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Antitubercular agent

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https://www.readbyqxmd.com/read/28764227/portal-venous-thrombosis-disseminated-tuberculosis-in-rheumatoid-arthritis
#1
Vasanthi Natarajan, Kevin John, David Jose, Pradeep Kalaiselvan, Ashok Kumar Das
Vascular thrombosis is one of the complications of tuberculosis. Deep vein thrombosis and pulmonary thrombosis have been reported with pulmonary and extrapulmonary tuberculosis. Splenic involvement in abdominal tuberculosis is among the rarest manifestations. Disseminated tuberculosis is predominantly reported in rheumatoid arthritis following ingestion of biological agents. Here, we report a case of disseminated tuberculosis in a rheumatoid arthritis patient who was on steroids and methotrexate for a long period, presenting with multiple splenic lesion and portal vein thrombosis, which was not reported earlier...
June 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/28763645/the-antitrypanosomal-and-antitubercular-activity-of-some-nitro-triazole-imidazole-based-aromatic-amines
#2
Maria V Papadopoulou, William D Bloomer, Howard S Rosenzweig, Marcel Kaiser
A limited number of novel 3-nitrotriazole- and 2-nitroimidazole-linked quinolines and quinazolines were synthesized and screened for in vitro antitrypanosomal and antitubercular activities as well as cytotoxicity in normal cells. All compounds were active against T. cruzi amastigotes, while all but one were active or moderately active against T. b. rhodesiense. However, only two chloroquinolines exhibited satisfactory selectivity indices (SI) against T. cruzi and only one of them demonstrated a satisfactory SI against T...
July 25, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28749666/substituted-n-phenyl-5-2-phenylamino-thiazol-4-yl-isoxazole-3-carboxamides-are-valuable-antitubercular-candidates-that-evade-innate-efflux-machinery
#3
Elisa Azzali, Diana Machado, Amit Kaushik, Federica Vacondio, Sara Flisi, Clotilde Silvia Cabassi, Gyanu Lamichhane, Miguel Viveiros, Gabriele Costantino, Marco Pieroni
Tuberculosis remains one of the deadliest infectious diseases in the world, and the increased number of multidrug-resistant and extremely drug-resistant strains is a significant reason for concern. This makes the discovery of novel antitubercular agents a cogent priority. We have previously addressed this need by reporting a series of substituted 2-aminothiazoles capable to inhibit the growth of actively replicating, nonreplicating persistent, and resistant Mycobacterium tuberculosis strains. Clues from the structure-activity relationships lining up the antitubercular activity were exploited for the rational design of improved analogues...
August 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28720801/mapping-and-characterization-of-g-quadruplexes-in-mycobacterium-tuberculosis-gene-promoter-regions
#4
Rosalba Perrone, Enrico Lavezzo, Erika Riello, Riccardo Manganelli, Giorgio Palù, Stefano Toppo, Roberta Provvedi, Sara N Richter
Mycobacterium tuberculosis is the causative agent of tuberculosis (TB), one of the top 10 causes of death worldwide in 2015. The recent emergence of strains resistant to all current drugs urges the development of compounds with new mechanisms of action. G-quadruplexes are nucleic acids secondary structures that may form in G-rich regions to epigenetically regulate cellular functions. Here we implemented a computational tool to scan the presence of putative G-quadruplex forming sequences in the genome of Mycobacterium tuberculosis and analyse their association to transcription start sites...
July 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28715707/design-synthesis-and-2d-qsar-study-of-novel-pyridine-and-quinolone-hydrazone-derivatives-as-potential-antimicrobial-and-antitubercular-agents
#5
Mohamed A Abdelrahman, Ismail Salama, Mohamed S Gomaa, Mahmoud M Elaasser, Marwa M Abdel-Aziz, Dalia H Soliman
The increased development of highly resistant bacterial strains and tuberculosis, constitute a serious public health threat, highlighting the urgent need of novel antibacterial agents. In this work, two novel series of nicotinic acid hydrazone derivatives (6a-r) and quinolone hydrazide derivatives (12a-l) were synthesized and evaluated as antimicrobial and antitubercular agents. The synthesized compounds were evaluated in vitro for their antibacterial, antifungal and antimycobacterial activities. Compounds 6f and 6p bearing the 3,4,5- (OCH3)3 and 2,5-(OCH3)2 benzylidene motifs were the most potent and as antibacterial, antifungal (MIC: 0...
