part of our ongoing SAR studies on 2,5,6-trisubstituted benzimidazoles as antitubercular agents targeting

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Haranahalli K, Tong S, Kim S, et al. Structure-activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting . RSC Med Chem. 2020;12(1):78-94doi: 10.1039/d0md00256a.
Haranahalli, K., Tong, S., Kim, S., Awwa, M., Chen, L., Knudson, S. E., Slayden, R. A., Singleton, E., Russo, R., Connell, N., & Ojima, I. (2021). Structure-activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting . RSC medicinal chemistry, 12(1), 78-94. https://doi.org/10.1039/d0md00256a
Haranahalli, Krupanandan, et al. "Structure-activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting ." RSC medicinal chemistry vol. 12,1 (2021): 78-94. doi: https://doi.org/10.1039/d0md00256a
Haranahalli K, Tong S, Kim S, Awwa M, Chen L, Knudson SE, Slayden RA, Singleton E, Russo R, Connell N, Ojima I. Structure-activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting . RSC Med Chem. 2020 Oct 16;12(1):78-94. doi: 10.1039/d0md00256a. eCollection 2021 Jan 01. PMID: 34046600; PMCID: PMC8132993.
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Paradoxical Deterioration During Anti-Tuberculous Therapy in Non-HIV-Infected Patients with Pleural Tuberculosis: A Pragmatic Approach.

European journal of case reports in internal medicine

Corral-Gudino L, Rivas-Lamazares A, González-Fernández A, Hernando-García JC.
PMID: 30755892
Eur J Case Rep Intern Med. 2016 Aug 30;3(6):000475. doi: 10.12890/2016_000475. eCollection 2016.

We report a case of paradoxical deterioration. A male patient diagnosed with pleural tuberculosis, but who was not infected with human immunodeficiency virus (HIV), experienced clinical deterioration 3 weeks after the initiation of anti-tuberculous treatment. After other diagnoses were...

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Corral-Gudino L, Rivas-Lamazares A, González-Fernández A, et al. Paradoxical Deterioration During Anti-Tuberculous Therapy in Non-HIV-Infected Patients with Pleural Tuberculosis: A Pragmatic Approach. Eur J Case Rep Intern Med. 2016;3(6):000475doi: 10.12890/2016_000475.
Corral-Gudino, L., Rivas-Lamazares, A., González-Fernández, A., & Hernando-García, J. C. (2016). Paradoxical Deterioration During Anti-Tuberculous Therapy in Non-HIV-Infected Patients with Pleural Tuberculosis: A Pragmatic Approach. European journal of case reports in internal medicine, 3(6), 000475. https://doi.org/10.12890/2016_000475
Corral-Gudino, Luis, et al. "Paradoxical Deterioration During Anti-Tuberculous Therapy in Non-HIV-Infected Patients with Pleural Tuberculosis: A Pragmatic Approach." European journal of case reports in internal medicine vol. 3,6 (2016): 000475. doi: https://doi.org/10.12890/2016_000475
Corral-Gudino L, Rivas-Lamazares A, González-Fernández A, Hernando-García JC. Paradoxical Deterioration During Anti-Tuberculous Therapy in Non-HIV-Infected Patients with Pleural Tuberculosis: A Pragmatic Approach. Eur J Case Rep Intern Med. 2016 Aug 30;3(6):000475. doi: 10.12890/2016_000475. eCollection 2016. PMID: 30755892; PMCID: PMC6346842.
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Synthesis and evaluation of antimicrobial, antitubercular and anticancer activities of 2-(1-benzoyl-1H-benzo[d]imidazol-2-ylthio)-N-substituted acetamides.

Chemistry Central journal

Yadav S, Lim SM, Ramasamy K, Vasudevan M, Shah SAA, Mathur A, Narasimhan B.
PMID: 29804151
Chem Cent J. 2018 May 26;12(1):66. doi: 10.1186/s13065-018-0432-3.

BACKGROUND: The study describes the synthesis, characterization, in vitro antimicrobial and anticancer evaluation of a series of 2-(1-benzoyl-1H-benzo[d]imidazol-2-ylthio)-N-substituted acetamide derivatives. The synthesized derivatives were also assessed for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv. The compounds found active...

