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Littérature scientifique sur le sujet « Antitubercular »

Auteur : Grafiati

Publié le 4 juin 2021

Mis à jour le 1 février 2022

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Articles de revues sur le sujet "Antitubercular"

Zitko, Jan, et Martin Doležal. « Old Drugs and New Targets as an Outlook for the Treatment of Tuberculosis ». Current Medicinal Chemistry 25, n^o 38 (7 janvier 2019) : 5142–67. http://dx.doi.org/10.2174/0929867324666170920154325.

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Background: Despite of the globally positive trends in the epidemiology of tuberculosis, the increasing rates of drug-resistant strains are urging to introduce new antituberculars into clinical practice. Development of a new chemical entity from hit to marketed drug is an extremely time and resources consuming process with uncertain outcome. Repurposing of clinically used drugs can be a cheaper alternative to develop new drugs effective in the treatment of tuberculosis. Objective: To extract the latest information on new mechanisms of action described or proposed for clinically used antitubercular drugs. To identify drugs from various pharmacodynamic groups as candidates for repurposing to become effective in combatting tuberculosis. Attention will be paid to elucidate the connection between repurposed drugs and new antituberculars in clinical practice or in clinical trials. Methods: Scientific databases were searched for the keywords. Results: We reviewed the latest aspects of usage and new mechanisms of action for both first-line and second-line antitubercular drugs in clinical practice. Further, we found that surprisingly large number of clinically used drugs from various pharmacodynamic groups have potential to be used in the treatment of tuberculosis, including antimicrobial drugs not typically used against tuberculosis, statins, CNS drugs (tricyclic phenothiazines, antidepressants, anticonvulsants), non-steroidal anti-inflammatory drugs, kinase inhibitors, and others (metformin, disulfiram, verapamil, lansoprazole). Repurposed drugs may become effective antituberculars, acting either by direct effects on mycobacteria or as adjunct, host-directed therapy. Conclusion: In this review, we showed that proper research of old drugs is a very efficient tool to develop new antituberculars.

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&NA;. « Antitubercular interactions reviewed ». Reactions Weekly &NA;, n^o 524 (octobre 1994) : 2. http://dx.doi.org/10.2165/00128415-199405240-00001.

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&NA;. « Modern antitubercular therapy ». Inpharma Weekly &NA;, n^o 731 (avril 1990) : 2–3. http://dx.doi.org/10.2165/00128413-199007310-00004.

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HUSAIN, Asif, Aftab AHMAD, Anil BHANDARI et Veerma RAM. « ANTITUBERCULAR ACTIVITY OF SOME NEWER 6-PYRIDAZINONE DERIVATIVES ». SOUTHERN BRAZILIAN JOURNAL OF CHEMISTRY 19, n^o 19 (20 décembre 2011) : 17–23. http://dx.doi.org/10.48141/sbjchem.v19.n19.2011.22_2011.pdf.

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Two series of 6-pyridazinone derivatives (17-30) were synthesized and evaluated for antitubercular activities against the Mycobacterium tuberculosis H37Rv strain. The results indicated that among the synthesized compounds, 5-( 4-hydroxy-3-methoxybenzyl}-3-phenyl-1,6-dihydro-6-pyridazinone (23) showed good antitubercular activity. Three more compounds, (18, 25 & 27) were significant in their antitubercular action. The present study reveals the antitubercular potential of 6-pyridazinones.

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Kar, Sidhartha S., et Cinu A. Thomas. « Strategically Placed Trifluoromethyl Substituent in the Realm of Antitubercular Drug Design ». Current Drug Therapy 14, n^o 2 (27 août 2019) : 114–23. http://dx.doi.org/10.2174/1574885513666180906101732.

