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Antitubercular agent

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https://www.readbyqxmd.com/read/28196957/a-novel-small-molecule-inhibitor-of-the-mycobacterium-tuberculosis-demethylmenaquinone-methyltransferase-meng-is-bactericidal-to-both-growing-and-nutritionally-deprived-persister-cells
#1
Paridhi Sukheja, Pradeep Kumar, Nisha Mittal, Shao-Gang Li, Eric Singleton, Riccardo Russo, Alexander L Perryman, Riju Shrestha, Divya Awasthi, Seema Husain, Patricia Soteropoulos, Roman Brukh, Nancy Connell, Joel S Freundlich, David Alland
Active tuberculosis (TB) and latent Mycobacterium tuberculosis infection both require lengthy treatments to achieve durable cures. This problem has partly been attributable to the existence of nonreplicating M. tuberculosis "persisters" that are difficult to kill using conventional anti-TB treatments. Compounds that target the respiratory pathway have the potential to kill both replicating and persistent M. tuberculosis and shorten TB treatment, as this pathway is essential in both metabolic states. We developed a novel respiratory pathway-specific whole-cell screen to identify new respiration inhibitors...
February 14, 2017: MBio
https://www.readbyqxmd.com/read/28185538/synthesis-and-biological-evaluation-of-hybrid-1-5-and-2-5-disubstituted-indoles-as-potentially-new-antitubercular-agents
#2
Ana Soares, Mónica S Estevão, M Manuel B Marques, Vasily Kovalishyn, Diogo A R S Latino, João Aires-de-Sousa, Jorge Ramos, Miguel Viveiros, Filomena Martins
BACKGROUND: Tuberculosis (TB) is the second leading cause of mortality worldwide being a highly contagious and insidious illness caused by Mycobacterium tuberculosis, Mtb. Additionally, the emergence of multidrug-resistant and extensively drug-resistant strains of Mtb, together with significant levels of co-infection with HIV and TB (HIV/TB) makes the search for new antitubercular drugs urgent and challenging. METHODS: This work was based on the hypothesis that an active compound could be obtained if substituents present in some other active compounds were attached on a core of an important structure, in this case the indole scaffold, thus generating a hybrid compound...
February 9, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28166917/two-cases-of-eyelid-tuberculosis-an-uncommon-presentation-of-ocular-tuberculosis
#3
D K Bajaj, A Srivastava, R A S Kushwaha, A Joshi, M K Pandey, P Mishra, M Asnani
Mycobacterium tuberculosis apart from being the causative agent of pulmonary tuberculosis is also notorious to cause tuberculosis at various sites in the human body and ocular tuberculosis is one of the extra pulmonary manifestations of this organism. The most common presentation of ocular tuberculosis is anterior uveitis or choroiditis caused by hematogenous infection or hypersensitivity after another organ infection. Eyelid involvement by tuberculosis is most of the times secondary to orbital involvement and often seen in the form of drainage sinus...
January 2017: Indian Journal of Tuberculosis
https://www.readbyqxmd.com/read/28163562/hydrazide-hydrazones-as-potential-antimicrobial-agents-overview-of-the-literature-since-2010
#4
REVIEW
Łukasz Popiołek
Hydrazide-hydrazone derivatives are present in many bioactive molecules and display a wide variety of biological activities, such as antibacterial, antitubercular, antifungal, anticancer, anti-inflammatory, anticonvulsant, antiviral, and antiprotozoal action. Therefore, many medicinal chemists synthesize various hydrazide-hydrazones and evaluate them for biological activities. Among biological properties of this class of compounds, antimicrobial activity is the most frequently encountered in scientific literature...
2017: Medicinal Chemistry Research
https://www.readbyqxmd.com/read/28124614/synthesis-of-adamantane-aminoethers-with-antitubercular-potential
#5
Angeliki-Sofia Foscolos, Ioannis Papanastasiou, Andrew Tsotinis, Nicolas Kolocouris, George B Foscolos, Anthony Vocat, Stewart T Cole
BACKGROUND: Intrigued by the fact that aminoadamantane derivatives, bearing the active 1,2-ethylenediamine moiety, are promising antitubercular agents, we report herein on the synthesis and the antitubercular evaluation of N,N'-substituded-4,4'-[adamantane-2,2-diyl]bis(phenoxyalkyl amines) 1a-g, 1,1'-{4,4'-[adamantane-1,3-diyl]bis(phenoxyalkyl)} amines 2a-f, N,N'-substituded-[4-(1-adamantane)phenoxy] alkylamines) 3a-d and 2-[4-(dimethylaminoalkoxy)phenyl]adamantan-2-ol 4a,b, Methods: A substituted diarylmethane moiety was introduced on the adamantane skeleton of the new derivatives...