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Yadav S, Lim SM, Ramasamy K, et al. Synthesis and evaluation of antimicrobial, antitubercular and anticancer activities of 2-(1-benzoyl-1H-benzo[d]imidazol-2-ylthio)-N-substituted acetamides. Chem Cent J. 2018;12(1):66doi: 10.1186/s13065-018-0432-3.
Yadav, S., Lim, S. M., Ramasamy, K., Vasudevan, M., Shah, S. A. A., Mathur, A., & Narasimhan, B. (2018). Synthesis and evaluation of antimicrobial, antitubercular and anticancer activities of 2-(1-benzoyl-1H-benzo[d]imidazol-2-ylthio)-N-substituted acetamides. Chemistry Central journal, 12(1), 66. https://doi.org/10.1186/s13065-018-0432-3
Yadav, Snehlata, et al. "Synthesis and evaluation of antimicrobial, antitubercular and anticancer activities of 2-(1-benzoyl-1H-benzo[d]imidazol-2-ylthio)-N-substituted acetamides." Chemistry Central journal vol. 12,1 (2018): 66. doi: https://doi.org/10.1186/s13065-018-0432-3
Yadav S, Lim SM, Ramasamy K, Vasudevan M, Shah SAA, Mathur A, Narasimhan B. Synthesis and evaluation of antimicrobial, antitubercular and anticancer activities of 2-(1-benzoyl-1H-benzo[d]imidazol-2-ylthio)-N-substituted acetamides. Chem Cent J. 2018 May 26;12(1):66. doi: 10.1186/s13065-018-0432-3. PMID: 29804151; PMCID: PMC5971037.
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Culture conversion at six months in patients receiving bedaquiline- and delamanid-containing regimens for the treatment of multidrug-resistant tuberculosis.

International journal of infectious diseases : IJID : official publication of the International Society for Infectious Diseases

Maretbayeva SM, Rakisheva AS, Adenov MM, Yeraliyeva LT, Algozhin YZ, Stambekova AT, Berikova EA, Yedilbayev A, Rich ML, Seung KJ, Issayeva AM.
PMID: 33823277
Int J Infect Dis. 2021 Dec;113:S91-S95. doi: 10.1016/j.ijid.2021.03.075. Epub 2021 Apr 03.

Rifampicin-resistant/multidrug-resistant (RR/MDR) and extensively drug-resistant (XDR) strains of M. tuberculosis (TB) are serious public health problem in Kazakhstan. In 2012 and 2013, stringent regulatory authorities approved the first new TB drugs in fifty years, bedaquiline and delamanid, offering hope...

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Maretbayeva SM, Rakisheva AS, Adenov MM, et al. Culture conversion at six months in patients receiving bedaquiline- and delamanid-containing regimens for the treatment of multidrug-resistant tuberculosis. Int J Infect Dis. 2021;113:S91-S95doi: 10.1016/j.ijid.2021.03.075.
Maretbayeva, S. M., Rakisheva, A. S., Adenov, M. M., Yeraliyeva, L. T., Algozhin, Y. Z., Stambekova, A. T., Berikova, E. A., Yedilbayev, A., Rich, M. L., Seung, K. J., & Issayeva, A. M. (2021). Culture conversion at six months in patients receiving bedaquiline- and delamanid-containing regimens for the treatment of multidrug-resistant tuberculosis. International journal of infectious diseases : IJID : official publication of the International Society for Infectious Diseases, 113S91-S95. https://doi.org/10.1016/j.ijid.2021.03.075
Maretbayeva, Shynar M, et al. "Culture conversion at six months in patients receiving bedaquiline- and delamanid-containing regimens for the treatment of multidrug-resistant tuberculosis." International journal of infectious diseases : IJID : official publication of the International Society for Infectious Diseases vol. 113 (2021): S91-S95. doi: https://doi.org/10.1016/j.ijid.2021.03.075
Maretbayeva SM, Rakisheva AS, Adenov MM, Yeraliyeva LT, Algozhin YZ, Stambekova AT, Berikova EA, Yedilbayev A, Rich ML, Seung KJ, Issayeva AM. Culture conversion at six months in patients receiving bedaquiline- and delamanid-containing regimens for the treatment of multidrug-resistant tuberculosis. Int J Infect Dis. 2021 Dec;113:S91-S95. doi: 10.1016/j.ijid.2021.03.075. Epub 2021 Apr 03. PMID: 33823277.
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Structural and Activity Relationships of 6-Sulfonyl-8-Nitrobenzothiazinones as Antitubercular Agents.

