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Anti tuberculosis agents

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https://www.readbyqxmd.com/read/27907875/s-substituted-3-5-dinitrophenyl-1-3-4-oxadiazole-2-thiols-and-tetrazole-5-thiols-as-highly-efficient-antitubercular-agents
#1
Galina Karabanovich, Jan Němeček, Lenka Valášková, Alejandro Carazo, Klára Konečná, Jiřina Stolaříková, Alexandr Hrabálek, Oto Pavliš, Petr Pávek, Kateřina Vávrová, Jaroslav Roh, Věra Klimešová
Two new classes of antitubercular agents, namely 5-alkylsulfanyl-1-(3,5-dinitrophenyl)-1H-tetrazoles and 2-alkylsulfanyl-5-(3,5-dinitrophenyl)-1,3,4-oxadiazoles, and their structure-activity relationships are described. These compounds possessed excellent activity against Mycobacterium tuberculosis, including the clinically isolated multidrug (MDR) and extensively drug-resistant (XDR) strains, with no cross resistance with first or second-line anti-TB drugs. The minimum inhibitory concentration (MIC) values of the most promising compounds reached 0...
November 21, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27905500/targeting-intracellular-p-aminobenzoic-acid-production-potentiates-the-anti-tubercular-action-of-antifolates
#2
Joshua M Thiede, Shannon L Kordus, Breanna J Turman, Joseph A Buonomo, Courtney C Aldrich, Yusuke Minato, Anthony D Baughn
The ability to revitalize and re-purpose existing drugs offers a powerful approach for novel treatment options against Mycobacterium tuberculosis and other infectious agents. Antifolates are an underutilized drug class in tuberculosis (TB) therapy, capable of disrupting the biosynthesis of tetrahydrofolate, an essential cellular cofactor. Based on the observation that exogenously supplied p-aminobenzoic acid (PABA) can antagonize the action of antifolates that interact with dihydropteroate synthase (DHPS), such as sulfonamides and p-aminosalicylic acid (PAS), we hypothesized that bacterial PABA biosynthesis contributes to intrinsic antifolate resistance...
December 1, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27890360/anti-tubercular-peptides-a-quest-of-future-therapeutic-weapon-to-combat-tuberculosis
#3
REVIEW
Ameer Khusro, Chirom Aarti, Paul Agastian
Tuberculosis (TB) is a symbolic menace to mankind, infecting almost one third of the world's populace and causing over a million mortalities annually. Mycobacterium tuberculosis (Mtb) is the key pathogen of TB that invades and replicates inside the host's macrophage. With the emerging dilemma of multi-drug resistant tuberculosis (MDR-TB) and extensively-drug resistant tuberculosis (XDR-TB), the exigency for developing new TB drugs is an obligation now for worldwide researchers. Among the propitious antimycobacterial agents examined in last few decades, anti-tubercular peptides have been substantiated to be persuasive with multiple advantages such as low immunogenicity, selective affinity to bacterial negatively charged cell envelopes and most importantly divergent mechanisms of action...
November 2016: Asian Pacific Journal of Tropical Medicine
https://www.readbyqxmd.com/read/27866817/discovery-of-novel-n-phenyl-1-4-dihydropyridines-with-a-dual-mode-of-antimycobacterial-activity
#4
Fabian Lentz, Marc Hemmer, Norbert Reiling, Andreas Hilgeroth
There is an urgent need for novel drugs for the treatment of tuberculosis (TB) due to the increasing prevalence of antibiotic resistance among Mycobacterium tuberculosis (Mtb) strains against first-line and second-line therapeutics. We developed novel N-phenyl 1,4-dihydropyridines as potential antituberculotic agents. The observed activity depends on the substitution patterns of the aromatic residues. N-unsubstituted 1,4-dihydropyridines are known inhibitors of the cancer-relevant transmembrane efflux pump ABCB1...
