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Anti tuberculosis agents

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https://www.readbyqxmd.com/read/28717080/addison-s-disease-caused-by-tuberculosis-with-atypical-hyperpigmentation-and-active-pulmonary-tuberculosis
#1
Hiroki Namikawa, Yasuhiko Takemoto, Shigeto Kainuma, Sakurako Umeda, Ayako Makuuchi, Kazuo Fukumoto, Masanori Kobayashi, Shigeki Kinuhata, Yoshihiro Isaka, Hiromitsu Toyoda, Noriko Kamata, Yoshihiro Tochino, Yoshikazu Hiura, Mina Morimura, Taichi Shuto
We herein report a case of Addison's disease caused by tuberculosis characterized by atypical hyperpigmentation, noted as exacerbation of the pigmentation of freckles and the occurrence of new freckles, that was diagnosed in the presence of active pulmonary tuberculosis. The clinical condition of the patient was markedly ameliorated by the administration of hydrocortisone and anti-tuberculosis agents. When exacerbation of the pigmentation of the freckles and/or the occurrence of new freckles are noted, Addison's disease should be considered as part of the differential diagnosis...
2017: Internal Medicine
https://www.readbyqxmd.com/read/28715978/the-role-of-efflux-pumps-in-tuberculosis-treatment-and-their-promise-as-a-target-in-drug-development-unraveling-the-black-box
#2
Lindsey H M Te Brake, Gerjo J de Knegt, Jurriaan E de Steenwinkel, Teunis J P van Dam, David M Burger, Frans G M Russel, Reinout van Crevel, Jan B Koenderink, Rob E Aarnoutse
Insight into drug transport mechanisms is highly relevant to the efficacious treatment of tuberculosis (TB). Major problems in TB treatment are related to the transport of antituberculosis (anti-TB) drugs across human and mycobacterial membranes, affecting the concentrations of these drugs systemically and locally. Firstly, transporters located in the intestines, liver, and kidneys all determine the pharmacokinetics and pharmacodynamics of anti-TB drugs, with a high risk of drug-drug interactions in the setting of concurrent use of antimycobacterial, antiretroviral, and antidiabetic agents...
July 17, 2017: Annual Review of Pharmacology and Toxicology
https://www.readbyqxmd.com/read/28712709/synthesis-and-biological-evaluation-of-novel-1-2-3-triazole-derivatives-as-anti-tubercular-agents
#3
Abdul Aziz Ali, Dhrubajyoti Gogoi, Amrita K Chaliha, Alak K Buragohain, Priyanka Trivedi, Prakash J Saikia, Praveen S Gehlot, Arvind Kumar, Vinita Chaturvedi, Diganta Sarma
A library of seventeen novel 1,2,3-triazole derivatives were efficiently synthesized in excellent yields by the popular 'click chemistry' approach and evaluated in vitro for their anti-tubercular activity against Mycobacterium tuberculosis H37Ra (ATCC 25177 strain). Among the series, six compounds exhibited significant activity with minimum inhibitory concentration (MIC) values ranging from 3.12 to 0.78μg/mL and along with no significant cytotoxicity against MBMDMQs (mouse bone marrow derived macrophages)...
July 5, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28707584/a-review-of-recent-advancements-in-anti-tubercular-molecular-hybrids
#4
Parvesh Singh, Bukola Jaiyeola, Nagaraju Kerru, Oluwakemi Ebenezer, Ajay Bissessur
Tuberculosis (TB) accounts for millions of deaths worldwide every year. Diverse survival strategies adopted by Mycobacterium tuberculosis (Mtb) has substantially hindered the existing anti-TB regimen thereby leading to multidrug-resistant (MDR) and extremely drug-resistant (XDR) strains of TB. The steady decrease in current antibiotics' efficacy against these adversities is an indicator that their adequate replenishment in future is almost impossible, placing society on the precipice of a catastrophe. Over the past many years, researchers have been continuously generating new armamentarium of anti-TB drugs by tailoring the properties of available drugs or designing completely new agents...
