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https://www.readbyqxmd.com/read/29243578/design-synthesis-and-in-vitro-anti-microbial-evaluation-of-ethylene-propylene-1h-1-2-3-triazole-4-methylene-tethered-isatin-coumarin-hybrids
#1
Xiaohong Jin, Yan Xu, Xuhong Yang, Xiuling Chen, Minghu Wu, Jianguo Guan, Lianshun Feng
A new class of ethylene/propylene-1H-1,2,3-triazole-4-methylene-tethered isatin-coumarin hybrids 8a-j, integrate three anti-tuberculosis pharmacophores coumarin, isatin and 1,2,3-triazole was designed and synthesized. These hybrids were assessed for their in vitro anti-TB activity against MTB H37Rv and MDR-TB, as well as anti-bacterial activity against Gram-positive and Gram-negative strains, and cytotoxicity in VERO cell line. The results showed that all hybrids with acceptable cytotoxicity (CC50: 64-512 μg/mL) exhibited weak to moderate anti-microbial activity...
December 14, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29241413/novel-missense-mutations-in-gidb-gene-associated-with-streptomycin-resistance-in-mycobacterium-tuberculosis-insights-from-molecular-dynamics
#2
Bharati Pandey, Sonam Grover, Sukriti Goyal, Salma Jamal, Aditi Singh, Jagdeep Kaur, Abhinav Grover
Streptomycin was the first antibiotic used for the treatment of tuberculosis by inhibiting translational proof reading. Point mutation in gidB gene encoding S-adenosyl methionine (SAM)-dependent 7-methylguanosine (m7G) methyltransferase required for methylation of 16S rRNA confers streptomycin (STR) resistance. As there was no structural substantiation experimentally, gidB protein model was built by threading algorithm. In this work, molecular dynamics (MD) simulations coupled with binding free energy calculations were performed to outline the mechanism underlying high-level streptomycin resistance associated with three novel missense mutants including S70R, T146M and R187M...
December 14, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29229273/mannose-functionalized-solid-lipid-nanoparticles-are-effective-in-targeting-alveolar-macrophages
#3
Ana Costa, Bruno Sarmento, Vítor Seabra
Mannose receptor is highly expressed on alveolar macrophages, being a potential target to promote the specific local drug delivery of anti-tuberculosis agents through the use of functionalized nanocarriers. In this work, isoniazid (Isn)-loaded solid lipid nanoparticles (SLN), reinforced with stearylamine (SA) were produced by double emulsion technique and further surface-functionalized with mannose in a straightforward chemical approach. Upon pre-formulation assessment, SLN close to 500 nm average size, positively charged and with association efficiency of ISN close to 50% were obtained...
December 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29227930/synthesis-and-in%C3%A2-vitro-evaluation-of-novel-substituted-isatin-propylene-1h-1-2-3-triazole-4-methylene-moxifloxacin-hybrids-for-their-anti-mycobacterial-activities
#4
Xinjia Yan, Zaosheng Lv, Jing Wen, Shijia Zhao, Zhi Xu
Twelve novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids 5a-l were designed, synthesized and screened for their in vitro anti-mycobacterial activities against drug-sensitive and multidrug-resistant Mycobacterium tuberculosis as well as cytotoxicity in VERO cell line. All hybrids exhibited excellent activities against two Mycobacterium tuberculosis strains with minimum inhibitory concentration in the range from 0.05 to 2.0 μg/mL. The most active hybrid 5i was 2-8 times more potent than the reference agents (moxifloxacin and rifampicin) in vitro against Mycobacterium tuberculosis H37Rv, while 2->2048 times more potent than the reference agents (moxifloxacin, rifampicin and isoniazid) in vitro against multidrug-resistant Mycobacterium tuberculosis...
December 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29226732/pharmacokinetics-and-pharmacogenetics-of-anti-tubercular-drugs-a-tool-for-treatment-optimization
#5
Ilaria Motta, Andrea Calcagno, Stefano Bonora
Introduction WHO global strategy is to end tuberculosis epidemic by 2035. Pharmacokinetic and pharmacogenetic studies are increasingly performed and might confirm their potential role in optimizing treatment outcome in specific settings and populations. Insufficient drug exposure seems to be a relevant factor in tuberculosis outcome and for the risk of phenotypic resistance. Areas Covered This review discusses available pharmacokinetic and pharmacogenetic data of first and second-line antitubercular agents in relation to efficacy and toxicity...