December 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27853505/current-strategies-to-treat-tuberculosis
#5
REVIEW
Anthony T Podany, Susan Swindells
Tuberculosis (TB) has been a leading cause of death for more than a century. While effective therapies exist, treatment is long and cumbersome. TB control is complicated by the overlapping problems created by global inadequacy of public health infrastructures, the interaction of the TB and human immunodeficiency virus (HIV) epidemics, and the emergence of drug-resistant TB. After a long period of neglect, there is now significant progress in the development of novel treatment regimens for TB. Focusing on treatment for active disease, we review pathways to TB regimen development and the new and repurposed anti-TB agents in clinical development...
2016: F1000Research
https://www.readbyqxmd.com/read/27837427/microwave-assisted-zrsio2-catalysed-synthesis-characterization-and-computational-study-of-novel-spiro-indole-thiazolidines-derivatives-as-anti-tubercular-agents
#6
Mayuri A Borad, Manoj N Bhoi, Sanjay K Rathwa, Mahesh S Vasava, Hitesh D Patel, Chirag N Patel, Himanshu A Pandya, Edwin A Pithawala, John J Georrge
In the current investigation, we prepared a series of novel spiro[indole-thiazolidines] derivatives (5a-5h) from 5-substituted isatin derivatives and thioglycolic acid (TGA) with ZrSiO2 as an efficient catalyst under microwave irradiation. The significant merits of this protocol have some significant merits such as simplicity in operation, simple, efficient workup, good practical yields of product and the employment of recyclable catalyst. All the new synthesized scaffold has been well characterized by various spectroscopic methods and elemental analysis...
November 11, 2016: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/27817127/the-conversion-rate-of-tuberculosis-screening-tests-during-biological-therapies-in-patients-with-rheumatoid-arthritis
#7
Giovanna Cuomo, Virginia D'Abrsca, Daniela Iacono, Ilenia Pantano
Screening for active tuberculosis (TB) and latent TB infection (LTBI) is mandatory to the initiation of biological therapy in patients with rheumatic diseases. To determine the prevalence of LTBI in patients with rheumatoid arthritis before treatment with biological therapy (anti-TNF, abatacept, and tocilizumab) and the rate of TB conversion during treatment in rheumatoid arthritis (RA) patients, we evaluated the file of 275 patients with RA treated with biological agents. We considered patients with negative baseline TB screening (tuberculin skin test (TST); quantiferon TB gold in tube (QFT-GIT); chest x-ray) and with rescreening for a TB assay every year...
November 5, 2016: Clinical Rheumatology
https://www.readbyqxmd.com/read/27810467/mycobacterium-tuberculosis-drug-resistance-testing-challenges-recent-developments-and-perspectives
#8
REVIEW
T Schön, P Miotto, C U Köser, M Viveiros, E Böttger, E Cambau
Drug-resistance testing, or antimicrobial susceptibility testing (AST), is mandatory for Mycobacterium tuberculosis in cases of failure on standard therapy. We reviewed the different methods and techniques of phenotypic and genotypic approaches. Although multiresistant and extensively drug-resistant (MDR/XDR) tuberculosis is present worldwide, AST for M. tuberculosis (AST-MTB) is still mainly performed according to the resources available rather than the drug-resistance rates. Phenotypic methods, i.e. culture-based AST, are commonly used in high-income countries to confirm susceptibility of new cases of tuberculosis...
November 1, 2016: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/27809952/tuberculosis-and-transplantation
#9
José M Aguado, José Tiago Silva, Palash Samanta, Nina Singh
Mycobacterium tuberculosis is a major opportunistic pathogen in transplant recipients. Compared to that in the general population, the frequency of tuberculosis (TB) is 10 to 40 times higher in hematopoietic stem cell transplant (HSCT) recipients and 20 to 74 times higher in solid-organ transplant (SOT) recipients. Transplant recipients with TB are also more likely to develop disseminated disease, have longer time to definitive diagnosis, require more invasive diagnostic procedures, and experience greater anti-TB treatment-related toxicity than the general population...
