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https://www.readbyqxmd.com/read/28818767/recent-advances-of-pyrazole-containing-derivatives-as-anti-tubercular-agents
#1
Zhi Xu, Chuan Gao, Qing-Cheng Ren, Xu-Feng Song, Lian-Shun Feng, Zao-Sheng Lv
One-third of the world's population infected tuberculosis (TB), and more than 1 million deaths annually. The co-infection between the mainly pathogen Mycobacterium tuberculosis (MTB) and HIV, and the incidence of drug-resistant TB, multi-drug resistant TB, extensively drug-resistant TB as well as totally drug-resistant TB have further aggravated the mortality and spread of this disease. Thus, there is an urgent need to develop novel anti-TB agents against both drug-susceptible and drug-resistant TB. The wide spectrum of biological activities and successful utilization of pyrazole-containing drugs in clinic have inspired more and more attention towards this kind of heterocycles...
August 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28808382/allium-sativum-constituents-exhibit-anti-tubercular-activity-in-vitro-and-in-raw-264-7-mouse-macrophage-cells-infected-with-mycobacterium-tuberculosis-h37rv
#2
Swapna S Nair, Sujay S Gaikwad, Savita P Kulkarni, Alka Pravin Mukne
BACKGROUND: Long duration of treatment, side-effects of currently used anti-tubercular drugs and emergence of drug-resistant forms of Mycobacterium tuberculosis (MTB) warrants the need to develop new drugs to tackle the scourge of tuberculosis (TB). Garlic is an edible plant reported to have anti-tubercular activity. However, previous researches on anti-tubercular effect of garlic were focused mostly on preliminary in vitro screening. OBJECTIVE: To identify constituents responsible for anti-tubercular activity of thiosulfinate-derivative rich extract of garlic (GE) and to evaluate activity of the most active constituent in RAW 264...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28791993/-morphological-signs-of-inflammatory-activity-in-different-clinical-forms-of-drug-resistant-pulmonary-tuberculosis
#3
A A Elipashev, V O Nikolsky, A S Shprykov
AIM: to determine whether the activity of tuberculous inflammation is associated with different clinical forms of drug-resistant pulmonary tuberculosis. SUBJECTS AND METHODS: The material taken from 310 patients operated on in 2010-2015 were retrospectively examined. The patients underwent economical lung resections of limited extent (typical and atypical ones of up to 3 segments) for circumscribed forms of tuberculosis with bacterial excretion. A study group consisted of 161 (51...
2017: Arkhiv Patologii
https://www.readbyqxmd.com/read/28749949/2-aminoimidazoles-potentiate-%C3%A3-lactam-antimicrobial-activity-against-mycobacterium-tuberculosis-by-reducing-%C3%A3-lactamase-secretion-and-increasing-cell-envelope-permeability
#4
Albert B Jeon, Andrés Obregón-Henao, David F Ackart, Brendan K Podell, Juan M Belardinelli, Mary Jackson, Tuan V Nguyen, Meghan S Blackledge, Roberta J Melander, Christian Melander, Benjamin K Johnson, Robert B Abramovitch, Randall J Basaraba
There is an urgent need to develop new drug treatment strategies to control the global spread of drug-sensitive and multidrug-resistant Mycobacterium tuberculosis (M. tuberculosis). The ß-lactam class of antibiotics is among the safest and most widely prescribed antibiotics, but they are not effective against M. tuberculosis due to intrinsic resistance. This study shows that 2-aminoimidazole (2-AI)-based small molecules potentiate ß-lactam antibiotics against M. tuberculosis. Active 2-AI compounds significantly reduced the minimal inhibitory and bactericidal concentrations of ß-lactams by increasing M...
2017: PloS One
https://www.readbyqxmd.com/read/28748751/update-on-nitazoxanide-a-multifunctional-chemotherapeutic-agent
#5
Anshul Shakya, Hans Raj Bhat, Surjit Kumar Ghosh
Background: The thiazolide nitazoxanide (NTZ) is a broad-spectrum anti-infective drug that adversely affects viability, growth, and proliferation of a range of extracellular and intracellular protozoan, helminths, anaerobic and microaerophilic bacteria, and viruses. Methods: Current review compiled the potential chemotherapeutic efficacy of NTZ against a variety of such disease-causing macro and/or micro-organisms as well as neoplastic cells, using various search engines viz...
July 27, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28743650/analysis-of-interactions-of-clinical-mutants-of-catalase-peroxidase-katg-responsible-for-isoniazid-resistance-in-mycobacterium-tuberculosis-with-derivatives-of-isoniazid
#6
Ameeruddin Nusrath Unissa, George Priya Doss C, Thirumal Kumar, Sukumar Swathi, Appisetty Ramya Lakshmi, Luke Elizabeth Hanna
OBJECTIVES: In order to identify good leads based on isoniazid (INH) derivatives against INH resistance, which is one of the major contributors to the emergence of multidrug-resistant (MDR) that hampers the success of tuberculosis treatment. Mutations at codon 315 in the katG gene coding for catalase-peroxidase (KatG) is the major cause for INH resistance in Mycobacterium tuberculosis(MTB). The most prevalent mutation at this codon is Ser to Thr substitution (S315T). The other substitutions include S315I, S315R, S315N and S315G...
July 22, 2017: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/28717080/addison-s-disease-caused-by-tuberculosis-with-atypical-hyperpigmentation-and-active-pulmonary-tuberculosis
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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