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Background:Fluorinated substituents have played, and continue to play an important role in antitubercular drug design. Nonetheless, previous works have indicated that organofluorines like –F, CF3, -OCF3, and CHF2 etc have been used to modulate the pharmacodynamic and pharmacokinetic behaviour of antitubercular agents. Among the fluorinated groups, trifluoromethyl (-CF3) substituent is a very familiar pharmacophore used widely in antitubercular research.Objective:This review assesses the development of selected trifluoromethyl group bearing antitubercular agents that are either in treatment or considered to be potential. The prime objective of the present investigation was to provide initial evidences for the hypothesis that addition of trifluoromethyl group to antiTB agents could improve their potency. We also aimed to contribute to a better understanding of the role of trifluoromethyl group on drug-likeness antitubercular activity.Methods:In this review, we first brief out the possible effect of –CF3 substituent on pharmacodynamic and pharmacokinetic properties of drugs. Next, we turn to emphasize on the effect of trifluoromethyl substituent on different antitubercular scaffolds. Finally, we open the topic for the researchers to design potential antitubercular agents suitably substituted with fluorinated groups.Results:This review suggests that the replacement of –CF3 group in heterocyclic as well as phenyl ring led to the improvement in pharmacodynamic and pharmacokinetic properties of the compounds. Hence it's not surprising to see –CF3 group emerging as an alternative electron withdrawing group instead of halogens in many promising antitubercular agents.Conclusion:This unusual spectrum of advantage allied with its lipophilicity enhancing effect, made –CF3 group distinct from other substituents in modern antitubercular drug design. The present study provides conceptual advances to the understanding of the physicochemical properties of –CF3 group and its effect on antitubercular activity.

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K, Ishwar Bhat, et Abhishek Kumar. « PYRAZOLINES AS POTENT ANTITUBERCULAR AND CYTOTOXIC AGENTS ». Asian Journal of Pharmaceutical and Clinical Research 10, n^o 6 (1 juin 2017) : 247. http://dx.doi.org/10.22159/ajpcr.2017.v10i6.17344.

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Objective: Pyrazolines are known to exhibit different biological and pharmacological properties such as anticancer, antibacterial, antifungal and antitubercular activities. Chalcones with an enone group between two aromatic rings exhibit remarkable pharmacological activities such as antiinflammatory, antibacterial, antitumor, antifungal, and antimalarial activity. A series of pyrazolines from chalcones have been synthesized and evaluated for antitubercular and cytotoxic activity studies.Methods: Chalcones [3-substituted phenyl-1-(p-tolyl)prop-2-en-1-one] were synthesized from various substituted aldehydes and 4-methyl acetophenone and cyclized into pyrazolines [5-substituted phenyl-3-(p-tolyl)-4,5-dihydro-1H-pyrazole] using hydrazine hydrate. Antitubercular and cytotoxic activity studies were carried out.Results: Antitubercular and cytotoxic activity studies of synthesized pyrazoline revealed that some compounds have showed promising activity.Conclusion: The observed results proved that pyrazolines are found to be interesting lead molecules for further synthesis as antitubercular and cytotoxic agents.

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Bakshi, S., M. Kaur, N. Saini, AA Mir, A. Duseja, SK Sinha et S. Sharma. « Altered expressions of circulating microRNAs 122 and 192 during antitubercular drug induced liver injury indicating their role as potential biomarkers ». Human & ; Experimental Toxicology 40, n^o 9 (17 mars 2021) : 1474–84. http://dx.doi.org/10.1177/0960327121997975.

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Drug induced liver toxicity is a serious health complication leading to high mortality rates and post marketing withdrawal of drugs. Although considered to be the gold standard biomarkers; aspartate aminotransferase, alanine aminotransferase, total bilirubin and alkaline phosphatase have been found to have specificities beyond liver, therefore more specific and predictive markers for the detection of antitubercular drug mediated liver damage are required. Unfortunately, the effectiveness of currently used first line antitubercular drugs namely isoniazid, rifampicin, pyrazinamide is often accompanied with liver injury, impeding the cure of patients. Keeping in view, the prognostic and diagnostic applications of microRNAs in various diseases, we tried to assess the importance of microRNAs 122 and 192 in antitubercular drug associated liver injuries. The study included subjects having tuberculosis of any type with antitubercular drug induced liver injury; naïve or newly diagnosed tuberculosis patients, tuberculosis patients on drugs not having toxicity and healthy controls. Observations from this study revealed that expression levels of miR-122 and miR-192 were significantly decreased in the serum of antitubercular drug induced liver injury patients only. Therefore, these microRNAs or the pathways associated with them can be used as a tool to predict or cure antitubercular drug associated liver injury in future.