November 2016: Microbiology Spectrum
https://www.readbyqxmd.com/read/27798208/mechanisms-of-action-and-therapeutic-efficacies-of-the-lipophilic-antimycobacterial-agents-clofazimine-and-bedaquiline
#10
REVIEW
Moloko C Cholo, Maborwa T Mothiba, Bernard Fourie, Ronald Anderson
Drug-resistant (DR)-TB is the major challenge confronting the global TB control programme, necessitating treatment with second-line anti-TB drugs, often with limited therapeutic efficacy. This scenario has resulted in the inclusion of Group 5 antibiotics in various therapeutic regimens, two of which promise to impact significantly on the outcome of the therapy of DR-TB. These are the 're-purposed' riminophenazine, clofazimine, and the recently approved diarylquinoline, bedaquiline. Although they differ structurally, both of these lipophilic agents possess cationic amphiphilic properties that enable them to target and inactivate essential ion transporters in the outer membrane of Mycobacterium tuberculosis...
October 20, 2016: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/27796146/new-antimycobacterial-agents-in-the-pre-clinical-phase-or-beyond-recent-advances-in-patent-literature-2001-2016
#11
Patricia Bento da Silva, Débora L Campos, Camila M Ribeiro, Isabel C Silva, Fernando Rogério Pavan
Tuberculosis, an infectious disease, has caused more deaths worldwide than any other single infectious disease, killing more than 1.5 million people each year; equating to 4,100 deaths a day. In the past 60 years, no new drugs have been added to the first line regimen, in spite of the fact that thousands of papers have been published on drugs against tuberculosis and hundreds of drugs have received patents as new potential products. Thus, there is undoubtedly an urgent need for the deployment of new effective drugs against tuberculosis...
October 31, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27787607/cytokine-neutralization-at-specific-cellular-source-a%C3%A2-new-therapeutic-paradigm
#12
A A Kruglov, S A Nedospasov
BACKGROUND: Currently, treatment of autoimmune diseases is based on manipulation of general control mechanisms, including those mediated by immunoregulatory cytokines. This approach is non-curative and may cause unwanted side effects due to numerous beneficial and non-redundant functions of a particular cytokine. METHODS: Techniques of reverse genetics, such as conditional gene targeting, were employed to uncover the contributions of two proinflammatory and immunomodulatory cytokines, tumour necrosis factor (TNF) and interleukin 6 (IL-6), in various disease states...
October 27, 2016: Zeitschrift Für Rheumatologie
https://www.readbyqxmd.com/read/27776583/carbapenems-against-mycobacterium-tuberculosis-a-review-of-the-evidence
#13
D Jaganath, G Lamichhane, M Shah
Carbapenems, a more recent β-lactam class, represent a unique anti-tuberculosis option, as emerging evidence demonstrates that they target the Mycobacterium tuberculosis cell wall and β-lactamase. This provides a potentially new agent against M. tuberculosis, in particular for multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis (TB), where options are limited. In this review, we examine the current evidence on the activity of carbapenems against M. tuberculosis. The predominance of work is in vitro, and suggests that carbapenems kill M...
November 2016: International Journal of Tuberculosis and Lung Disease
https://www.readbyqxmd.com/read/27750198/synthesis-and-structure-activity-studies-of-side-chain-analogues-of-the-anti-tubercular-agent-q203
#14
Sunhee Kang, Young Mi Kim, Ryang Yeo Kim, Min Jung Seo, Zaesung No, Kiyean Nam, Sanghee Kim, Jaeseung Kim
The anti-tubercular activity of 6-chloro-2-ethyl-N-(4-(4-(4-(trifluoromethoxy)phenyl)piperidin-1-yl)benzyl)imidazo [1,2-a]pyridine-3-carboxamide (Q203) is modified by varying its side chain. In this study, we synthesized Q203 analogues with different side chains and studied their effects on anti-tubercular activity. Many analogues showed good potency against M. tuberculosis replicating in liquid broth culture medium (extracellular activity) regardless of chain length and conformational changes. However, a polar character in the side chain region was unfavorable for anti-tubercular activity...
September 28, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27738913/strategies-for-the-discovery-and-development-of-new-antibiotics-from-natural-products-three-case-studies
#15
Jennifer Herrmann, Tadeja Lukežič, Angela Kling, Sascha Baumann, Stephan Hüttel, Hrvoje Petković, Rolf Müller
Natural products continue to be a predominant source for new anti-infective agents. Research at the Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) and the Helmholtz Centre for Infection Research (HZI) is dedicated to the development of new lead structures against infectious diseases and, in particular, new antibiotics against hard-to-treat and multidrug-resistant bacterial pathogens. In this chapter, we introduce some of the concepts currently being employed in the field of antibiotic discovery...
