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https://www.readbyqxmd.com/read/28043639/identification-of-novel-mycobacterium-tuberculosis-dihydrofolate-reductase-inhibitors-through-rational-drug-design
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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...
November 21, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27894872/synthesis-screening-and-docking-analysis-of-hispolon-analogs-as-potential-antitubercular-agents
#8
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
#9
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
https://www.readbyqxmd.com/read/27823561/synthesis-antitubercular-and-anticancer-activities-of-p-nitrophenylethylenediamine-derived-schiff-bases
#10
Raquel S Amim, Cláudia Pessoa, Maria C S Lourenço, Marcus V N de Souza, Josane A Lessa
BACKGROUND: Schiff bases have been greatly studied in biological field due to their wide range of pharmacological activities, such as antitubercular and antitumour. In the search of novel antitubercular agents, several compounds containing pharmacophoric group of ethambutol have been synthesized and evaluated against mycobacteria species causing tuberculosis. In this work, we investigate whether ethylenediamine, Schiff base as well as nitro group together could contribute to the formation of novel molecules with dual biological activities: antitubercular and anticancer...
November 4, 2016: Medicinal Chemistry
https://www.readbyqxmd.com/read/27810439/preliminary-sar-and-biological-evaluation-of-antitubercular-triazolothiadiazine-derivatives-against-drug-susceptible-and-drug-resistant-mtb-strains
#11
Ziqiang Li, Xiaoguang Bai, Qi Deng, Guoning Zhang, Lei Zhou, Yishuang Liu, Juxian Wang, Yucheng Wang
Following up the SAR study of triazolothiadiazoles for their antitubercular activities targeting Mt SD in our previous study, on the principle of scaffold hopping, the C3 and C6 positions of triazolothiadiazine were examined systematically to define a preliminary structure-activity relationship (SAR) with respect to biological activity. This study herein highlights the potential of two highly potent advanced leads 6c-3, 6g-3 and several other compounds with comparable potencies as promising new candidates for the treatment of TB (6c-3, MIC-H37Rv=0...
January 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27775177/recent-advances-and-structural-features-of-enoyl-acp-reductase-inhibitors-of-mycobacterium-tuberculosis
#12
Bharathkumar Inturi, Gurubasavaraj V Pujar, Madhusudhan N Purohit
Mycobacterium tuberculosis enoyl-ACP reductase (InhA) has been validated as a promising target for antitubercular agents. Isoniazid (INH), the most prescribed drug to treat tuberculosis (TB), inhibits a NADH-dependent InhA that provides precursors of mycolic acids, which are components of the mycobacterial cell wall. It is a pro-drug that needs activation to form the inhibitory INH-NAD adduct by KatG coding for catalase-peroxidase. The INH resistance of M. tuberculosis is caused by mutations in KatG, which may lead to multidrug-resistant TB (MDR-TB)...
November 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27769030/differential-characterization-using-readily-accessible-nmr-experiments-of-novel-n-and-o-alkylated-quinolin-4-ol-1-5-naphthyridin-4-ol-and-quinazolin-4-ol-derivatives-with-antimycobacterial-activity
#13
Eleni Pitta, Olga Balabon, Maciej K Rogacki, Jesús Gómez, Fraser Cunningham, Jurgen Joosens, Koen Augustyns, Pieter van der Veken, Robert Bates
During the construction of bioactive molecules, regioselective alkylation of heterocyclic, N/O ambident nucleophiles is a frequently encountered synthetic transformation. In this framework, specific attention is required to unambiguously determine the structures of obtained reaction products. As part of our project on quinoloxyacetamide based antimycobacterial agents, a series of N- or O- alkylated quinolin-4-ol, 1,5-naphthyridin-4-ol and quinazolin-4-ol derivatives were prepared during the course of which we observed unexpected selectivity issues...
January 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27676224/structure-activity-relationships-of-the-mepicides-n-acyl-and-o-linked-analogs-of-fr900098-as-inhibitors-of-dxr-from-mycobacterium-tuberculosis-and-yersinia-pestis
#14
Géraldine San Jose, Emily R Jackson, Amanda Haymond, Chinchu Johny, Rachel L Edwards, Xu Wang, R Carl Brothers, Emma K Edelstein, Audrey R Odom, Helena I Boshoff, Robin D Couch, Cynthia S Dowd
Despite continued research efforts, the threat of drug resistance from a variety of bacteria continues to plague clinical communities. Discovery and validation of novel biochemical targets will facilitate development of new drugs to combat these organisms. The methylerythritol phosphate (MEP) pathway to make isoprene units is a biosynthetic pathway essential to many bacteria. We and others have explored inhibitors of the MEP pathway as novel antibacterial agents. Mycobacterium tuberculosis, the causative agent of tuberculosis, and Yersinia pestis, resulting in the plague or "black death", both rely on the MEP pathway for isoprene production...