January 25, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28118738/design-of-potent-fluoro-substituted-chalcones-as-antimicrobial-agents
#6
Serdar Burmaoglu, Oztekin Algul, Arzu Gobek, Derya Aktas Anil, Mahmut Ulger, Busra Gul Erturk, Engin Kaplan, Aylin Dogen, Gönül Aslan
Owing to ever-increasing bacterial and fungal drug resistance, we attempted to develop novel antitubercular and antimicrobial agents. For this purpose, we developed some new fluorine-substituted chalcone analogs (3, 4, 9-15, and 20-23) using a structure-activity relationship approach. Target compounds were evaluated for their antitubercular efficacy against Mycobacterium tuberculosis H37Rv and antimicrobial activity against five common pathogenic bacterial and three common fungal strains. Three derivatives (3, 9, and 10) displayed significant antitubercular activity with IC50 values of ≤16,760...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28117201/development-of-gallic-acid-formazans-as-novel-enoyl-acyl-carrier-protein-reductase-inhibitors-for-the-treatment-of-tuberculosis
#7
Vanita D Saharan, Supriya S Mahajan
The enoyl acyl carrier protein reductase (InhA) of Mycobacterium tuberculosis (MTB) is an attractive target for developing novel antitubercular agents. A series of gallic acid formazans, were computationally designed and docked into the active site of InhA to understand their binding mode and potential to inhibit InhA. Nine compounds from the designed series were identified as potential InhA inhibitors, on the basis of good Glide score. These compounds were synthesized in the laboratory and evaluated for in vitro antitubercular activity against drug-sensitive and multi-drug resistant strains of MTB...
January 11, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28115355/synergistic-interactions-of-mmpl3-inhibitors-with-antitubercular-compounds-in-vitro
#8
Wei Li, Andrea Sanchez-Hidalgo, Victoria Jones, Vinicius Calado Nogueira de Moura, E Jeffrey North, Mary Jackson
A number of inhibitors of the essential Mycobacterium tuberculosis mycolic acid transporter, MmpL3, are currently under development as potential novel antituberculosis agents. Using the checkerboard method to study the interaction profiles of various antituberculosis drugs or experimental compounds with two different chemotypes inhibiting this transporter (indolcarboxamides and adamantyl ureas), we show that MmpL3 inhibitors act synergistically with rifampin, bedaquiline, clofazimine and β-lactams.
January 23, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28110868/quinolidene-based-monocarbonyl-curcumin-analogues-as-promising-antimycobacterial-agents-synthesis-and-molecular-docking-study
#9
Dnyaneshwar D Subhedar, Mubarak H Shaikh, Laxman Nawale, Dhiman Sarkar, Vijay M Khedkar, Bapurao B Shingate
A series of quinoline incorporated monocarbonyl curcumin analogues was efficiently synthesized using [HDBU][HSO4] as catalyst via Knoevenagel type condensation and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB) and Mycobacterium bovis BCG in dormant state. The analogues 3e, 3h, 4a and 4e exhibited very good antitubercular activity. The antiproliferative activity of the analogues against MCF-7, A549 and HCT-116 cell lines was evaluated using modified MTT assay and these compounds were found to be non-cytotoxic...
January 5, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28103537/hybrids-of-thienopyrimidinones-and-thiouracils-as-anti-tubercular-agents-sar-and-docking-studies
#10
Mahesh M Pisal, Laxman U Nawale, Manoj D Patil, Sujit G Bhansali, Jayant M Gajbhiye, Dhiman Sarkar, Subhash P Chavan, Hanumant B Borate
A number of hybrid molecules containing thienopyrimidinones and thiouracil moieties were designed, synthesized and tested against Mycobacterium tuberculosis H37Ra wherein it was observed that the compounds 11-14 exhibited antitubercular activity in vitro (MIC 7.6-19.1 μg/mL, 12-35 μM) against dormant stage while the compound 15 exhibited antitubercular activity in vitro against dormant (MIC 23.4 μg/mL, 41 μM) as well as active (MIC 25.4 μg/mL, 45 μM) stage. Structural modifications of the compound 15 were carried out to study the structure-activity relationship and it was observed that the compound 18 exhibited antitubercular activity comparable to the compound 15...