October 15, 2016: Current Topics in Microbiology and Immunology
https://www.readbyqxmd.com/read/27731818/metal-ii-complexes-of-ethambutol-as-good-enzyme-inhibitor-and-promising-antioxidant
#16
Muhammad Jahangir, Ume Farwa, Farhana Mazhar, Afza Malik, Ejaz Ahmad
Ethambutoldihydrogenchloride (EMB) with chemical formula C10H24N2O2.2HCl is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogen is substituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is an FDA approved drug and has been used for treatment of tuberculosis since 1960's. Prolong use of EMB has a side effect of visual impairment and in literature it is related with the depletion of Zn metal from the body. As it is a good chelating agent, many metal II complexes have been synthesized with anti-tubercular activity...
September 2016: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27723725/tuberculosis-is-the-landscape-changing
#17
REVIEW
Sutapa Khatua, Abby M Geltemeyer, Anand Gourishankar
Robert Heinrich Herman Koch, a German physician and microbiologist, received Nobel Prize in 1905 for identifying the specific causative agent of tuberculosis (TB). During his time it was believed that TB was an inherited disease. However he was convinced that the disease was caused by a bacterium and was infectious, tested his postulates using guinea pigs, and found the causative agent to be slow growing mycobacterium tuberculosis. TB is the second most common cause of death from infectious diseases after HIV/AIDS...
November 16, 2016: Pediatric Research
https://www.readbyqxmd.com/read/27723166/understanding-the-complications-of-anti-tnf-therapy-in-east-asian-patients-with-inflammatory-bowel-disease
#18
Jae Hee Cheon
Remarkable advances have been made in the treatment of inflammatory bowel disease (IBD) since the introduction of anti-tumor necrosis factor (TNF)-α agents, especially for patients who are refractory to or cannot tolerate conventional therapies. Currently, infliximab, adalimumab, and golimumab are available in the East Asian medical market, and these agents have been shown to be effective for inducing and maintaining long-term remission of IBD. Despite their clinical benefits, anti-TNF therapy can also lead to increased vulnerability to infections, development of autoimmune diseases and malignancy, and decreased immunogenicity of vaccinations...
October 10, 2016: Journal of Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/27699578/re-initiation-of-biologics-after-the-development-of-tuberculosis-under-anti-tnf-therapy
#19
Yesim Ozguler, Gulen Hatemi, Serdal Ugurlu, Emire Seyahi, Melike Melikoglu, Sermin Borekci, Ersan Atahan, Gul Ongen, Vedat Hamuryudan
The use of anti-TNF agents is associated with an increased risk of tuberculosis (TB) and anti-TNF agents are stopped when active TB develops. However, discontinuation of treatment can result in flare of the underlying disease. The charts of 22 patients who developed active TB among a cohort of 2754 patients using anti-TNF agents between 2001 and 2013 were reviewed retrospectively. Patients restarting biologics during further follow-up were identified. One patient with miliary TB died within 1 month. A biologic agent was restarted in 16 of the remaining 21 patients (76 %)...
December 2016: Rheumatology International
https://www.readbyqxmd.com/read/27695555/calvarial-tubercular-osteomyelitic-abscess-in-an-elderly
#20
Bhavanam Hanuma Srinivas, Megha Shantveer Uppin, Sateesh Killi, Malladi Venkata Surya Subbalaxmi, Madhusudan Patil, Alugolu Rajesh
Tuberculous osteomyelitis of skull is very rare, even in areas where tuberculosis is endemic. We herein describe an elderly woman who was apparently immunocompetent and presented with left frontal scalp swelling and right cervical lymphadenopathy. CT scan showed irregular bony destruction of the frontal bone. MRI revealed a large extradural, multiseptate, solid-cystic lesion with peripheral enhancement. FNAC from the lesion showed granulomas with caseation suggestive of tuberculosis. The lesion was debrided and she was started on anti-tubercular therapy...
October 2016: Asian Journal of Neurosurgery
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