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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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...
June 6, 2017: Clinical Rheumatology
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...
May 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28576632/the-synthesis-and-evaluation-of-triazolopyrimidines-as-anti-tubercular-agents
#10
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...
May 19, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28559525/reactivation-pulmonary-tuberculosis-in-two-patients-treated-with-pirfenidone
#11
Mohammad Khan, Majed Alghamdi, Hamdan Al-Jahdali
We report two cases of patients with biopsy-proven idiopathic pulmonary fibrosis (IPF) who were treated with new antifibrotic agent for pirfenidone for more than 12 months. Both cases developed cavitary pulmonary tuberculosis (TB) proven by positive sputum TB culture. Both cases were treated with standard anti-TB drugs for 9 months and had complete clinical and radiological resolution. To our knowledge, these are the first reported human cases of patients with IPF who have been on pirfenidone and developed cavitary pulmonary TB...
April 2017: International Journal of Mycobacteriology
https://www.readbyqxmd.com/read/28559519/phenotypic-low-level-isoniazid-resistance-as-a-marker-to-predict-ethionamide-resistance-in-mycobacterium-tuberculosis
#12
Salima Qamar, Joveria Q Farooqi, Kausar Jabeen, Rumina Hasan
BACKGROUND: Tuberculosis is one of the most prevalent diseases in Pakistan. Pakistan has the highest burden of MDR-TB in the Eastern Mediterranean region. Ethionamide is an anti-tuberculous drug frequently used to treat MDR-TB. Its drug susceptibility testing is not easily available in resource limited settings. Since it acts on the same target protein as isoniazid (inhA protein encoded by inhA gene), we sought to find out if phenotypic isoniazid resistance can be a marker of ethionamide resistance...
April 2017: International Journal of Mycobacteriology
https://www.readbyqxmd.com/read/28559515/in-silico-structure-based-drug-screening-of-novel-antimycobacterial-pharmacophores-by-dock-gold-tandem-screening
#13
Junichi Taira, Takashi Ito, Hitomi Nakatani, Tomohiro Umei, Hiroki Baba, Shotaro Kawashima, Taira Maruoka, Hideyuki Komatsu, Hiroshi Sakamoto, Shunsuke Aoki
BACKGROUND: Enzymes responsible for cell wall development in Mycobacterium tuberculosis are considered as potential targets of anti-tuberculosis (TB) agents. Mycobacterial cyclopropane mycolic acid synthase 1 (CmaA1) is essential for mycobacterial survival because of its critical role in synthesizing mycolic acids. MATERIALS AND METHODS: We screened compounds that were capable of interacting with the mycobacterial CmaA1 active site using a virtual compound library with an in silico structure-based drug screening (SBDS)...
April 2017: International Journal of Mycobacteriology
https://www.readbyqxmd.com/read/28558683/inhibition-of-biofilm-formation-in-mycobacterium-smegmatis-by-parinari-curatellifolia-leaf-extracts
#14
Benjamin Bhunu, Ruvimbo Mautsa, Stanley Mukanganyama
BACKGROUND: Tuberculosis (TB) is a serious public health problem worldwide. Mycobacterium tuberculosis (M. tuberculosis) grows as drug tolerant pellicles. Agents that inhibit biofilm formation in M. tuberculosis have the potential to reduce the disease treatment period and improve the quality of tuberculosis chemotherapy. Parinari curatellifolia (P. curatellifolia) leaf extracts are claimed to treat symptoms similar to tuberculosis in ethnomedicinal practices. Mycobacterium smegmatis (M...
May 30, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28552479/biopharmaceutic-parameters-pharmacokinetics-transport-and-cyp-mediated-drug-interactions-of-iiim-017-a-novel-nitroimidazooxazole-analogue-with-anti-tuberculosis-activity
#15
Gurleen Kour, Parvinder Pal Singh, Asha Bhagat, Zabeer Ahmed
Nitroimidazoles are emerging as a new class of therapeutic agents with potent anti-tubercular activity. CSIR-IIIM has synthesized a novel nitrohydroimidazooxazole (NHIO) analogue, IIIM-017 with a MIC of 0.37μg/ml (against H37Rv). Here, we aim at further exploration of physicochemical properties and preclinical absorption, metabolism, disposition and pharmacokinetics of IIIM-017. In this study, in silico physicochemical parameters, lipophilicity, permeability, transport, hepatotoxicity, CYP mediated drug interactions and pharmacokinetics of IIIM-017 were investigated...
May 26, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28545436/thymoquinone-tq-inhibits-the-replication-of-intracellular-mycobacterium-tuberculosis-in-macrophages-and-modulates-nitric-oxide-production
#16
Hafij Al Mahmud, Hoonhee Seo, Sukyung Kim, Md Imtiazul Islam, Kung-Woo Nam, Hyun-Deuk Cho, Ho-Yeon Song
BACKGROUND: Human tuberculosis, which is caused by the pathogen Mycobacterium tuberculosis, remains a major public health concern. Increasing drug resistance poses a threat of disease resurgence and continues to cause considerable mortality worldwide, which necessitates the development of new drugs with improved efficacy. Thymoquinone (TQ), an essential compound of Nigella sativa, was previously reported as an active anti-tuberculosis agent. METHODS: In this study, the effects of TQ on intracellular mycobacterial replication are examined in macrophages...