July 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28701180/influence-of-genetic-variants-on-toxicity-to-anti-tubercular-agents-a-systematic-review-and-meta-analysis-protocol
#5
Marty Richardson, Jamie Kirkham, Kerry Dwan, Derek Sloan, Geraint Davies, Andrea Jorgensen
BACKGROUND: Tuberculosis patients receiving anti-tuberculosis treatment may experience serious adverse drug reactions, such as hepatotoxicity. Genetic risk factors, such as polymorphisms of the NAT2, CYP2E1 and GSTM1 genes, may increase the risk of experiencing such toxicity events. Many pharmacogenetic studies have investigated the association between genetic variants and anti-tuberculosis drug-related toxicity events, and several meta-analyses have synthesised data from these studies, although conclusions from these meta-analyses are conflicting...
July 13, 2017: Systematic Reviews
https://www.readbyqxmd.com/read/28697688/plumbago-auriculata-leaf-extract-mediated-agnps-and-its-activities-as-antioxidant-anti-tb-and-dye-degrading-agents
#6
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/28692915/triazole-derivatives-and-their-anti-tubercular-activity
#7
Shu Zhang, Zhi Xu, Chuan Gao, Qing-Cheng Ren, Le Chang, Zao-Sheng Lv, Lian-Shun Feng
Tuberculosis (TB) remains one of the most widespread and leading deadliest diseases, threats one-third of the world's population. Although numerous efforts have been undertaken to develop new anti-TB agents, only a handful of compounds have entered human trials in the past 5 decades. Triazoles including 1,2,3-triazole and 1,2,4-triazole are one of the most important classes of nitrogen containing heterocycles that exhibited various biological activities. Triazole derivatives are regarded as a new class of effective anti-TB candidates owing to their potential anti-TB potency...
June 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28659665/risk-of-tuberculosis-reactivation-in-patients-with-rheumatoid-arthritis-ankylosing-spondylitis-and-psoriatic-arthritis-receiving-non-anti-tnf-targeted-biologics
#8
REVIEW
Fabrizio Cantini, Carlotta Nannini, Laura Niccoli, Linda Petrone, Giuseppe Ippolito, Delia Goletti
Tuberculosis (TB) still represents an important issue for public health in underdeveloped countries, but the use of antitumor necrosis factor agents (anti-TNF) for the treatment of inflammatory rheumatic disorders has reopened the problem also in countries with low TB incidence, due to the increased risk of TB reactivation in subjects with latent tuberculosis infection (LTBI). Over the last 5 years, several non-anti-TNF-targeted biologics have been licensed for the treatment of rheumatoid arthritis, ankylosing spondylitis, and psoriatic arthritis...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28646854/treatment-delay-and-fatal-outcomes-of-pulmonary-tuberculosis-in-advanced-age-a-retrospective-nationwide-cohort-study
#9
Chih-Hsin Lee, Jann-Yuan Wang, Hsien-Chun Lin, Pai-Yang Lin, Jer-Hwa Chang, Chi-Won Suk, Li-Na Lee, Chou-Chin Lan, Kuan-Jen Bai
BACKGROUND AND OBJECTIVE: Studies focusing on pulmonary tuberculosis in advanced age (≥80 years) are lacking. This study aimed to explore treatment delay, outcomes and their predictors in this group. METHODS: Adult (≥20 years) patients with pulmonary tuberculosis were identified from the National Health Insurance Research Database of Taiwan from 2004 to 2009. Treatment completion and mortality rates were noted at one year after treatment. RESULTS: Among the 81,081 patients with pulmonary tuberculosis identified, 13,923 (17...
June 24, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/28646434/performance-of-quantiferon-%C3%A2-tb-gold-in-tube-assay-in-children-receiving-disease-modifying-anti-rheumatic-drugs
#10
Francesca Gabriele, Maria Trachana, Maria Simitsopoulou, Polixeni Pratsidou-Gertsi, Elias Iosifidis, Zoi Dorothea Pana, Emmanuel Roilides
BACKGROUND: To evaluate the performance of the Quantiferon(®)-TB Gold In-Tube (QFT-IT) interferon (IFN)-γ assay for the detection of latent tuberculosis infection (LTBI) in children receiving anti-rheumatic treatment in a tertiary referral hospital of Northern Greece. METHODS: A total of 79 consecutive children receiving anti-rheumatic treatment [of which 18 screened prior to antitumor necrosis factor (TNF)-α treatment] were tested using Mantoux tuberculin skin test (TST) and QFT-IT...