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Durand, Francois, Gilles Jebrak, Dominique Pessayre, Michel Fournier et Jacques Bernuau. « Hepatotoxicity of Antitubercular Treatments ». Drug Safety 15, n^o 6 (décembre 1996) : 394–405. http://dx.doi.org/10.2165/00002018-199615060-00004.

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Wang, Lishu, Jungfeng Wang, Juan Liu et Yonghong Liu. « Antitubercular Marine Natural Products ». Current Medicinal Chemistry 25, n^o 20 (14 juin 2018) : 2304–28. http://dx.doi.org/10.2174/0929867324666170113120221.

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Due to the importance of nature as a source of new drug candidates, the purpose of this article is to emphasize the marine natural products, which exhibit antitubercular activity, published between January 2000 and May 2016, with 138 quotations to 250 compounds obtained from marine resources. These metabolites are organized by chemical constitution and named as simple alkyl lipids derivatives, aromatics derivatives, peptides, alkaloids, terpenoids, steroids, macrolides, and polycyclic polyketides.

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de Oliveira Viana, Jessika, Hamilton Mitsugu Ishiki, Marcus Tullius Scotti et Luciana Scotti. « Multi-Target Antitubercular Drugs ». Current Topics in Medicinal Chemistry 18, n^o 9 (31 juillet 2018) : 750–58. http://dx.doi.org/10.2174/1568026618666180528124414.

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Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis, which has high levels of mortality worldwide and has already gained resistance to first- and second-line drugs. The study by new chemical entities with promising activities becomes paramount to broaden the therapeutic strategies in the cure of the patients affected with this disease. In this context, in this review we report the discovery of 3 classes of compounds that can simultaneously interact with more than one target of Mycobacterium tuberculosis.

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Thèses sur le sujet "Antitubercular"

Li, Jinjing. « Supramolecular modification of selected antitubercular drugs ». Doctoral thesis, University of Cape Town, 2010. http://hdl.handle.net/11427/10906.

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The author's objective was to prepare new solid phases of the antitubercular drug isoxyl [specifically polymorphs, solvates, cyclodextrin (CD) inclusion complexes and cocrystals] and to isolate and characterise a range of solvated forms of the rifamycin antibioticsrifampicin and rifaximin.

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Jin, Wentao. « Antimicrobial and antitubercular natural products from polypore mushrooms / ». Full text available from ProQuest UM Digital Dissertations, 2006. http://0-proquest.umi.com.umiss.lib.olemiss.edu/pqdweb?index=0&did=1383464621&SrchMode=1&sid=2&Fmt=2&VInst=PROD&VType=PQD&RQT=309&VName=PQD&TS=1217354515&clientId=22256.

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Chigutsa, Emmanuel. « Population pharmacokinetics and pharmacokinetic-pharmacodyamic modeling of antitubercular drugs ». Doctoral thesis, University of Cape Town, 2013. http://hdl.handle.net/11427/3275.

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The pharmacokinetics of rifampicin, isoniazid, pyrazinamide and ethambutol in 78 patients with tuberculosis were described using non-linear mixed effects modeling. Pharmacodynamic data was comprised of weekly sputum liquid culture (using mycobacterial growth indicator tubes) time to detection results from 144 patients during the first 2 months of treatment. The effect of drug exposure on patient outcomes was investigated. To determine the adequacy of ofloxacin drug exposure, the probability of attaining the required area-under-the-curve to minimum inhibitory concentration ratio (AUC/MIC) of ofloxacin was determined in 65 patients on treatment for multidrug resistant tuberculosis. To improve efficiency in the clinical development of new drug regimens, clinical trial simulation was used to determine the optimal study design for a study investigating the efficacy of a new antitubercular drug regimen. The SLCO1B1 rs4149032 polymorphism existed at a high frequency of 0.70 in South Africans and resulted in a 28% decrease in bioavailability of rifampicin. The rifampicin peak concentration was a significant predictor of the 2 month treatment outcomes. A semimechanistic time to event model was developed to analyze days to positivity (time to detection) data. The model was comprised of a biexponential decay model describing bacillary decline in sputum from patients, followed by a logistic model with a lag time for growth of the mycobacteria in liquid culture. For the current 800 mg daily dose of ofloxacin, the probability of attaining an AUC/MIC target ratio of at least 100 was only 0.45. Based on clinical trial simulation, the optimum parallel study design was comprised of 125 study participants in each of 2 arms to achieve a study power of at least 80%. Increasing the study length beyond 42 days reduced study power perhaps due to increased amounts of censored data. Higher doses of rifampicin are required in the majority of South African patients with tuberculosis. A novel pharmacodynamic model of tuberculosis treatment is presented, which can be used for investigation of covariates such as drug exposure. Ofloxacin should be replaced with a more potent fluoroquinolone for treatment of multidrug resistant tuberculosis. Clinical trials should not be unduly long otherwise this may compromise study power.

