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Showing 13 to 24 of 87 entries
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Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents.

Bioorganic & medicinal chemistry

Wang A, Xu S, Chai Y, Xia G, Wang B, Lv K, Wang D, Qin X, Jiang B, Wu W, Liu M, Lu Y.
PMID: 34861474
Bioorg Med Chem. 2021 Nov 25;53:116529. doi: 10.1016/j.bmc.2021.116529. Epub 2021 Nov 25.

Three series of novel nitrofuran-1,3,4-oxadiazole hybrids were designed and synthesized as new anti-TB agents. The structure activity relationship study indicated that the linkers and the substituents on the oxadiazole moiety greatly influence the activity, and the substituted benzenes are...

Synthesis, antitubercular, antimicrobial activities and molecular docking study of quinoline bearing dihydropyrimidines.

Bioorganic chemistry

Desai NC, Kotadiya GM, Jadeja KA, Shah KN, Malani AH, Manga V, Vani T.
PMID: 34329996
Bioorg Chem. 2021 Oct;115:105173. doi: 10.1016/j.bioorg.2021.105173. Epub 2021 Jul 15.

In order to develop the antimicrobial and antitubercular agents, we have derived quinoline bearing dihydropyrimidine analogues 5a-o and structures of these compounds were determined by spectroscopic techniques. Further, we have calculated the molecular properties prediction and drug-likeness by Molinspiration...

Increased diversity, fungal burden, and virulence of oral Candida spp. in patients undergoing anti-tuberculosis treatment.

Microbial pathogenesis

Orlandini RK, Rocha ACSD, Silva GA, Watanabe E, Motta ACF, Silva-Lovato CH, Oliveira VC, Bollela VR, Lourenço AG.
PMID: 34742893
Microb Pathog. 2021 Dec;161:105280. doi: 10.1016/j.micpath.2021.105280. Epub 2021 Nov 04.

Some studies have demonstrated a high prevalence of Candida species in patients with tuberculosis (TB). This is most likely due to long-term antimicrobial therapy. To date, no longitudinal studies addressed the effects of anti-TB treatment on the fungal burden...

A Comparative Study of 1D Descriptors Supported CoMFA and CoMSIA QSAR Models to Gain Novel Insights into 1,2,4-Triazoles Acting As Antitubercular Agents.

Current computer-aided drug design

Ray R, Shenoy GG, Kumar TNVG.
PMID: 32116196
Curr Comput Aided Drug Des. 2021;17(2):281-293. doi: 10.2174/1573409916666200302115432.

BACKGROUND: Tuberculosis is one of the leading causes of deaths due to infectious disease worldwide. There is an urgent need for developing new drugs due to the rising incidents of drug resistance. Previously, triazole molecules showing antitubercular activity, were...

Discovery of 5-methylpyrimidopyridone analogues as selective antimycobacterial agents.

Bioorganic & medicinal chemistry

Wu Y, Cheung CY, Zhou Y, Wang Z, Tu Z, Cook GM, Lu X.
PMID: 34624820
Bioorg Med Chem. 2021 Nov 01;49:116426. doi: 10.1016/j.bmc.2021.116426. Epub 2021 Sep 27.

With the emergence of multidrug-resistant strains of Mycobacterium tuberculosis (MDR-TB) and extensive drug-resistant strains (XDR-TB), there is an urgent need to develop novel drugs for the treatment of tuberculosis. Here, we designed and synthesized a series of 5-methylpyrimidopyridone analogues...

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

Deciphering the Structural Requirements of Nucleoside Bisubstrate Analogues for Inhibition of MbtA in Mycobacterium tuberculosis: A FB-QSAR Study and Combinatorial Library Generation for Identifying Potential Hits.

Molecular informatics

Maganti L, Das SK, Mascarenhas NM, Ghoshal N.
PMID: 27468106
Mol Inform. 2011 Oct;30(10):863-72. doi: 10.1002/minf.201100056. Epub 2011 Sep 07.