Journal of medicinal chemistry

Fan D, Wang B, Stelitano G, Savková K, Shi R, Huszár S, Han Q, Mikušová K, Chiarelli LR, Lu Y, Qiao C.
PMID: 34609861
J Med Chem. 2021 Oct 14;64(19):14526-14539. doi: 10.1021/acs.jmedchem.1c01049. Epub 2021 Oct 05.

The benzothiazinone (BTZ) scaffold compound PBTZ169 kills

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Fan D, Wang B, Stelitano G, et al. Structural and Activity Relationships of 6-Sulfonyl-8-Nitrobenzothiazinones as Antitubercular Agents. J Med Chem. 2021;64(19):14526-14539doi: 10.1021/acs.jmedchem.1c01049.
Fan, D., Wang, B., Stelitano, G., Savková, K., Shi, R., Huszár, S., Han, Q., Mikušová, K., Chiarelli, L. R., Lu, Y., & Qiao, C. (2021). Structural and Activity Relationships of 6-Sulfonyl-8-Nitrobenzothiazinones as Antitubercular Agents. Journal of medicinal chemistry, 64(19), 14526-14539. https://doi.org/10.1021/acs.jmedchem.1c01049
Fan, Dongguang, et al. "Structural and Activity Relationships of 6-Sulfonyl-8-Nitrobenzothiazinones as Antitubercular Agents." Journal of medicinal chemistry vol. 64,19 (2021): 14526-14539. doi: https://doi.org/10.1021/acs.jmedchem.1c01049
Fan D, Wang B, Stelitano G, Savková K, Shi R, Huszár S, Han Q, Mikušová K, Chiarelli LR, Lu Y, Qiao C. Structural and Activity Relationships of 6-Sulfonyl-8-Nitrobenzothiazinones as Antitubercular Agents. J Med Chem. 2021 Oct 14;64(19):14526-14539. doi: 10.1021/acs.jmedchem.1c01049. Epub 2021 Oct 05. PMID: 34609861.
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Novel candidates in the clinical development pipeline for TB drug development and their synthetic approaches.

Chemical biology & drug design

Kumar A, Karkara BB, Panda G.
PMID: 34397161
Chem Biol Drug Des. 2021 Nov;98(5):787-827. doi: 10.1111/cbdd.13934. Epub 2021 Sep 16.

Tuberculosis (TB) is an infection caused by Mycobacterium tuberculosis (Mtb) and one of the deadliest infectious diseases in the world. Mtb has the ability to become dormant within the host and to develop resistance. Hence, new antitubercular agents are...

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Kumar A, Karkara BB, Panda G. Novel candidates in the clinical development pipeline for TB drug development and their synthetic approaches. Chem Biol Drug Des. 2021;98(5):787-827doi: 10.1111/cbdd.13934.
Kumar, A., Karkara, B. B., & Panda, G. (2021). Novel candidates in the clinical development pipeline for TB drug development and their synthetic approaches. Chemical biology & drug design, 98(5), 787-827. https://doi.org/10.1111/cbdd.13934
Kumar, Amit, et al. "Novel candidates in the clinical development pipeline for TB drug development and their synthetic approaches." Chemical biology & drug design vol. 98,5 (2021): 787-827. doi: https://doi.org/10.1111/cbdd.13934
Kumar A, Karkara BB, Panda G. Novel candidates in the clinical development pipeline for TB drug development and their synthetic approaches. Chem Biol Drug Des. 2021 Nov;98(5):787-827. doi: 10.1111/cbdd.13934. Epub 2021 Sep 16. PMID: 34397161.
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