December 10, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29220797/primaquine-hybrids-as-promising-antimycobacterial-and-antimalarial-agents
#6
Kristina Pavić, Ivana Perković, Šárka Pospíšilová, Marta Machado, Diana Fontinha, Miguel Prudêncio, Josef Jampilek, Aidan Coffey, Lorraine Endersen, Hrvoje Rimac, Branka Zorc
Four series of primaquine (PQ) derivatives were screened for antitubercular and antiplasmodial activity: amides 1a-k, ureas 2a-s, semicarbazides 3a-c and bis-ureas 4a-u. Antimycobacterial activity of PQ derivatives against Mycobacterium tuberculosis (MTB), M. avium complex (MAC) and M. avium subsp. paratuberculosis (MAP) were evaluated in vitro and compared with PQ and the standard antitubercular drugs. In general, the PQ derivatives showed higher potency than the parent compound. Most of the compounds of series 1 and 2 showed high activity against MAP, comparable or even higher than the relevant drug ciprofloxacin, and weak or no activity against MTB and MAC...
December 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29205566/transglutaminase-type-2-plays-a-key-role-in-the-pathogenesis-of-mycobacterium-tuberculosis-infection
#7
I Palucci, I Matic, L Falasca, M Minerva, G Maulucci, M De Spirito, E Petruccioli, D Goletti, F Rossin, M Piacentini, G Delogu
BACKGROUND: Mycobacterium tuberculosis (MTB), the aetiological agent of tuberculosis (TB), is capable of interfering with the phagosome maturation pathway, by inhibiting phagosome-lysosome fusion and the autophagic process to ensure survival and replication in macrophages. Thus, it has been proposed that the modulation of autophagy may represent a therapeutic approach to reduce MTB viability by enhancing its clearance. OBJECTIVE: The aim of this study was to investigate whether transglutaminase type 2 (TG2) is involved in the pathogenesis of MTB...
December 4, 2017: Journal of Internal Medicine
https://www.readbyqxmd.com/read/29184888/targeting-dna-replication-and-repair-for-the-development-of-novel-therapeutics-against-tuberculosis
#8
REVIEW
Michael A Reiche, Digby F Warner, Valerie Mizrahi
Mycobacterium tuberculosis is the etiological agent of tuberculosis (TB), an infectious disease which results in approximately 10 million incident cases and 1.4 million deaths globally each year, making it the leading cause of mortality from infection. An effective frontline combination chemotherapy exists for TB; however, this regimen requires the administration of four drugs in a 2 month long intensive phase followed by a continuation phase of a further 4 months with two of the original drugs, and is only effective for the treatment of drug-sensitive TB...
2017: Frontiers in Molecular Biosciences
https://www.readbyqxmd.com/read/29184553/tumor-necrosis-factor-alpha-targeting-can-protect-against-arthritis-with-low-sensitization-to-infection
#9
Nadia Belmellat, Luca Semerano, Noria Segueni, Diane Damotte, Patrice Decker, Bernhard Ryffel, Valérie Quesniaux, Marie-Christophe Boissier, Eric Assier
Tumor necrosis factor-alpha (TNF-α) blockade is an effective treatment for rheumatoid arthritis (RA) and other inflammatory diseases, but in patients, it is associated with reduced resistance to the infectious agents Mycobacterium tuberculosis and Listeria monocytogenes, among others. Our goal was to model infection and arthritis in mice and to compare etanercept, a currently used anti-TNF-α inhibitor, to an anti-TNF-α vaccine. We developed a murine surrogate of the TNF-α kinoid and produced an anti-murine TNF-α vaccine (TNFKi) composed of keyhole limpet hemocyanin conjugated to TNF-α, which resulted in anti-TNF-α antibody production in mice...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/29174840/physicochemical-pharmacokinetic-efficacy-and-toxicity-profiling-of-a-potential-nitrofuranyl-methyl-piperazine-derivative-iiim-mcd-211-for-oral-tuberculosis-therapy-via-in-silico-in-vitro-in-vivo-approach
#10
Asmita Magotra, Anjna Sharma, Samsher Singh, Probir Kumar Ojha, Sunil Kumar, Naveen Bokolia, Priya Wazir, Shweta Sharma, Inshad Ali Khan, Parvinder Pal Singh, Ram A Vishwakarma, Gurdarshan Singh, Utpal Nandi
Recent tuberculosis (TB) drug discovery programme involve continuous pursuit for new chemical entity (NCE) which can be not only effective against both susceptible and resistant strains of Mycobacterium tuberculosis (Mtb) but also safe and faster acting with the target, thereby shortening the prolonged TB treatments. We have identified a potential nitrofuranyl methyl piperazine derivative, IIIM-MCD-211 as new antitubercular agent with minimum inhibitory concentration (MIC) value of 0.0072 μM against H37Rv strain...