January 9, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28091937/ocular-mycobacteriosis-dual-infection-of-m-tuberculosis-complex-with-m-fortuitum-and-m-bovis
#11
Kusum Sharma, Natasha Gautam, Megha Sharma, Mohit Dogra, Priya Bajgai, Basavaraj Tigari, Aman Sharma, Vishali Gupta, Surya Prakash Sharma, Ramandeep Singh
BACKGROUND: We report unfavorable outcome in a patient with subretinal granuloma caused by dual infection of Mycobacterium tuberculosis complex with Mycobacterium fortuitum and Mycobacterium bovis in an immunosuppressed, non-HIV patient. We did a systematic review of literature on dual infection due to M. tuberculosis and M. fortuitum via MEDLINE and PUBMED and could not find any case reported of causing this kind of dual infection in the eye. RESULTS: A 38-year-old Indian male patient presented with decreased vision in the left eye for 3 months, diagnosed as tubercular choroidal granuloma with associated retinal angiomatosis proliferans (RAP) lesion...
December 2017: Journal of Ophthalmic Inflammation and Infection
https://www.readbyqxmd.com/read/28043639/identification-of-novel-mycobacterium-tuberculosis-dihydrofolate-reductase-inhibitors-through-rational-drug-design
#12
Mymoona Akhter
OBJECTIVES/BACKGROUND: Dihydrofolate reductase (DHFR) is one of the validated drug targets in Mycobacterium tuberculosis (Mtb) infection. DHFR inhibitors have been used to treat various life-threatening diseases such as cancer, malaria, and several bacterial infections. However, all clinically effective DHFR inhibitors are non-selective, and inhibit both human and pathogenic DHFRs more or less to a similar extent. The crystal structure of various DHFRs complexed with nicotinamide adenine dinucleotide phosphate and different inhibitors is available in the protein data bank...
December 2016: International Journal of Mycobacteriology
https://www.readbyqxmd.com/read/28002883/cholesterol-metabolism-a-potential-therapeutic-target-in-mycobacteria
#13
REVIEW
Areej Abuhammad
Tuberculosis (TB), although a curable disease, has remained one of the most difficult infections to treat. Mycobacterium tuberculosis (M. tuberculosis.) infects 10 million people worldwide and kills 1.5 million people each year. Reactivation of latent infection is the major cause of TB. Cholesterol is a critical carbon source during latent infection. Catabolism of cholesterol contributes to the pool of propionyl-CoA, a precursor that is incorporated into lipid virulence factors. The M. tuberculosis genome contains a large regulon of cholesterol catabolic genes suggesting that the microorganism can utilise host sterol for infection and persistence...
December 21, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27994751/identification-of-n-2-phenoxyethyl-imidazo-1-2-a-pyridine-3-carboxamides-as-new-antituberculosis-agents
#14
Zhaoyang Wu, Yu Lu, Linhu Li, Rui Zhao, Bin Wang, Kai Lv, Mingliang Liu, Xuefu You
A series of imidazo[1,2-a]pyridine carboxamides (IPAs) bearing an N-(2-phenoxyethyl) moiety was designed and synthesized as new antitubercular agents. Seven 2,6-dimethyl IPAs demonstrated excellent in vitro activity (MIC: 0.025-0.054 μg/mL) against the drug susceptive H37Rv strain and two clinically isolated multidrug-resistant Mycobacterium tuberculosisstrains. Compound 10j displayed acceptable safety and pharmacokinetic properties, opening a new direction for further development.
December 8, 2016: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27955741/medical-plant-extracts-and-natural-compounds-with-a-hepatoprotective-effect-against-damage-caused-by-antitubercular-drugs-a-review
#15
REVIEW
María Adelina Jiménez-Arellanes, Gabriel Alfonso Gutiérrez-Rebolledo, Mariana Meckes-Fischer, Rosalba León-Díaz
Drug-induced liver injury encompasses a spectrum of diseases ranging from mild biochemical abnormalities to acute liver failure; example of this scenery is hepatotoxicity caused by the first-line antituberculous drugs isoniazid, rifampin and pyrazinamide, which are basic for treatment of drug-sensible and drug-resistant tuberculosis. In the search for pharmacological alternatives to prevent liver damage, antitubercular drugs have been the subject of numerous studies and published reviews, a great majority of them carried out by Asian countries...