June 22, 2017: World Journal of Pediatrics: WJP
https://www.readbyqxmd.com/read/28629306/%C3%AE-ca-specific-inhibitor-dithiocarbamate-fc14-584b-a-novel-antimycobacterial-agent-with-potential-to-treat-drug-resistant-tuberculosis
#11
Ashok Aspatwar, Milka Hammarén, Sanni Koskinen, Bruno Luukinen, Harlan Barker, Fabrizio Carta, Claudiu T Supuran, Mataleena Parikka, Seppo Parkkila
Inhibition of novel biological pathways in Mycobacterium tuberculosis (Mtb) creates the potential for alternative approaches for treating drug-resistant tuberculosis. In vitro studies have shown that dithiocarbamate-derived β-carbonic anhydrase (β-CA) inhibitors Fc14-594 A and Fc14-584B effectively inhibit the activity of Mtb β-CA enzymes. We screened the dithiocarbamates for toxicity, and studied the in vivo inhibitory effect of the least toxic inhibitor on M. marinum in a zebrafish model. In our toxicity screening, Fc14-584B emerged as the least toxic and showed minimal toxicity in 5-day-old larvae at 300 µM concentration...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28625143/infection-and-malignancy-risk-in-patients-treated-with-tnf-inhibitors-for-immune-mediated-inflammatory-diseases
#12
Rui Pereira, Raquel Faria, Paula Lago, Tiago Torres
BACKGROUND: Infectious and malignant events are responsible for morbidity and mortality in patients with Immune-Mediated Inflammatory Diseases (IMIDs). Anti-tumor necrosis factor (Anti-TNF) agents appear to have an impact, however the individual effect of these agents in the different conditions is still unclear. OBJECTIVE: The goal of this study is to estimate the Incidence Rates (IR) of infections and malignancies in patients treated with anti-TNFs across different IMIDs, as well as potential risk factors...
June 15, 2017: Current Drug Safety
https://www.readbyqxmd.com/read/28621733/discovery-of-indeno-1-2-c-quinoline-derivatives-as-potent-dual-antituberculosis-and-anti-inflammatory-agents
#13
Chih-Hua Tseng, Chun-Wei Tung, Chen-Hsin Wu, Cherng-Chyi Tzeng, Yen-Hsu Chen, Tsong-Long Hwang, Yeh-Long Chen
A series of indeno[1,2-c]quinoline derivatives were designed, synthesized and evaluated for their anti-tuberculosis (anti-TB) and anti-inflammatory activities. The minimum inhibitory concentration (MIC) of the newly synthesized compound was tested against Mycobacterium tuberculosis H37RV. Among the tested compounds, (E)-N'-[6-(4-hydroxypiperidin-1-yl)-11H-indeno[1,2-c]quinolin-11-ylidene]isonicotino-hydrazide (12), exhibited significant activities against the growth of M. tuberculosis (MIC values of 0.96 μg/mL) with a potency approximately equal to that of isoniazid (INH), an anti-TB drug...
June 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28606115/peripheral-neuropathy-in-a-diabetic-child-treated-with-linezolid-for-multidrug-resistant-tuberculosis-a-case-report-and-review-of-the-literature
#14
Aravind Swaminathan, Philipp du Cros, James A Seddon, Shamsiya Mirgayosieva, Rajabov Asladdin, Zulfiya Dusmatova
BACKGROUND: Extensively drug-resistant (XDR) tuberculosis (TB) and multidrug resistant (MDR)-TB with additional resistance to injectable agents or fluoroquinolones are challenging to treat due to lack of available, effective drugs. Linezolid is one of the few drugs that has shown promise in treating these conditions. Long-term linezolid use is associated with toxicities such as peripheral and optic neuropathies. Diabetes mellitus (DM), especially when uncontrolled, can also result in peripheral neuropathy...
