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Anti tuberculosis agents

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
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
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
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. 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...
October 10, 2016: Pediatric Research
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
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 %)...
October 3, 2016: Rheumatology International
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
Vinayak Singh, Neeraj Dhar, János Pató, Gaëlle S Kolly, Jana Korduláková, Martin Forbak, Joanna C Evans, Rita Székely, Jan Rybniker, Zuzana Palčeková, Júlia Zemanová, Isabella Santi, François Signorino-Gelo, Liliana Rodrigues, Anthony Vocat, Adrian S Covarrubias, Monica G Rengifo, Kai Johnsson, Sherry Mowbray, Joseph Buechler, Vincent Delorme, Priscille Brodin, Graham W Knott, José A Aínsa, Digby F Warner, György Kéri, Katarína Mikušová, John D McKinney, Stewart T Cole, Valerie Mizrahi, Ruben C Hartkoorn
There is an urgent need to discover new anti-tubercular agents with novel mechanisms of action in order to tackle the scourge of drug-resistant tuberculosis. Here, we report the identification of such a molecule - an AminoPYrimidine-Sulfonamide (APYS1) that has potent, bactericidal activity against M. tuberculosis. Mutations in APYS1-resistant M. tuberculosis mapped exclusively to wag31, a gene that encodes a scaffolding protein thought to orchestrate cell elongation. Recombineering confirmed that a Gln201Arg mutation in Wag31 was sufficient to cause resistance to APYS1, however, neither overexpression nor conditional depletion of wag31 impacted M...
September 28, 2016: Molecular Microbiology
Dimitrios Papaventsis, Nicola Casali, Irina Kontsevaya, Francis Drobniewski, Daniela Maria Cirillo, Vlad Nikolayevskyy
OBJECTIVES: We conducted a systematic review to determine the diagnostic accuracy of Whole Genome Sequencing (WGS) of M. tuberculosis for the detection of resistance to first and second line anti-tuberculosis (TB) drugs. METHODS: The study was conducted according to the criteria of the Preferred Reporting Items for Systematic Reviews group. A total of 20 publications were included. The sensitivity, specificity, PPV and NPV of WGS using phenotypic Drug Susceptibility Testing (DST) methods as a gold standard were determined...
September 22, 2016: Clinical Microbiology and Infection
Mohammad A Alam, Kriti Arora, Shirisha Gurrapu, Sravan K Jonnalagadda, Grady L Nelson, Paul Kiprof, Subash C Jonnalagadda, Venkatram R Mereddy
Several derivatives of aminobenzoboroxole have been prepared starting from 2-boronobenzaldehyde. All of these derivatives have been evaluated for their anti-mycobacterial activity on Mycobacterium smegmatis and cytotoxicity on breast cancer cell line MCF7. Based on these studies, all the tested molecules have been found to be generally non-toxic and benzoboroxoles with unsubstituted (primary) amines have been found to exhibit good anti-mycobacterial activity. Some of the key compounds have been evaluated for their anti-tubercular activity on Mycobacterium tuberculosis H37Rv using 7H9 and GAST media...
June 30, 2016: Tetrahedron
Garrett C Moraski, Natalie Seeger, Patricia A Miller, Allen G Oliver, Helena I Boshoff, Sanghyun Cho, Surafel Mulugeta, Jeffery R Anderson, Scott G Franzblau, Marvin J Miller
Increasing interest in the potent anti-tuberculosis activity and the novel target (QcrB) of imidazo[1,2-a]pyridine-3-carboxamides encouraged extended structure-activity relationship studies of additional scaffolds. This study reports on the in vitro profiling of the imidazo[2,1-b]thiazole-5-carboxamides as a new promising class of anti-tuberculosis compounds endowed with nanomolar potency against replicating and drug-resistant Mycobacterium tuberculosis (Mtb) as well as low toxicity to VERO cells. Compounds 6, 16, and 17 had MIC values <10 nM and toxicity >100 μM...
June 10, 2016: ACS Infectious Diseases
Lijun Song, Martijn D P Risseeuw, Matheus Froeyen, Izet Karalic, Jan Goeman, Davie Cappoen, Johan Van der Eycken, Paul Cos, Hélène Munier-Lehmann, Serge Van Calenbergh
We report the design and synthesis of a series of non-nucleoside MtbTMPK inhibitors (1-14) based on the gram-positive bacterial TMPK inhibitor hit compound 1. A practical synthesis was developed to access these analogues. Several compounds show promising MtbTMPK inhibitory potency and allow the establishment of a structure-activity relationship, which is helpful for further optimization.
November 1, 2016: Bioorganic & Medicinal Chemistry
Weijie Zhao, Meiqin Zheng, Bin Wang, Xiaopan Mu, Peng Li, Lei Fu, Shuo Liu, Zhenyong Guo
OBJECTIVES: The objectives of this study were to evaluate the interactions between linezolid (LZD) and second-line anti-tuberculosis (TB) agents in susceptible and multidrug-resistant (MDR) TB in vitro, and to validate the in vitro results in a murine TB model. METHODS: The minimum inhibitory concentrations of LZD and seven second-line anti-TB drugs against H37Rv and three multidrug-resistant clinical isolates were determined by Alamar Blue assay, and the interaction patterns of LZD and the seven second-line anti-TB agents against the four isolates were studied using a dynamic checkerboard method...