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Hans, Renate Hazel. « Novel Antimalarial and Antitubercular Agents Based on Natural Products ». Doctoral thesis, University of Cape Town, 2009. http://hdl.handle.net/11427/6311.

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Malaria and tuberculosis are listed among the major infectious diseases. They are responsible for severe morbidity and mortality especially in resource-poor settings where control interventions are inaccessible, unaffordable and plagued by widespread resistance. According to current estimates, malaria afflicts over 40% of the worldâs population and claims the lives of 1-3 million annually. The epidemiology of tuberculosis is just as grim. About one third of the world population is reported to be infected with Mycobacterium tuberculosis and it is responsible for 2-3 million deaths annually. Of particular interest to this project, is the fact that natural products have always been on the frontline in the battle against these diseases, that is, most of the clinically used drugs in antimalarial and antitubercular chemotherapy are of natural product-origin. In this project we therefore focussed on the design, synthesis, characterization and biological evaluation of novel antimalarial and antitubercular agents obtained by synthetically hybridizing and decorating scaffolds based on natural products or derivatives - with a history in the aforementioned disease models. Scaffolds selected include the thiolactone ring system, a key intermediate of the natural product thiolactomycin, the non-peptidic natural product isatin and the chalcone scaffold. In this way a series of hybrids were constructed which can be subdivided into three main groups: (i) thiolactone-isatin hybrids, (ii) -amino alcohol thiolactone-chalcone and isatin-chalcone hybrids, and (iii) dihydroartemisinin-isatin, dihydroartemisinin-chalcones and other miscellaneous hybrids. These were evaluated for antiplasmodial activity against the chloroquine resistant (W2) and chloroquine sensitive (D10) strains of Plasmodium falciparum as well as for inhibitory activity against cysteine proteases. Evaluation of antimycobacterial activity of the synthesized compounds against the drug sensitive H37Rv strain of M. tuberculosis was also undertaken. (i) For the first group of hybrids we used the C-4 hydroxyl group of the thiolactone ring as a handle for functionalization by attaching it via a variable, non-hydrolyzable alkyl linker to the isatin scaffold. Most striking, is the operational simplicity of the synthesis methodology employed and how it led to the discovery of a novel tetracyclic ring system. Identified from the latter is the compound 3.8p which is the most active antimalarial from this series with an IC50 of 6.92 Î¼M in the W2 strain. Some of the hybrids (3.7 and 3.8) were more active than the monomers and the parent drug thiolactomycin, thus demonstrating the potential of hybridization as a drug discovery tool. Antimalarial structure activity relationships for the novel tetracycles 3.8 revealed the importance of substitution at C-5 of the isatin scaffold and vi the need for increased lipophilicity. Although the antitubercular activity of the hybrids was inferior compared to the control drugs, a number of advanced intermediates were identified which displayed promising activity against both fast growing and slow-growing, persistent forms of M. tuberculosis. (ii) The second group of hybrids consisted of a 36-member library obtained by the covalent linkage of methoxylated chalcones with the thiolactone ring and the isatin scaffold. Incorporated in their design is the -amino alcohol moiety, a known bioactiphore. For the synthesis of these hybrids we employed the copper-catalyzed Huisgen 1,3-dipolar cycloaddition reaction (also know as âclickâ chemistry) which in addition to expediting structure activity relationship studies yielded the 1,2,3-triazole ring system. The antiplasmodial results showed that the thiolactone-chalcones, with IC50s ranging from 0.68 to 6.08 Î¼M, were more active against the W2 strain than the isatin-chalcones (IC50 = 2.09 - 14.90 Î¼M). More so, structure activity relationships delineated for the former indicated the preference for triOMe substitution on ring A of the chalcone scaffold. The most active compound for this series 4.14f [IC50 = 0.68 Î¼M (W2)] is 10-fold less active than chloroquine but has a greater efficacy than the parent natural product thiolactomycin. Results obtained for cysteine protease activity showed that the isatin-chalcone hybrids inhibited falcipain-2 activity, whereas the thiolactone-chalcone hybrids were devoid of enzyme inhibitory activity. With regard to antitubercular activity, the advanced intermediates were more active than the hybrid constructs. The most promising antitubercular agent identified is the acetylenic chalcone 4.10f (MIC = 13.1 Î¼M) which is 2-fold more active than one of the controls, moxifloxacin (MIC = 31.1 Î¼M) against the slow-growing persistent forms of M. tuberculosis. (iii) The final group of compounds is a limited series of semi-synthetic artemisinin analogues obtained by hybridizing the first generation analogue, dihydroartemisinin with previously mentioned scaffolds (isatin, chalcones, thiolactone) and other biologically relevant scaffolds such as the 4-aminoquinoline unit and azidovudine (AZT). As with the previous series we utilized the âclickâ reaction to effect the synthesis of these hybrids. The most active compound identified is the intermediate 5.4 [IC50 = 6.13 nM (W2)] which is more active than the parent natural product artemisinin [IC50 = 10.84 nM (W2)], 16 times more active than chloroquine and 2-times less active than dihydroartemisinin. The lack of antitubercular activity of compounds in this series moreover confirmed the antimalarial specificity of artemisinin analogues.