July 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28699723/fermentation-isolation-purification-and-characterization-of-an-antitubercular-antibiotic-from-streptomyces-luridus-mtcc-4402
#6
S Anuradha, K Shravan Kumar, S Bhama, V Kishan
Tuberculosis, caused by Mycobacterium tuberculosis, continues to be a serious public health problem around the world, and it urges the need for development of new antitubercular drugs. An antibiotic producing strain, Streptomyces luridus (MTCC 4402) was earlier isolated from soil by our group. In this work, the phylogenic status was established by 16S rRNA gene sequence analysis. The strain was found to be active against clinically resistant strains. The culture was grown in shake flasks in a medium containing cornsteep liquor, glucose, CaCO(3), soyabean meal and starch...
September 2016: Indian Journal of Experimental Biology
https://www.readbyqxmd.com/read/28697688/plumbago-auriculata-leaf-extract-mediated-agnps-and-its-activities-as-antioxidant-anti-tb-and-dye-degrading-agents
#7
Neeraj Jaryal, Harpreet Kaur
In the present work, silver nanoparticles have been biosynthesized by utilizing the alcoholic extract of Plumbago auriculata. The optimization of reaction conditions was carried out by monitoring the reactions with the help of UV-Visible absorption spectroscopy. The characterization of AgNP was carried out by infrared spectroscopy, transmission electron microscopy and X-Ray diffraction (XRD) studies. The biogenic AgNPs were tested against Mycobacterium tuberculosis using Microplate Almar Blue assay (MABA) and their antioxidant activity was also evaluated...
July 20, 2017: Journal of Biomaterials Science. Polymer Edition
https://www.readbyqxmd.com/read/28626525/identification-of-better-pharmacokinetic-benzothiazinone-derivatives-as-new-antitubercular-agents
#8
Kai Lv, Xuefu You, Bin Wang, Zengquan Wei, Yun Chai, Bo Wang, Apeng Wang, Guocheng Huang, Mingliang Liu, Yu Lu
A series of new 8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one(BTZ) derivatives containing a C-2 nitrogen spiro-heterocycle moiety based on the structures of BTZ candidates BTZ043 and PBTZ169 were designed and synthesized as new antitubercular agents. Many of them were found to have excellent in vitro activity (MIC < 0.15 μM) against the drug susceptive Mycobacterium tuberculosis H37Rv strain and two clinically isolated multidrug-resistant strains. Compounds 11l and 11m display acceptable safety, greater aqueous solubility, and better pharmacokinetic profiles than PBTZ169, suggesting their promising potential to be lead compounds for future antitubercular drug discovery...
June 8, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28582669/qsar-driven-design-synthesis-and-discovery-of-potent-chalcone-derivatives-with-antitubercular-activity
#9
Marcelo N Gomes, Rodolpho C Braga, Edyta M Grzelak, Bruno J Neves, Eugene Muratov, Rui Ma, Larry L Klein, Sanghyun Cho, Guilherme R Oliveira, Scott G Franzblau, Carolina Horta Andrade
New anti-tuberculosis (anti-TB) drugs are urgently needed to battle drug-resistant Mycobacterium tuberculosis strains and to shorten the current 6-12-month treatment regimen. In this work, we have continued the efforts to develop chalcone-based anti-TB compounds by using an in silico design and QSAR-driven approach. Initially, we developed SAR rules and binary QSAR models using literature data for targeted design of new heteroaryl chalcone compounds with anti-TB activity. Using these models, we prioritized 33 compounds for synthesis and biological evaluation...