September 7, 2016: International Journal of Infectious Diseases: IJID
Lucas Noboru Fatori Trevizan, Kamilla Felipe do Nascimento, Joyce Alencar Santos, Candida Aparecida Leite Kassuya, Claudia Andrea Lima Cardoso, Maria do Carmo Vieira, Flora Martinez Figueira Moreira, Julio Croda, Anelise Samara Nazari Formagio
ETHNOPHARMACOLOGICAL RELEVANCE: The leaves of Allophylus edulis (A. St.-Hil., A. Juss. & Cambess.) Radlk. (Sapindaceae) are traditionally used as a natural anti-inflammatory agent; however, there are no scientific studies demonstrating its activity essential oil. The content of essential oil in A. edulis may be the chemical basis to explain its ethnobotanical uses, since infusions of this plant are used to treat inflammation in the traditional medicine in Brazil. AIM OF THE STUDY: This study evaluated the anti-inflammatory, antioxidant and anti-mycobacterial activities of the essential oil (EOAE) and viridiflorol, its main compound...
November 4, 2016: Journal of Ethnopharmacology
Majid Marjani, Parvaneh Baghaei, Mehdi Kazempour Dizaji, Pegah Gorji Bayani, Fanak Fahimi, Payam Tabarsi, Ali Akbar Velayati
Hepatic toxicity is the most serious adverse effect of anti-tuberculosis drugs. This study was performed to evaluate the efficacy of silymarin as a hepatoprotective herbal agent. In a randomized double blind clinical trial, 70 new cases of pulmonary tuberculosis were divided into two groups. The intervention group was assigned to receive silymarin and the control group received placebo. Tuberculosis was treated by classic regimen consisting isoniazid, rifampin, pyrazinamide and ethambutol. No statistically significant difference was found between the two groups concerning the frequency of drug induced liver injury or mild elevation of liver enzymes...
2016: Iranian Journal of Pharmaceutical Research: IJPR
Hon Chan, Seth Pearson, Cathleen M Green, Zhong Li, Jing Zhang, Georges Belfort, Alex Shekhtman, Hongmin Li, Marlene Belfort
Inteins, self-splicing protein elements, interrupt genes and proteins in many microbes, including the human pathogen Mycobacterium tuberculosis. Using conserved catalytic nucleophiles at their N- and C-termini, inteins are able to excise out of precursor polypeptides. The splicing of the intein in the mycobacterial recombinase, RecA, is specifically inhibited by the widely used cancer therapeutic cisplatin, cis-[Pt(NH3)2Cl2], and this compound inhibits mycobacterial growth. Mass spectrometric and crystallographic studies of Pt(II) binding to the RecA intein revealed a complex in which two platinum atoms bind at N- and C-terminal catalytic cysteine residues...
September 8, 2016: Journal of Biological Chemistry
Ennio Lubrano, Fabrizio Cantini, Alessandro Mathieu, Ignazio Olivieri, Carlo Salvarani, Raffaele Scarpa, Antonio Marchesoni
OBJECTIVES: Accurate diagnosis and appropriate management of psoriatic arthritis (PsA) is essential to avoid unnecessary morbidity. Our aim in this study was to evaluate the current approach to the management of PsA among rheumatologists. METHODS: A 16-item online questionnaire, produced using the Delphi method, was submitted to a panel of rheumatologists who anonymously expressed their opinions on a scale from 1 (maximum disagreement) to 5 (maximum agreement). Positive consensus was defined by ≥66% of the respondents scoring an item 3, 4 or 5...
August 31, 2016: Clinical and Experimental Rheumatology
Hongbo Shen, Feifei Wang, Gucheng Zeng, Ling Shen, Han Cheng, Dan Huang, Richard Wang, Lijun Rong, Zheng W Chen
While there is an urgent need to develop new and effective drugs for treatment of tuberculosis (TB) and multi-drug resistant TB (MDR-TB), repurposing FDA (U.S. Food and Drug Administration) -approved drugs for development of anti-TB agents may decrease time and effort from bench to bedside. Here, we employed host cell-based high throughput screening (HTS) assay to screen and characterize FDA-approved, off-patent library drugs for anti-Mycobacterium tuberculosis (MTB) activities. The cell-based HTS allowed us to identify an anti-cancer drug of bis-biguanide dihydrochloride (BBD) as potent anti-mycobacteria agent...
2016: Scientific Reports
Shaveta, Sahil Mishra, Palwinder Singh
The practice of polypharmacology is not a new concept but the approaches which are being adopted for administering the two or more drugs together are varied from time to time. Taking two or more drugs simultaneously, co-formulation of two or more active agents in a single tablet and development of hybrid molecular entities capable to modulate multiple targets are the three popular approaches for multidrug therapy. The simultaneous use of more than one drug for the chemotherapy of a single disease demands a lot of patient compliance...
August 21, 2016: European Journal of Medicinal Chemistry
Ashish Anand, Manohar V Kulkarni, Shrinivas D Joshi, Sheshagiri R Dixit
2-Propargylthiobenzimidazole 1, 4-bromomethyl coumarins/1-aza-coumarins 2/3 and sodium azide have been reacted in one pot under Click chemistry conditions to give exclusively 1,4-disubstituted triazoles 5a-n. Anti-tubercular assays against M. tuberculosis (H37Rv) coupled with in silico molecular docking studies indicated that dimethyl substituents 5c and 5d showed promising activity with higher C-score values.
October 1, 2016: Bioorganic & Medicinal Chemistry Letters
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