November 21, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29174699/neoteric-advancement-in-tb-drugs-and-an-overview-on-the-anti-tubercular-role-of-peptides-through-computational-approaches
#11
REVIEW
Ameer Khusro, Chirom Aarti, Alberto Barbabosa-Pliego, Abdelfattah Z M Salem
Tuberculosis (TB) is a devastating threat to human health whose treatment without the emergence of drug resistant Mycobacterium tuberculosis (M. tuberculosis) is the million-dollar question at present. The pathogenesis of M. tuberculosis has been extensively studied which represents unique defence strategies by infecting macrophages. Several anti-tubercular drugs with varied mode of action and administration from diversified sources have been used for the treatment of TB that later contributed to the emergence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB)...
November 23, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29163427/antimycobacterial-and-anti-inflammatory-mechanisms-of-baicalin-via-induced-autophagy-in-macrophages-infected-with-mycobacterium-tuberculosis
#12
Qingwen Zhang, Jinxia Sun, Yuli Wang, Weigang He, Lixin Wang, Yuejuan Zheng, Jing Wu, Ying Zhang, Xin Jiang
Tuberculosis (TB) remains a leading killer worldwide among infectious diseases and the effective control of TB is still challenging. Autophagy is an intracellular self-digestion process which has been increasingly recognized as a major host immune defense mechanism against intracellular microorganisms like Mycobacterium tuberculosis (Mtb) and serves as a key negative regulator of inflammation. Clinically, chronic inflammation surrounding Mtb can persist for decades leading to lung injury that can remain even after successful treatment...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29151986/pyrrolyl-pyrazoline-carbaldehydes-as-enoyl-acp-reductase-inhibitors-design-synthesis-and-antitubercular-activity
#13
Sheshagiri R Dixit, Shrinivas D Joshi, Venkatarao H Kulkarni, Sunil S Jalalpure, Vijay M Kumbar, Tulasigiriyappa Y Mudaraddi, Mallikarjuna N Nadagouda, Tejraj M Aminabhavi
Introduction: In efforts to develop new antitubercular (anti-TB) compounds, herein we describe cytotoxic evaluation of 15 newly synthesized pyrrolyl pyrazoline carbaldehydes. Method & Materials: Surflex-Docking method was used to study binding modes of the compounds at the active site of the enzyme enoyl ACP reductase from Mycobacterium tuberculosis (M. tuberculosis), which plays an important role in FAS-II biosynthetic pathway of M. tuberculosis and also it is an important target for designing novel anti-TB agents...
2017: Open Medicinal Chemistry Journal
https://www.readbyqxmd.com/read/29118816/synthesis-of-novel-fluorene-bisamide-derivatives-via-ugi-reaction-and-evaluation-their-biological-activity-against-mycobacterium-species
#14
Ali Hossein Rezayan, Safoura Hariri, Parisa Azerang, Ghazaleh Ghavami, Isabel Portugal, Soroush Sardari
A series of new fluorene bisamide derivatives were synthesized through multi-component Ugi reaction and tested for their in-vitro anti-mycobacterial activity. The structures of the products 5a-w were deduced from their IR, 1H NMR, and 13C NMR spectra. Elemental analyses (CHN) for novel compounds (5a, 5d, 5f, 5h, 5k, 5l, 5p, 5s, 5t, 5v, 5w) was done. These compounds were evaluated as anti-bacterial agents against Mycobacterium bovis and M. tuberculosis, while their activity expressed as the minimum inhibitory concentration (MIC) in μg/mL...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/29110620/vitamins-based-novel-target-pathways-molecules-as-possible-emerging-drug-targets-for-management-of-tuberculosis
#15
Abha Sharma, Keert Jain, Swaran J S Flora
BACKGROUND: Tuberculosis (TB) is a deadly infectious disease caused by the pathogen Mycobacterium tuberculosis (M.tb). Approximately, 1.8 and 1.3 billion people are infected and die, respectively from TB each year as estimated by World Health Organization. Due to increase in the incidence of drug-resistant strains of M.tb, there is an urgent need to accelerate research which focuses on the development of new drugs with novel mechanism of action that can treat both drug-sensitive and resistant TB infections...