June 12, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/28605994/structure-based-screening-and-molecular-dynamics-simulations-offer-novel-natural-compounds-as-potential-inhibitors-of-mycobacterium-tuberculosis-isocitrate-lyase
#15
Rohit Shukla, Harish Shukla, Amit Sonkar, Tripti Pandey, Timir Tripathi
Mycobacterium tuberculosis is the etiological agent of tuberculosis in humans and is responsible for more than two million deaths annually. M. tuberculosis isocitrate lyase (MtbICL) catalyzes the first step in the glyoxylate cycle, plays a pivotal role in the persistence of M. tuberculosis, which acts as a potential target for an anti-tubercular drug. To identify the potential anti-tuberculosis compound, we conducted a structure-based virtual screening of natural compounds from the ZINC database (n = 1,67,748) against the MtbICL structure...
June 12, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28602386/respiratory-infections-associated-with-anti-tnf%C3%AE-agents
#16
REVIEW
E Blanchard, M-E Truchetet, I Machelart, J Séneschal, C Raherison-Semjen
Anti-TNFα agents have proved effective in the treatment of various inflammatory, rheumatologic, dermatologic, and gastrointestinal diseases. Severe respiratory tract infections of bacterial or fungal origin have emerged as important complications in patients receiving such treatments. The risk of infection due to anti-TNFα therapy is difficult to assess in these patients who are immunocompromised because of the underlying disease itself and of previous or concomitant immunosuppressive drugs. This excessive infection risk seems real, particularly in the first six months following treatment initiation, and higher for patients receiving anti-TNFα monoclonal antibodies than for those receiving soluble TNFα receptor...
June 8, 2017: Médecine et Maladies Infectieuses
https://www.readbyqxmd.com/read/28598559/new-structural-classes-of-antituberculosis-agents
#17
REVIEW
Vajinder Kumar, Sanjay Patel, Rahul Jain
Tuberculosis (TB), one of the deadliest diseases is shattering the health and socioeconomic status of the society. The emergence of multidrug resistant (MDR) and extremely drug resistant (XDR) strains has provided unprecedented lethal character to TB. The development of MDR and XDR strains of TB results in more deaths, longer duration of therapy, and appearance of the disease in the immunocompromised patients. Because of the development of rapid resistance by Mycobacterium tuberculosis, researchers are confronted with serious challenges in combating TB...
June 9, 2017: Medicinal Research Reviews
https://www.readbyqxmd.com/read/28589321/latent-tuberculosis-infection-and-tuberculosis-in-patients-with-rheumatic-diseases-treated-with-anti-tumor-necrosis-factor-agents
#18
Giovana Garziera, André Luis Bittencourt Morsch, Felipe Otesbelgue, Fernanda Luiza Staub, Penélope Esther Palominos, Claiton Viegas Brenol, Denise Rossato Silva
The introduction of biological agents, especially the tumor necrosis factor inhibitors (anti-TNF), for the treatment of rheumatic diseases increased the risk of developing tuberculosis (TB). Screening for latent TB infection (LTBI) is strongly recommended before starting therapy with anti-TNF agents. The objective of this study was to identify the prevalence of LTBI and TB among patients with rheumatic diseases on anti-TNF agents. This is a cross-sectional study. The electronic medical records of all adult patients (≥18 years old) undergoing anti-TNF treatment were reviewed...
August 2017: Clinical Rheumatology
https://www.readbyqxmd.com/read/28582669/qsar-driven-design-synthesis-and-discovery-of-potent-chalcone-derivatives-with-antitubercular-activity
#19
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/28576632/the-synthesis-and-evaluation-of-triazolopyrimidines-as-anti-tubercular-agents
#20
Edison S Zuniga, Aaron Korkegian, Steven Mullen, Erik J Hembre, Paul L Ornstein, Guillermo Cortez, Kallolmay Biswas, Naresh Kumar, Jeffrey Cramer, Thierry Masquelin, Philip A Hipskind, Joshua Odingo, Tanya Parish
We identified a di-substituted triazolopyrimidine with anti-tubercular activity against Mycobacterium tuberculosis. Three segments of the scaffold were examined rationally to establish a structure-activity relationship with the goal of improving potency and maintaining good physicochemical properties. A number of compounds displayed sub-micromolar activity against Mycobacterium tuberculosis with no cytotoxicity against eukaryotic cells. Non-substituted aromatic rings at C5 and a two-carbon chain connecting a terminal aromatic at C7 were preferred features; the presence of NH at C7 and a lack of substituent at C2 were essential for potency...
August 1, 2017: Bioorganic & Medicinal Chemistry
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