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Xu, Jun. « Research on the post-PKS modification steps of rifamycin B biosynthesis in Amycolatopsis mediterranei S699 / ». Thesis, Connect to this title online ; UW restricted, 2005. http://hdl.handle.net/1773/11532.

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Krajewski, Wojciech W. « Structural Studies of Glutamine Synthetases – Towards the Development of Novel Antitubercular Agents ». Doctoral thesis, Uppsala universitet, Strukturell molekylärbiologi, 2008. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-9286.

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Glutamine synthetase (GS) plays an important role in nitrogen metabolism, where it catalyzes the ATP-dependent condensation of glutamate and ammonia to yield glutamine. Recent studies showed the importance of M. tuberculosis GS (MtGS) for growth and survival of the bacterium, and demonstrated its potential as a drug target. This thesis presents structural studies of MtGS and mammalian GSs, which are aimed at identifying and developing novel inhibitors against the mycobacterial target. The structure of MtGS was solved in complex with a phosphorylated form of the inhibitor methionine sulfoximine, magnesium and ADP. The complex structure provides a detailed picture of the active site, offering several insights into catalysis and inhibition, as well as forming a solid basis for structure-based drug design. The apo canine GS and liganded human GS structures described in this thesis represent the first structures of the mammalian enzymes. Comparison of the structures revealed substrate-induced conformational changes. Inspection of the nucleotide-binding site showed that it differs from that of MtGS, thus offering good opportunities to design specific and selective inhibitors of the mycobacterial enzyme. The amino acid-binding site of MtGS was evaluated as a target for inhibition, using a combination of a literature survey, structure-based virtual screening and the synthesis of a small library of compounds. As a result, several new inhibitors of MtGS could be identified. Finally, the structural basis for inhibition of MtGS by a purine analogue (PA) is provided. PA, an analogue of a class of compounds found to inhibit MtGS in a high-throughput screening assay, targets the nucleotide-binding site. The architecture of the HsGS nucleotide-binding site indicates that PA would not be able to bind to the human enzyme, offering good prospects for selective inhibition of MtGS.

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Jamadar, Abeda. « Copper(II) and Zinc(II) complexes of aroyl hydrazones as potential antitubercular agents ». Thesis, University of York, 2012. http://etheses.whiterose.ac.uk/3099/.

