scholarly journals Optimization and Evaluation of 5-Styryl-Oxathiazol-2-one Mycobacterium tuberculosis Proteasome Inhibitors as Potential Antitubercular Agents

ChemistryOpen ◽  
2015 ◽  
Vol 4 (3) ◽  
pp. 342-362 ◽  
Author(s):  
Francesco Russo ◽  
Johan Gising ◽  
Linda Åkerbladh ◽  
Annette K. Roos ◽  
Agata Naworyta ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Proteasome Inhibitors ◽  
Antitubercular Agents

scholarly journals Synthesis and Preliminary Evaluation of Benzofuran-Oxadiazole Conjugates as Potential Antitubercular Agents

2019 ◽  
Vol 31 (4) ◽  
pp. 965-970 ◽  
Author(s):  
Veerabhadrayya S. Negalurmath ◽  
Obelannavar Kotresh ◽  
Mahantesha Basanagouda
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Spectral Data ◽  
13C Nmr ◽  
Antitubercular Activity ◽  
Preliminary Evaluation ◽  
Antitubercular Agents ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Mycobacterium Tuberculosis H37rv ◽  
Mycobacterium Phlei

In the present study, a series of benzofuran-oxadiazole conjugates 7(a-o) was designed, synthesized and characterized through IR, 1H NMR, 13C NMR and mass spectral data. All the compounds were screened for preliminary antitubercular activity against Mycobacterium phlei and Mycobacterium tuberculosis H37RV. Among all the target compounds, the compound possessing chlorine (7k, MIC 1.56 μg/mL) and bromine (7m, MIC 1.56 μg/mL) on 6th position of benzofuran showed highest activity against Mycobacterium phlei. Whereas, bromine on either 5th position (7l, MIC 3.125 μg/mL) or 6th position (7m MIC 3.125 μg/mL) on benzofuran exhibited highest activity for Mycobacterium tuberculosis (H37 RV).

Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis

2016 ◽  
Vol 59 (6) ◽  
pp. 2362-2380 ◽  
Author(s):  
Galina Karabanovich ◽  
Júlia Zemanová ◽  
Tomáš Smutný ◽  
Rita Székely ◽  
Michal Šarkan ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Antitubercular Agents

Design, synthesis and evaluation of diphenyl ether analogues as antitubercular agents

RSC Advances ◽  
2016 ◽  
Vol 6 (112) ◽  
pp. 110571-110582 ◽  
Author(s):  
Bharathkumar Inturi ◽  
Gurubasavaraj V. Pujar ◽  
Madhusudhan N. Purohit ◽  
Viswanathan B. Iyer ◽  
Sowmya G. S. ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Drug Design ◽  
Acyl Carrier Protein ◽  
Diphenyl Ether ◽  
Design Approach ◽  
Carrier Protein ◽  
Antitubercular Agents ◽  
Structure Based Drug Design ◽  
Design Synthesis ◽  
Diphenyl Ethers

We herein report the investigation of new diphenyl ethers asMycobacterium tuberculosisenoyl-acyl carrier protein reductase (InhA) inhibitors by structure-based drug design approach.

ChemInform Abstract: [1,2,3]Triazolo[4,5-h]quinolones. A New Class of Potent Antitubercular Agents Against Multidrug Resistant Mycobacterium tuberculosis Stains.

ChemInform ◽  
2008 ◽  
Vol 39 (1) ◽  
Author(s):  
Antonio Carta ◽  
Michele Palomba ◽  
Giuseppe Paglietti ◽  
Paola Molicotti ◽  
Bianca Paglietti ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Multidrug Resistant ◽  
Antitubercular Agents ◽  
New Class

The dependence of the inflammatory reaction on the properties of mycobacterium tuberculosis and the course of specific pulmonary process

2013 ◽  
Vol 59 (4) ◽  
pp. 469-478 ◽  
Author(s):  
O.T. Titarenko ◽  
M.E. Dyakova ◽  
D.S. Esmedlyaeva ◽  
O.A. Manicheva ◽  
N.P. Alekseeva ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Inflammatory Process ◽  
Acute Phase Proteins ◽  
Pathological Process ◽  
The Body ◽  
Newly Diagnosed ◽  
Antitubercular Agents ◽  
Multifactorial Analysis ◽  
Systemic Analysis ◽  
Protective Systems

The systemic analysis of the inflammatory process in untreated patients with newly diagnosed infiltrative-destructive tuberculosis has been performed in the context of host mycobacterium interaction. Variability of acute phase proteins (APP) reflecting mobilization of nonspecific protective systems of the body did not depend on cytotoxicity of Mycobacterium tuberculosis (MBT). In 87.5% of patients the dependence between effectiveness of antitubercular chemotherapy (for three months) and combination of MBT characteristics and initial APP levels was found. Patients with effectiveness of therapy, which was inadequate to MBT cytotoxicity, were characterized by its dependence on the APP level and MBT sensitivity to antitubercular agents. Results of multifactorial analysis of parameters reflecting intensity of the inflammatory response, pathological process in the lungs, and characteristics of MBT suggest that the overall result of the host-pathogen interactions primarily depend on adequateness of protective systems of the body

scholarly journals Erratum to: Discovery of new Mycobacterium tuberculosis proteasome inhibitors using a knowledge-based computational screening approach

2015 ◽  
Vol 20 (1) ◽  
pp. 367-367 ◽  
Author(s):  
Rukmankesh Mehra ◽  
Reena Chib ◽  
Gurunadham Munagala ◽  
Kushalava Reddy Yempalla ◽  
Inshad Ali Khan ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Proteasome Inhibitors ◽  
Knowledge Based ◽  
Computational Screening ◽  
Screening Approach

[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains

2007 ◽  
Vol 17 (17) ◽  
pp. 4791-4794 ◽  
Author(s):  
Antonio Carta ◽  
Michele Palomba ◽  
Giuseppe Paglietti ◽  
Paola Molicotti ◽  
Bianca Paglietti ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Multidrug Resistant ◽  
Antitubercular Agents ◽  
New Class

Synthesis & Evaluation of Antitubercular Activity of Novel Mannich Bases of imidazo[2,1-b][1,3,4]thiadiazoles

2013 ◽  
Vol 816-817 ◽  
pp. 1197-1201 ◽  
Author(s):  
Naveen P.Badiger ◽  
I.M. Khazi
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Pharmacological Activity ◽  
Mannich Reaction ◽  
Antitubercular Activity ◽  
Mannich Bases ◽  
Ring Structure ◽  
Membered Ring ◽  
Ring Size ◽  
Antitubercular Agents ◽  
Radiometric Assay

A series of 2-(4-methoxybenzyl)-6-aryl-5-pyrrolidin/piperidin/morpholin-1-ylmethyl-imidazo [2,1-[1,3, thiadiazoles (3a-e, 4a-e & 5a-e) were synthesized by Mannich reaction by condensing 2-(4-methoxybenzyl)-6-arylimidazo [2,1-[1,3,thiadiazoles with pyrrolidine, piperidine and morpholine. The title compounds were screened for antitubercular activity againstMycobacterium tuberculosisH37Rv using the BACTEC 460 radiometric assay. Mannich bases with pyrrolidine substitution were found to be most active antitubercular agents. It proves that as the ring size decreases it becomes much potent in its activity. Pyrrolidine being 5 membered ring structure & further combined with imidazothiadiazole nucleus enhances the pharmacological activity.

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