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Antitubercular agent

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https://www.readbyqxmd.com/read/28527405/synthesis-and-structure-activity-relationships-of-novel-fused-ring-analogues-of-q203-as-antitubercular-agents
#1
Sunhee Kang, Young Mi Kim, Heekyung Jeon, Sejin Park, Min Jung Seo, Saeyeon Lee, Dongsik Park, Jiyeon Nam, Seokwoo Lee, Kiyean Nam, Sanghee Kim, Jaeseung Kim
A set of fused ring analogues of a new antitubercular agent, Q203, was designed and synthesized. To reduce the lipophilicity of Q203 caused by linearly extended side chains, shorter and heteroatoms containing fused rings were introduced into the side chain region. Antitubercular activity was tested against H37Rv-GFP replicating in liquid broth culture medium (extracellular) and within macrophages (intracellular). Many analogues showed potent extracellular activities as well as intracellular activities without cytotoxicity...
May 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28497493/natural-and-synthetic-flavonoids-as-potent-mycobacterium-tuberculosis-ugm-inhibitors
#2
Stephane Vincent, Sydney Villaume, Jian Fu, Inès N'Go, Huayong Lou, Hui Liang, Laurent Kremer, Weidong Pan
This study reports a novel class of inhibitors of UDP-galactopyranose mutase (UGM) derived from a screening of natural products. This enzyme is an essential biocatalyst involved in the cell wall biosynthesis of Mycobacterium tuberculosis. Flavonoids were found to be potent inhibitors of UGM. The synthesis of novel methylated flavonoids allowed to perform a structure-activity relationship analysis and to determine which functional groups and structural elements are required for UGM inhibition.The binding mode of one of the best inhibitor was found to be non-competitive...
May 11, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28462696/hybrid-docking-qsar-studies-of-1-4-dihydropyridine-3-5-dicarboxamides-as-potential-antitubercular-agents
#3
Yasaman Rasouli, Asghar Davood
BACKGROUND: Tuberculosis is one of the main medical problems that some people are suffering still from this infectious disease. 1, 4-dihydropyridines are a multi-target ligands that recently are recognized as an anti-tubercular agents. METHOD: In the current research we did computational studies of some synthesized 1, 4-dihydropyridine-3, 5-dicarboxamides in non-hydrolyzed and hydrolyzed forms to find the drug-receptor interactions profile. RESULTS: Among equations that obtained for non-hydrolyzed compounds, the model with better statistical parameters such as R2= 0...
April 26, 2017: Current Computer-aided Drug Design
https://www.readbyqxmd.com/read/28459575/7-substituted-2-nitro-5-6-dihydroimidazo-2-1-b-1-3-oxazines-novel-antitubercular-agents-lead-to-a-new-preclinical-candidate-for-visceral-leishmaniasis
#4
Andrew M Thompson, Patrick D O'Connor, Andrew J Marshall, Vanessa Yardley, Louis Maes, Suman Gupta, Delphine Launay, Stephanie Braillard, Eric Chatelain, Scott G Franzblau, Baojie Wan, Yuehong Wang, Zhenkun Ma, Christopher B Cooper, William A Denny
Within a backup program for the clinical investigational agent pretomanid (PA-824), scaffold hopping from delamanid inspired the discovery of a novel class of potent antitubercular agents that unexpectedly possessed notable utility against the kinetoplastid disease visceral leishmaniasis (VL). Following the identification of delamanid analogue DNDI-VL-2098 as a VL preclinical candidate, this structurally related 7-substituted 2-nitro-5,6-dihydroimidazo[2,1-b][1,3]oxazine class was further explored, seeking efficacious backup compounds with improved solubility and safety...
May 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28446777/structural-investigations-on-orotate-phosphoribosyltransferase-from-mycobacterium-tuberculosis-a-key-enzyme-of-the-de-novo-pyrimidine-biosynthesis
#5
Stefano Donini, Davide M Ferraris, Riccardo Miggiano, Alberto Massarotti, Menico Rizzi
The Mycobacterium tuberculosis orotate phosphoribosyltransferase (MtOPRT) catalyses the conversion of α-D-5-phosphoribosyl-1-pyrophosphate (PRPP) and orotate (OA) in pyrophosphate and orotidine 5'-monophosphate (OMP), in presence of Mg(2+). This enzyme is the only responsible for the synthesis of orotidine 5'-monophosphate, a key precursor in the de novo pyrimidine biosynthesis pathway, making MtOPRT an attractive drug target for the development of antitubercular agents. We report the crystal structures of MtOPRT in complex with PRPP (2...
April 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28419153/biochemical-and-structural-investigations-on-phosphoribosylpyrophosphate-synthetase-from-mycobacterium-smegmatis
#6
Stefano Donini, Silvia Garavaglia, Davide M Ferraris, Riccardo Miggiano, Shigetarou Mori, Keigo Shibayama, Menico Rizzi
Mycobacterium smegmatis represents one model for studying the biology of its pathogenic relative Mycobacterium tuberculosis. The structural characterization of a M. tuberculosis ortholog protein can serve as a valid tool for the development of molecules active against the M. tuberculosis target. In this context, we report the biochemical and structural characterization of M. smegmatis phosphoribosylpyrophosphate synthetase (PrsA), the ortholog of M. tuberculosis PrsA, the unique enzyme responsible for the synthesis of phosphoribosylpyrophosphate (PRPP)...