December 9, 2016: ACS Infectious Diseases
https://www.readbyqxmd.com/read/27665179/investigation-of-c-5-alkynyl-alkynyloxy-or-hydroxymethyl-and-or-n-3-propynyl-substituted-pyrimidine-nucleoside-analogs-as-a-new-class-of-antimicrobial-agents
#15
Saurabh Garg, Neeraj Shakya, Naveen C Srivastav, Babita Agrawal, Dennis Y Kunimoto, Rakesh Kumar
The resurgence of mycobacterial infections and the emergence of drug-resistant strains urgently require a new class of agents that are distinct than current therapies. A group of 5-ethynyl (6-10), 5-(2-propynyloxy) (16, 18, 20, 22, 24), 5-(2-propynyloxy)-3-N-(2-propynyl) (17, 19, 21, 23, 25) and 5-hydroxymethyl-3-N-(2-propynyl) (30-33) derivatives of pyrimidine nucleosides were synthesized and evaluated against mycobacteria [Mycobacterium tuberculosis (Mtb), Mycobacterium bovis (BCG) and Mycobacterium avium], gram-positive bacteria (Staphylococcus aureus and Enterococcus faecalis) and gram-negative bacteria (Escherichia coli, Salmonella typhimurium and Pseudomonas aeruginosa) alone and in combination with existing drugs in in vitro assays...
November 1, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27649943/identification-and-validation-of-novel-drug-targets-in-mycobacterium-tuberculosis
#16
Vinayak Singh, Valerie Mizrahi
Tuberculosis (TB) is a global epidemic associated increasingly with resistance to first- and second-line antitubercular drugs. The magnitude of this global health threat underscores the urgent need to discover new antimycobacterial agents that have novel mechanisms of action (MOA). In this review, we highlight some of the key advances that have enabled the strengths of target-led and phenotypic approaches to TB drug discovery to be harnessed both independently and in combination. Critically, these promise to fuel the front-end of the TB drug pipeline with new, pharmacologically validated drug targets together with lead compounds that act on these targets...
September 17, 2016: Drug Discovery Today
https://www.readbyqxmd.com/read/27649942/new-prodrugs-against-tuberculosis
#17
Giorgia Mori, Laurent Roberto Chiarelli, Giovanna Riccardi, Maria Rosalia Pasca
The term 'prodrug' was first introduced by Albert in 1958. Generally, prodrugs can be utilized for improving active drug solubility and bioavailability, increasing drug permeability and absorption, modifying the distribution profile, preventing fast metabolism and excretion, and reducing toxicity. Previously, the prodrug approach was a final resort during the drug discovery process only after all other approaches had been exhausted. However, this strategy is now considered during the early stages of the drug development process...
September 17, 2016: Drug Discovery Today
https://www.readbyqxmd.com/read/27622945/computer-aided-drug-discovery-approaches-against-the-tropical-infectious-diseases-malaria-tuberculosis-trypanosomiasis-and-leishmaniasis
#18
Peter M Njogu, Eric M Guantai, Elumalai Pavadai, Kelly Chibale
Despite the tremendous improvement in overall global health heralded by the adoption of the Millennium Declaration in the year 2000, tropical infections remain a major health problem in the developing world. Recent estimates indicate that the major tropical infectious diseases, namely, malaria, tuberculosis, trypanosomiasis, and leishmaniasis, account for more than 2.2 million deaths and a loss of approximately 85 million disability-adjusted life years annually. The crucial role of chemotherapy in curtailing the deleterious health and economic impacts of these infections has invigorated the search for new drugs against tropical infectious diseases...
January 8, 2016: ACS Infectious Diseases
https://www.readbyqxmd.com/read/27591998/synthesis-and-evaluation-of-copper-ii-complexes-with-isoniazid-derived-hydrazones-as-anticancer-and-antitubercular-agents
#19
Gisele S S Firmino, Marcus V N de Souza, Claudia Pessoa, Maria C S Lourenco, Jackson A L C Resende, Josane A Lessa
In this study, the N,N,O metal chelator 2-pyridinecarboxaldehydeisonicotinoyl hydrazone (HPCIH, 1) and its derivatives 2-acetylpyridine-(HAPIH 2), 2-pyridineformamide-(HPAmIH, 3) and pyrazineformamide-(HPzAmIH, 4) were employed in the synthesis of four copper(II) complexes, [Cu(HPCIH)Cl2]·0.4H2O (5), [Cu(HAPIH)Cl2]·1.25H2O (6), [Cu(HPAmIH)Cl2]·H2O (7) and [Cu(HPzAmIH)Cl2]·1.25H2O (8). The compounds were assayed for their action toward Mycobacterium tuberculosis H37Rv ATCC 27294 strain and the human tumor cell lines OVCAR-8 (ovarian cancer), SF-295 (glioblastoma multiforme) and HCT-116 (colon adenocarcinoma)...
December 2016: Biometals: An International Journal on the Role of Metal Ions in Biology, Biochemistry, and Medicine
https://www.readbyqxmd.com/read/27585570/microwave-assisted-synthesis-of-2-styrylquinoline-4-carboxylic-acids-as-antitubercular-agents
#20
Gisela C Muscia, Silvia E Asis, Graciela Y Buldain
BACKGROUND: Many 2-substituted quinolines and especially 2-arylvinyl derivatives isolated from plants or prepared by synthesis have been designed from ethnopharmacological studies. OBJECTIVE: In order to explore new aspects of the structure-antituberculosis activity relationship, a series of styrylquinoline derivatives was prepared Method: A series of styrylquinoline derivatives was prepared from quinaldic acid and a variety of arylbenzaldehydes under eco-friendly conditions via Knoevenagel reaction and trifluoroacetic acid (TFA) as catalyst...
September 1, 2016: Medicinal Chemistry
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