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There is a continuing need to make new antitubercular drugs due to development of resistance towards present drugs. To do this, series of pyruvate hydrazones (PVAHs) and their respective Cu(II) complexes and Zn(II) complexes were synthesized and fully characterised. Variable temperature NMR studies of PVAHs indicate the presence of E and Z isomers in the solution. Determination of the obtained single crystal X-ray structures reveals that Cu(II) ion binds to PVAH ligand in 1:1 ratio resulting in square pyramidal geometry in most of the Cu(II) complexes, whereas Zn(II) ion binds to two PVAH ligands in 1:2 ratio giving rise to octahedral geometry. The electrochemical studies of Cu(II) complexes of PVAH performed using cyclic voltammogram indicate the presence of quasi-reversible behaviour assigned to a Cu2+/Cu1+ peak potential. This indicates structural reorganisation of Cu(II) square pyramidal geometry towards Cu(I) tetrahedral geometry. The tetrahedral geometry of a synthesized Cu(I) complex of PVAHs was confirmed by X-ray crystal structure. The stability studies of selected PVAH ligands and their metal complex indicate that the investigated compounds were stable in extreme basic conditions, but they were unstable in extreme acidic conditions due hydrolysis of azomethine bond. However, stability of these compounds in physiological conditions, i.e. in PBS buffer, reveals that ligand hydrolyses slowly over a period of time, whereas the Cu(II) complex remains quite stable over a monitored period of 120 hours. Interestingly, dihydrazide analogue of PVAH was fairly stable in PBS buffer. EPR studies of investigated Cu(II) complexes in DMSO indicate that PVAHs remains strongly coordinated to Cu(II) centre. The evaluation of the antimycobacterial activity showed that the anionic PVAHs and Zn(II) complexes are essentially inactive. Some of the corresponding neutral Cu(II) complexes, however, exhibit promising antimycobacterial activities if tested under high iron (8 μg Fe per mL) conditions. As observed for the related antimycobacterial agent isoniazid, the activity of the complexes decreases if the M. tuberculosis cells are grown under low iron (0.02 μg Fe per mL) conditions. The Cu(II) complexes may thus have a similar mode of action and may require an iron-containing heme-dependent peroxidase for activation. A series hydrophobic cinnamaldehyde hydrazones (CAHs) and their Cu(II) complexes were also synthesized and tested for their antitubercular activity under similar conditions to that of PVAH series. But they failed to show any inhibitory activity due to their poor cellular uptake owing to their limited solubility in aqueous buffer.

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Semenya, Manare Molahlegi Dorothy. « Non-Neuroleptic Antitubercular and Anticancer Therapeutics through Rational Drug Remodelling of Phenothiazines and Related Antipsychotics ». Thesis, Faculty of Science, 2021. http://hdl.handle.net/11427/33391.

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In light of shrinking pharmaceutical drug pipelines and drug resistance, innovative drug discovery strategies are of imperative need. Drug repurposing and related strategies such as drug rescue and drug remodelling have garnered significant research interest. Various clinically approved non-antibiotics including phenothiazines hold promise as novel classes of therapeutics in other indications. However, in addition to inherent neuroleptic properties, phenothiazines and related antipsychotics elicit adverse side effects at clinically relevant doses thus precluding their extensive clinical application. Herein, it was postulated that the selectivity of phenothiazines and related drugs for nonneuroleptic indications could be enhanced through rationalized structural remodelling. Phenothiazine and related neuroleptics are known to obey a lipophilic chromophore/basic side chain paradigm. Deviation from this paradigm is expected to decrease potential for neuroleptic effects. Therefore, the remodelling strategies involved introduction of novel functionalities that are dissimilar to native phenothiazine structures. Prior to chemical synthesis, drug metabolism and pharmacokinetic related properties were predicted in silico to assess drug-likeness of the new chemical entities derived from phenothiazines and related antipsychotics. The in silico profiling also included prediction of blood/brain partition coefficients and CNS activity to determine their likelihood of exhibiting neuroleptic effects. The new chemical entities were then evaluated against drug-susceptible Mycobacterium tuberculosis-H37Rv. Furthermore, a selected series was screened for binding to dopamine and serotonin receptors to corroborate in silico CNS activity predictions. Moreover, pharmacokinetic studies were conducted with the selected series to determine in vitro microsomal stability, kinetic solubility and in vivo toxicity profiles. Another objective of this study was to evaluate the new chemical entities for their potential as anticancer agents. The key findings herein demonstrated that it is possible to abolish neuroleptic effects through rationalized structural manipulation and still retain bio-activities of interest. Several new chemical entities including N-alkylsulfonates (DS0031, DS0032, DS0034, DS0035, DS00366) and nitrobenzenesulfonamides (DS00325, DS00326, DS00329) of phenothiazines, displayed notable antitubercular (GAST/Fe MIC90 range: 9.9-125 µM; 7H9 MIC range 12.5- 25 µg/mL) and anticancer (IC50 range 4.51-12.43 µM) activities in comparison to native phenothiazine drugs. Furthermore, in vitro and in vivo preclinical evaluation revealed favourable pharmacokinetic profiles. Overall, this study presents novel subclasses of phenothiazines that hold promise for further development as non-neuroleptic agents in either tuberculosis or cancer treatment regimens.