September 8, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28559262/metformin-adjunctive-therapy-does-not-improve-the-sterilizing-activity-of-the-first-line-antitubercular-regimen-in-mice
#10
Noton K Dutta, Michael L Pinn, Petros C Karakousis
Preliminary preclinical and observational studies suggest the potential utility of metformin as an adjunctive, host-directed agent for treatment of tuberculosis (TB). In this study, we sought to investigate the bactericidal and sterilizing activities of human-like exposures of metformin when given in combination with the first-line regimen against chronic tuberculosis in BALB/c mice. Mice receiving metformin adjunctive therapy had similar lung bacillary burdens with control mice during treatment, and the proportion of mice with microbiological relapse was similar between the two groups...
August 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28555087/strategic-incorporation-of-fluorine-in-the-drug-discovery-of-new-generation-antitubercular-agents-targeting-bacterial-cell-division-protein-ftsz
#11
Iwao Ojima, Divya Awasthi, Longfei Wei, Krupanandan Haranahalli
This article presents an account of our research on the discovery and development of new-generation fluorine-containing antibacterial agents against drug-resistant tuberculosis, targeting FtsZ. FtsZ is an essential protein for bacterial cell division and a highly promising therapeutic target for antibacterial drug discovery. Through design, synthesis and semi-HTP screening of libraries of novel benzimidazoles, followed by SAR studies, we identified highly potent lead compounds. However, these lead compounds were found to lack sufficient metabolic and plasma stabilities...
April 2017: Journal of Fluorine Chemistry
https://www.readbyqxmd.com/read/28550767/antibiotics-and-mania-a-systematic-review
#12
REVIEW
Simon Lambrichts, Lukas Van Oudenhove, Pascal Sienaert
OBJECTIVES: Mania can occur secondary to a medical condition and can be elicited by various pharmacological treatments, both in patients with or without a history of affective disorder. Antibiotic-induced mania or antibiomania is suggested to be a rare phenomenon. We reviewed the literature in order to collect published reports of antibiomania and to summarize new insights about its mechanism and management. METHODS: We performed a MEDLINE-search and used manual cross-referencing for reports of antibiotic-induced mania and included cases in which a (hypo)manic episode was diagnosed in close temporal relationship with the prescription of an antibiotic...
May 20, 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/28532916/spinal-intramedullary-tuberculosis-with-concurrent-supra-and-infratentorial-intracranial-disease-in-a-9-month-old-boy-case-report-and-review-of-the-literature
#13
REVIEW
Michael George Zaki Ghali, Visish M Srinivasan, C J Kim, Archana Malik
Tuberculous involvement of the spinal cord parenchyma is an exceedingly rare clinical entity; even more so is concurrent intracranial tuberculosis (TB). Spinal intramedullary TB presents with a characteristic subacute myelopathy, with slowly progressive paraplegia, sensory deficits, and/or bowel and bladder dysfunction. Diagnosis is strongly suspected with a clinical history of known TB in conjunction with characteristic findings on magnetic resonance imaging. Management involves multi-agent antitubercular chemotherapy without or with operative intervention...
May 19, 2017: World Neurosurgery
https://www.readbyqxmd.com/read/28527405/synthesis-and-structure-activity-relationships-of-novel-fused-ring-analogues-of-q203-as-antitubercular-agents
#14
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
#15
Sydney A Villaume, Jian Fu, Inès N'Go, Hui Liang, Huayong Lou, Laurent Kremer, Weidong Pan, Stéphane P Vincent
This study reports a novel class of inhibitors of uridine 5'-diphosphate (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 are potent inhibitors of UGM. The synthesis of novel methylated flavonoids allowed a structure-activity relationship analysis to be performed and which functional groups and structural elements were required for UGM inhibition could be determined...
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
#16
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
#17
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 25, 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
#18
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
#19
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
#20
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
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