November 2, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29105782/toxicity-effects-of-agzno-nanoparticles-and-rifampicin-on-mycobacterium-tuberculosis-into-the-macrophage
#16
Alireza Jafari, Saeedeh Jafari Nodooshan, Roya Safarkar, Farahnaz Movahedzadeh, Nader Mosavari, Aren Novin Kashani, Mahdi Dehghanpour, Morteza Kamalzadeh, Samira Rasouli Koohi, Sara Fathizadeh, Ali Majidpour
The World Health Organization acknowledges tuberculosis as a global threat. Tuberculosis infection is one of the top 10 causes of death worldwide. Nanotechnology and microbiology researchers are looking for new and safe nano drugs for eliminating Mycobacterium tuberculosis, the causative agent of tuberculosis. In this study, AgZnO nano-crystals (AgZnONCs) is synthesized via the decomposition of the precursor of oxalate method. Characterization of AgZnONCs were evaluated. Next, various concentrations of AgZnONCs, as well AgZnONCs+Rifampicin, were prepared...
November 6, 2017: Journal of Basic Microbiology
https://www.readbyqxmd.com/read/29094039/host-directed-therapeutic-strategies-for-tuberculosis
#17
REVIEW
Afsal Kolloli, Selvakumar Subbian
Tuberculosis (TB), caused by Mycobacterium tuberculosis (Mtb), remains a leading cause of morbidity and mortality in humans worldwide. Currently, the standard treatment for TB involves multiple antibiotics administered for at least 6 months. Although multiple antibiotics therapy is necessary to prevent the development of drug resistance, the prolonged duration of treatment, combined with toxicity of drugs, contributes to patient non-compliance that can leads to the development of drug-resistant Mtb (MDR and XDR) strains...
2017: Frontiers in Medicine
https://www.readbyqxmd.com/read/29081822/southeast-asian-medicinal-plants-as-a-potential-source-of-antituberculosis-agent
#18
REVIEW
Shuaibu Babaji Sanusi, Mohd Fadzelly Abu Bakar, Maryati Mohamed, Siti Fatimah Sabran, Muhammad Murtala Mainasara
Despite all of the control strategies, tuberculosis (TB) is still a major cause of death globally and one-third of the world's population is infected with TB. The drugs used for TB treatment have drawbacks of causing adverse side effects and emergence of resistance strains. Plant-derived medicines have since been used in traditional medical system for the treatment of numerous ailments worldwide. There were nine major review publications on antimycobacteria from plants in the last 17 years. However, none is focused on Southeast Asian medicinal plants...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/29079429/antimicrobial-peptides-as-an-alternative-to-anti-tuberculosis-drugs
#19
REVIEW
Manaf AlMatar, Essam A Makky, Gülfer Yakıcı, Işıl Var, Begüm Kayar, Fatih Köksal
Tuberculosis (TB) presently accounts for high global mortality and morbidity rates, despite the introduction four decades ago of the affordable and efficient four-drugs (isoniazid, rifampicin, pyrazinamide and ethambutol). Thus, a strong need exists for new drugs with special structures and uncommon modes of action to effectively overcome M. tuberculosis. Within this scope, antimicrobial peptides (AMPs), which are small, cationic and amphipathic peptides that comprise a section of the innate immune system, are currently the leading potential agents for the treatment of TB...
October 24, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29079215/design-and-synthesis-of-indolopyridone-hybrids-as-new-antituberculosis-agents
#20
Muzafar Ahmad Rather, Faheem Rasool, Zubair Shanib Bhat, Hafiz-Ullah Dar, Mubashir Maqbool, Shajrul Amin, Syed Khalid Yousuf, Zahoor Ahmad
Tuberculosis continues to be the most dangerous infectious disease globally and need for development of new therapies is of utmost importance. In this study we describe the rationale design for synthesis using molecular hybridization and subsequent in-vitro antimycobacterial activity of various indolo-pyridone hybrid molecules against Mycobacterium tuberculosis H37Rv. A total of 16 indolo-pyridone hybrid molecules were synthesized with 85-90% yields and characterized by various spectroscopic techniques. Four compounds were ineffective with MIC >256 μg/ml (highest concentration tested), six exhibited poor activity with MIC > 100 μg/ml, four showed moderate activity with MIC > 50 μg/ml and two had notable anti-TB activity with MIC values 32 μg/ml...
October 24, 2017: Microbial Pathogenesis
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