May 25, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28544982/an-evaluation-of-minor-groove-binders-as-anti-fungal-and-anti-mycobacterial-therapeutics
#17
Fraser J Scott, Ryan J O Nichol, Abedawn I Khalaf, Federica Giordani, Kirsten Gillingwater, Soumya Ramu, Alysha Elliott, Johannes Zuegg, Paula Duffy, Michael-Jon Rosslee, Lerato Hlaka, Santosh Kumar, Mumin Ozturk, Frank Brombacher, Michael Barrett, Reto Guler, Colin J Suckling
This study details the synthesis and biological evaluation of a collection of 19 structurally related Minor Groove Binders (MGBs), derived from the natural product distamycin, which were designed to probe antifungal and antimycobacterial activity. From this initial set, we report several MGBs that are worth more detailed investigation and optimisation. MGB-4, MGB-317 and MGB-325 have promising MIC80s of 2, 4 and 0.25 μg/mL, respectively, against the fungus C. neoformans.MGB-353 and MGB-354 have MIC99s of 3...
May 17, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28539734/honey-and-health-a-review-of-recent-clinical-research
#18
REVIEW
Saeed Samarghandian, Tahereh Farkhondeh, Fariborz Samini
Honey is one of the most appreciated and valued natural products introduced to humankind since ancient times. Honey is used not only as a nutritional product but also in health described in traditional medicine and as an alternative treatment for clinical conditions ranging from wound healing to cancer treatment. The aim of this review is to emphasize the ability of honey and its multitude in medicinal aspects. Traditionally, honey is used in the treatment of eye diseases, bronchial asthma, throat infections, tuberculosis, thirst, hiccups, fatigue, dizziness, hepatitis, constipation, worm infestation, piles, eczema, healing of ulcers, and wounds and used as a nutritious supplement...
April 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/28535545/portuguese-recommendations-for-the-use-of-methotrexate-in-rheumatic-diseases-2016-update
#19
Ana Catarina Duarte, Daniela Santos-Faria, Maria João Gonçalves, Alexandre Sepriano, Ana Filipa Mourão, Cátia Duarte, Joana Sousa Neves, Ana Filipa Águeda, Pedro Ávila Ribeiro, Alexandra Daniel, Adriano Neto, Ana Cordeiro, Ana Rodrigues, Anabela Barcelos, Cândida Silva, Cristina Ponte, Elsa Vieira-Sousa, Filipa Teixeira, Filipa Oliveira-Ramos, Filipe Araújo, Filipe Barcelos, Helena Canhão, Helena Santos, João Ramos, Joaquim Pereira, José Costa, José António Melo Gomes, Luís Cunha-Miranda, Lúcia Costa, Marcos Cerqueira, Margarida Cruz, Maria José Santos, Miguel Bernardes, Paula Oliveira, Pedro Abreu, Ricardo Figueira, Rita Barros, Sandra Falcão, Patrícia Pinto, Sofia Pimenta, Susana Capela, Vitor Teixeira, João Eurico Fonseca
BACKGROUND: Methotrexate (MTX) is the first-line drug in the treatment of rheumatoid arthritis (RA) and the most commonly prescribed disease modifying anti-rheumatic drug. Moreover, it is also used as an adjuvant drug in patients under biologic therapies, enhancing the efficacy of biologic agents. OBJECTIVES: To review the literature and update the Portuguese recommendations for the use of MTX in rheumatic diseases first published in 2009. METHODS: The first Portuguese guidelines for the use of MTX in rheumatic diseases were published in 2009 and were integrated in the multinational 3E Initiative (Evidence Expertise Exchange) project...
May 9, 2017: Acta Reumatológica Portuguesa
https://www.readbyqxmd.com/read/28527127/evaluation-of-heparg-cells-for-the-assessment-of-indirect-drug-induced-hepatotoxicity-using-inh-as-a-model-substance
#20
Anika Mann, Thomas Pelz, Knut Rennert, Alexander Mosig, Michael Decker, Amelie Lupp
HepaRG cells are widely used as an in vitro model to assess drug-induced hepatotoxicity. However, only few studies exist so far regarding their suitability to detect the effects of drugs requiring a preceding activation via the cytochrome P450 (CYP) system. A prototypic substance is the anti-tuberculosis agent INH, which is metabolized into N-acetylhydrazine, which then triggers hepatotoxicity. Therefore, the aim of the present study was to test if this effect can also be detected in HepaRG cells and if it can be counteracted by the known hepatoprotectant silibinin...
May 19, 2017: Human Cell
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