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Muthas, Daniel. « Development and Application of Computational Methods in Antitubercular Drug Design : Identification of Novel Inhibitors of Ribonucleotide Reductase ». Doctoral thesis, Uppsala universitet, Avdelningen för organisk farmaceutisk kemi, 2009. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-99173.

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Tuberculosis kills approximately 1.7 million people each year around the world making it one of the most lethal infectious diseases. This thesis concerns the development of two computational tools that can support the early stages of drug discovery, and their use in an anti-tubercular drug discovery program. One of the tools developed is a statistical molecular design (SMD) approach that generates information-rich libraries biased towards a lead structure. The other metod is a post-filtering technique to increase the success of virtual screening, has also been developed. Both methods have been validated using literature data. Ribonucleotide reductase (RNR) has been identified as a potential anti-tubercular target, and our focus has been to develop small-molecule inhibitors of this target. The enzyme consists of two subunits (a large R1 and a small R2 subunit) that have to associate in order to generate a bioactive complex. It had previously been shown that a heptapeptide corresponding to the small R2 subunits C-terminal inhibited the enzyme. In order to investigate the requirements for inhibitory effect of the peptide a library was designed using the developed SMD approach. The designed library was synthesized and evaluated for biological activity and an OPLS-DA model was derived to understand which positions were most important for activity. In order to identify small-molecule inhibitors of RNR a combined shape- and structure-based virtual screen was performed, employing ROCS, GlideXP and the developed post-filtering technique. Starting from a library of 1.5 million compounds 24 was acquired and evaluated for enzymatic activity. The best compounds were almost as potent as the starting peptide, but considerably more drug-like.

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Tiong, John. « Discovery of novel antibacterial and antitubercular compounds using chemical genetics and computational approach targeted at phospholipid biosynthesis ». Thesis, University of Strathclyde, 2012. http://oleg.lib.strath.ac.uk:80/R/?func=dbin-jump-full&object_id=18676.

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Bacterial membranes undergo dynamic rearrangements during cell division with lateral heterogeneity in phospholipid distribution. An understanding of the synthesis of the cell membrane can provide a basis for the rational design of new antibacterial compounds which will ultimately be developed towards potential new antibiotics. Mounting evidence is implicating the importance of phospholipid in the viability of mycobacteria. The genetically tractable and related organism, Streptomyces coelicolor represents an ideal model for analogous studies on Mycobacteria tuberculosis for the purpose of designing novel classes of anti-tuberculosis drugs targeting the phospholipid biosynthesis pathways. Genetic and biochemical studies carried out on phosphatidylserine synthase (Pss) and phosphatidylserine decarboxylase (Psd) demonstrated the essentiality of these membrane proteins in S. coelicolor. Alteration of pss expression affects the overall growth and morphology of S. coelicolor (i.e. hyphal growth, branching, septation and sporulation) therefore verified the potential of these proteins as drug targets. Although, the early stage "hit identification" approach using a modest collection of compounds was unsuccessful, further screening of relevant compounds should continue. Structural modifications should be carried out on some of the initial compounds which were devoid of antibacterial activity in order to address the possible pharmacodynamic issues. Protein X-ray crystallography or saturation transfer difference - nuclear magnetic resonance (STD-NMR) spectroscopy of these proteins should also be considered in the event of further futile attempts.

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Livres sur le sujet "Antitubercular"

Deloitte & Touche. Department for International Development, Zambia health and population sector aid : Report on distribution audits, destination checks, and usage assessment for TB drugs. Lusaka] : Deloitte Touche Tohmatsu, 2000.

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Wiegandt, Axel. Framework to address multi-drug-resistant TB in the Pacific island countries and territories. Noumea, New Caledonia : Secretariat of the Pacific community, 2010.