December 2016: Asian Pacific Journal of Tropical Medicine
https://www.readbyqxmd.com/read/27951471/bioanalysis-of-antitubercular-drugs-using-liquid-chromatography
#16
REVIEW
Kanumuri Siva Rama Raju, Manoj Gundeti, Mohd Yaseen Malik, Naveen Kadian, Mamunur Rashid, Isha Taneja, Sheelendra Pratap Singh, Muhammad Wahajuddin
Tuberculosis is a life threatening disease and second to HIV in terms of deaths due to infectious diseases. Drug resistance development of the first-line drugs is a major concern in the treatment of this disease. There is no comprehensive and critical review in the literature of the bioanalytical methods for the determination of anti-tubercular agents from last two decades. This work offers a detailed account on the liquid chromatographic methods reported in the literature for the estimation of various anti-tubercular drugs...
February 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27931683/in-silico-pass-analysis-and-determination-of-antimycobacterial-antifungal-and-antioxidant-efficacies-of-maslinic-acid-in-an-extract-rich-in-pentacyclic-triterpenoids
#17
Prasad G Jamkhande, Shahbaz K Pathan, Shailesh J Wadher
OBJECTIVE/BACKGROUND: Microbial infections such as tuberculosis is a major cause of mortality worldwide. Plant-derived phytochemicals have a long history of providing much-needed novel therapeutics. Triterpenoids are among the prominent phytochemicals that possess numerous biological activities. Among them is maslinic acid (MA), a biologically active olean-type pentacyclic triterpenoid. In search of a novel antimicrobial agent, we aimed to evaluate the antimicrobial potential of MA. METHODS: Antibacterial and antifungal activity was evaluated through the agar well diffusion method...
December 2016: International Journal of Mycobacteriology
https://www.readbyqxmd.com/read/27907875/s-substituted-3-5-dinitrophenyl-1-3-4-oxadiazole-2-thiols-and-tetrazole-5-thiols-as-highly-efficient-antitubercular-agents
#18
Galina Karabanovich, Jan Němeček, Lenka Valášková, Alejandro Carazo, Klára Konečná, Jiřina Stolaříková, Alexandr Hrabálek, Oto Pavliš, Petr Pávek, Kateřina Vávrová, Jaroslav Roh, Věra Klimešová
Two new classes of antitubercular agents, namely 5-alkylsulfanyl-1-(3,5-dinitrophenyl)-1H-tetrazoles and 2-alkylsulfanyl-5-(3,5-dinitrophenyl)-1,3,4-oxadiazoles, and their structure-activity relationships are described. These compounds possessed excellent activity against Mycobacterium tuberculosis, including the clinically isolated multidrug (MDR) and extensively drug-resistant (XDR) strains, with no cross resistance with first or second-line anti-TB drugs. The minimum inhibitory concentration (MIC) values of the most promising compounds reached 0...
January 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27894872/synthesis-screening-and-docking-analysis-of-hispolon-analogs-as-potential-antitubercular-agents
#19
Neduri V Balaji, Bollikolla Hari Babu, Gottumukkala V Subbaraju, Kurre Purna Nagasree, Muthyala Murali Krishna Kumar
A series of 20 hispolons/dihydrohispolons were synthesized and characterized by spectral data. These compounds were subjected to in vitro antitubercular activity screening against Mycobacterium tuberculosis (H37Rv) strain. The synthesized compounds showed varied antitubercular activity ranging from 100 to 1.6μg/mL. Among the screened compounds, four compounds (H1, H2, H3 and H15) have shown moderate activity with MIC 25μg/mL. Potent activities were observed for the dihydrohispolon derivative H14 (MIC 1.6μg/mL) followed by H13 (6...
January 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27843794/an-analysis-of-serious-adverse-drug-reactions-at-a-tertiary-care-teaching-hospital
#20
Kinjal Prajapati, Mira Desai, Samidh Shah, Jigar Panchal, Jigar Kapadia, Ramkumar Dikshit
OBJECTIVE: The objective of this study was to analyze the various aspects of serious adverse drug reactions (serious ADRs) such as clinical presentation, causality, severity, and preventability occurring in a hospital setting. MATERIALS AND METHODS: All serious ADRs reported from January 2010 to May 2015 at ADR Monitoring Centre, Department of Pharmacology, B. J. Medical College and Civil Hospital, Ahmedabad, were selected as per the World health Organization -Uppsala Monitoring Center (WHO-UMC) criteria...
October 2016: Perspectives in Clinical Research
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