2017: PloS One
https://www.readbyqxmd.com/read/28407303/rifampicin-reverses-nicardipine-effect-inducing-uncontrolled-essential-hypertension
#7
Elena-Mihaela Cordeanu, Sébastien Gaertner, Alix Faller, Corina Mirea, Jean-Marc Lessinger, Veronique Kemmel, Dominique Stephan
Dihydropyridine calcium-channel blockers are a known substrate for the cytochrome P450 isoform 3A4. Rifampicin, an antitubercular agent, is one of the most potent inducers of hepatic and intestinal CYP3A4 thus increasing dihydropyridine metabolism. We report a case of a 67-year-old hypertensive female treated with a 4-drug antihypertensive regimen including a dihydropyridine (nicardipine 50mg bid), who was admitted for septic arthritis of the knee requiring antibiotic treatment with teicoplanin 400mg od and rifampicin 600mg bid...
April 13, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28384546/in%C3%A2-vitro-biological-evaluation-of-new-antimycobacterial-salicylanilide-tuftsin-conjugates
#8
Zsuzsa Baranyai, Martin Krátký, Rudolf Vosátka, Eleonóra Szabó, Zsuzsanna Senoner, Sándor Dávid, Jiřina Stolaříková, Jarmila Vinšová, Szilvia Bősze
Tuberculosis is caused by Mycobacterium tuberculosis, an intracellular pathogen that can survive in host cells, mainly in macrophages. An increase of multidrug-resistant tuberculosis qualifies this infectious disease as a major public health problem worldwide. The cellular uptake of the antimycobacterial agents by infected host cells is limited. Our approach is to enhance the cellular uptake of the antituberculars by target cell-directed delivery using drug-peptide conjugates to achieve an increased intracellular efficacy...
March 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28372908/novel-quinoxalinyl-chalcone-hybrid-scaffolds-as-enoyl-acp-reductase-inhibitors-synthesis-molecular-docking-and-biological-evaluation
#9
Vidya Desai, Sulaksha Desai, Sonia Naik Gaonkar, Uddesh Palyekar, Shrinivas D Joshi, Sheshagiri K Dixit
We report herein, first ever synthesis of series of novel differently substituted quinoxalinyl chalcones using Claisen Schmidt condensation, its molecular docking studies, and potential to be good anti-microbial, anti-tubercular and anti-cancer agents. The antimicrobial studies were carried out against Staphylococcus aureus, Escherichia coli and Candida albicans using disc diffusion procedure. The selected chalcones were tested for anti-cancer and cytotoxicity activity against MCF-7 cancer cell line using MTT assay method...
March 24, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28279848/structure-activity-relationship-studies-on-3-5-dinitrophenyl-tetrazoles-as-antitubercular-agents
#10
Jan Němeček, Pavel Sychra, Miloslav Macháček, Markéta Benková, Galina Karabanovich, Klára Konečná, Věra Kavková, Jiřina Stolaříková, Alexandr Hrabálek, Kateřina Vávrová, Ondřej Soukup, Jaroslav Roh, Věra Klimešová
In this study, we described the structure-activity relationships of substituted 3,5-dinitrophenyl tetrazoles as potent antitubercular agents. These simple and readily accessible compounds possessed high in vitro antimycobacterial activities against Mycobacterium tuberculosis, including clinically isolated multidrug (MDR) and extensively drug-resistant (XDR) strains, with submicromolar minimum inhibitory concentrations (MICs). The most promising compounds showed low in vitro cytotoxicity and negligible antibacterial and antifungal activities, highlighting their highly selective antimycobacterial effects...
April 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28274627/three-component-one-pot-synthesis-of-anthranilamide-schiff-bases-bearing-4-aminoquinoline-moiety-as-mycobacterium-tuberculosis-gyrase-inhibitors
#11
Preeti S Salve, Shankar G Alegaon, Dharmarajan Sriram
An efficient three-component, one-pot protocol is described for the synthesis of biologically interesting 2-(benzylideneamino)-N-(7-chloroquinolin-4-yl)benzohydrazide derivatives from isatoic anhydride, 7-chloro-4-hydrazinylquinoline and aromatic and/or hetero aromatic aldehydes under catalyst free condensation by using water as reaction media. All synthesized compounds were evaluated for their antimycobacterial activity against Mycobacterium tuberculosis (MTB) and cytotoxicity activity against normal VERO cell lines...
February 17, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28260468/tuberculosis-after-renal-transplant
#12
Samia Barbouch, Meriam Hajji, Imed Helal, Mondher Ounissi, Mohammed Mongi Bacha, Fathi Ben Hamida, Ezzedine Abderrahim, Taieb Ben Abdallah
Tuberculosis is one of the leading infections after renal transplant, particularly in developing countries where the incidence and prevalence in the general population are high. Diagnosis requires bacteriologic and histologic confirmation. Interactions among the antitubercular drugs and the immunosuppressive agents have to be considered while prescribing, and surveillance for adverse effects is required. Although rare, case reports are available on extrapulmonary tuberculosis in allograft recipients. Here, we present a 25-year-old kidney transplant recipient who was diagnosed with lymph node tuberculosis under uncommon circumstances but who had a good outcome...
February 2017: Experimental and Clinical Transplantation
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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 showed that MmpL3 inhibitors act synergistically with rifampin, bedaquiline, clofazimine, and β-lactams.
April 2017: Antimicrobial Agents and Chemotherapy
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