The re-emergence of tuberculosis infections, which are resistant to conventional drug therapy, has steadily risen in the last decade. Inhibitors of aryl acid adenylating enzyme known as MbtA, involved in siderophore biosynthesis in Mycobacterium tuberculosis, are being explored as...

Discovery of tetrahydropyrazolopyrimidine carboxamide derivatives as potent and orally active antitubercular agents.

ACS medicinal chemistry letters

Yokokawa F, Wang G, Chan WL, Ang SH, Wong J, Ma I, Rao SP, Manjunatha U, Lakshminarayana SB, Herve M, Kounde C, Tan BH, Thayalan P, Ng SH, Nanjundappa M, Ravindran S, Gee P, Tan M, Wei L, Goh A, Chen PY, Lee KS, Zhong C, Wagner T, Dix I, Chatterjee AK, Pethe K, Kuhen K, Glynne R, Smith P, Bifani P, Jiricek J.
PMID: 24900693
ACS Med Chem Lett. 2013 Apr 01;4(5):451-5. doi: 10.1021/ml400071a. eCollection 2013 May 09.

Tetrahydropyrazolo[1,5-a]pyrimidine scaffold was identified as a hit series from a Mycobacterium tuberculosis (Mtb) whole cell high through-put screening (HTS) campaign. A series of derivatives of this class were synthesized to evaluate their structure-activity relationship (SAR) and structure-property relationship (SPR)....

Design, Synthesis, Toxicity Estimation and Molecular Docking Studies of N-(furan-2-yl)-1-(5-substituted) phenyl-1,3,4-oxadiazol-2-yl) methanimine as Antitubercular Agents.

Indian journal of pharmaceutical sciences

Mathew B, Suresh J, Mathew GE, Sonia G, Krishnan GK.
PMID: 25425753
Indian J Pharm Sci. 2014 Sep;76(5):401-6.

A series of novel N-(furan-2-yl)-1-(5-substituted) phenyl-1,3,4-oxadiazol-2-yl) methanimines (Fa-e) were synthesized and evaluated for antitubercular activity against Mycobacterium tuberculosis (H37Rv) strain by using alamar blue assay. The synthesized compounds were characterized based on IR, (1)HMR and mass spectral analysis. The...

Screening of the antimycobacterial activity of novel lipophilic agents by the modified broth based method.

Journal of clinical tuberculosis and other mycobacterial diseases

Zandhaghighi M, Ghazvini K, Meshkat Z, Rezaee SA, Derakhshan M, Soleimanpour S, Hadizadeh F.
PMID: 31723679
J Clin Tuberc Other Mycobact Dis. 2016 Feb 11;3:1-5. doi: 10.1016/j.jctube.2016.01.001. eCollection 2016 May.

Most of the introduced susceptibility methods of

Design, Synthesis and Biological Evaluation of Some Triazole Schiff's Base Derivatives as Potential Antitubercular Agents.

The open medicinal chemistry journal

Sager AA, Abood ZS, El-Amary WM, Bensaber SM, Al-Sadawe IA, Ermeli NB, Mohamed SB, Al-Forgany M, Mrema IA, Erhuma M, Hermann A, Gbaj AM.
PMID: 29854013
Open Med Chem J. 2018 Apr 30;12:48-59. doi: 10.2174/1874104501812010048. eCollection 2018.

BACKGROUND: Tuberculosis (TB) is the second important cause of death worldwide caused by a bacterium called METHODS: Our main aims are to design and synthesize analogues of TLM as new lead molecules which could be a possible anti-TB candidate....

Treatment of Latent Tuberculosis Infection and Its Clinical Efficacy.

Tuberculosis and respiratory diseases

Kim HW, Kim JS.
PMID: 29332319
Tuberc Respir Dis (Seoul). 2018 Jan;81(1):6-12. doi: 10.4046/trd.2017.0052.

The role of the treatment for latent tuberculosis infection (LTBI) has been underscored in the intermediate tuberculosis (TB) burden countries like South Korea. LTBI treatment is recommended only for patients at risk for progression to active TB-those with frequent...

Showing 13 to 24 of 87 entries