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Antituberculosis chemotherapy. Basel : Karger, 2011.

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Crofton, John Wenman. Guidelines for the management of drug-resistant tuberculosis. Geneva : World Health Organization, 1997.

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Canada, Canada Health. Tuberculosis : Drug resistance in Canada, 2003 : reported susceptibility results of the Canadian Tuberculosis Laboratory Surveillance System. [Ottawa] : Health Canada, 2004.

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World Health Organization (WHO). Treatment of tuberculosis : Guidelines. 4^e éd. Geneva : World Health Organization, 2010.

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Nguy, Shui. Drug-resistant tuberculosis : Causes, diagnosis, and treatments. Sous la direction de K'ung Zhou. Hauppauge NY : Nova Science Publishers, 2009.

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World Health Organization (WHO). Management of MDR-TB : A field guide, a companion document to Guidelines for the programmatic management of drug-resistant tuberculosis. Geneva : World Health Organization, 2009.

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McHugh, Timothy D. Tuberculosis : Laboratory diagnosis and treatment strategies. Oxfordshire : CAB International, 2013.

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The global threat of drug-resistant TB : A call to action for World TB Day : briefing and hearing before the Subcommittee on Africa and Global Health of the Committee on Foreign Affairs, House of Representatives, One Hundred Tenth Congress, first session, March 21, 2007. Washington : U.S. G.P.O., 2007.

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Plus de sources

Chapitres de livres sur le sujet "Antitubercular"

Barber, Peter G., William M. Goldman, Annette J. Stahl Avicolli, Rosemary Smith, Neal Rairden, Octavio Maragni, Jeneane Chirico et Constance Mangone. « Antitubercular drugs ». Dans Tuberculosis, 252–94. Boston, MA : Springer US, 1995. http://dx.doi.org/10.1007/978-1-4899-2869-6_11.

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Basso, Luiz A., et John S. Blanchard. « Resistance to Antitubercular Drugs ». Dans Resolving the Antibiotic Paradox, 115–44. Boston, MA : Springer US, 1998. http://dx.doi.org/10.1007/978-1-4615-4897-3_7.

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Ibrahim, Mariam, et Lucila Garcia-Contreras. « Preclinical Pharmacokinetics of Antitubercular Drugs ». Dans Drug Delivery Systems for Tuberculosis Prevention and Treatment, 131–55. Chichester, UK : John Wiley & Sons, Ltd, 2016. http://dx.doi.org/10.1002/9781118943182.ch7.

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Buttini, Francesca, et Gaia Colombo. « Formulation Strategies for Antitubercular Drugs by Inhalation ». Dans Drug Delivery Systems for Tuberculosis Prevention and Treatment, 197–212. Chichester, UK : John Wiley & Sons, Ltd, 2016. http://dx.doi.org/10.1002/9781118943182.ch10.

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de Oliveira Viana, Jéssika, Marcus T. Scotti et Luciana Scotti. « Molecular Docking Studies in Multitarget Antitubercular Drug Discovery ». Dans Methods in Pharmacology and Toxicology, 107–54. New York, NY : Springer New York, 2018. http://dx.doi.org/10.1007/7653_2018_28.

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Goldman, Jennifer L., Gregory L. Kearns et Susan M. Abdel-Rahman. « Chapter 17 : Pharmacological Considerations of Antitubercular Agents in Children ». Dans Antituberculosis Chemotherapy, 161–75. Basel : KARGER, 2011. http://dx.doi.org/10.1159/000324904.

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Kantevari, Srinivas, Anvesh Jallapally, Anjana Devi Tangutur et Dinesh Kumar. « Development of Antitubercular Agents Through Hybridization Strategies, Future Challenges and Perspectives ». Dans Microbial Biotechnology, 27–62. Toronto ; New Jersey : Apple Academic Press, 2015. : Apple Academic Press, 2017. http://dx.doi.org/10.1201/b19978-4.

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Schnöller, D., Cs B. Pénzes, K. Horváti, Sz Bősze, F. Hudecz et É. Kiss. « Membrane Affinity of New Antitubercular Drug Candidates Using a Phospholipid Langmuir Monolayer Model and LB Technique ». Dans Trends in Colloid and Interface Science XXIV, 131–37. Berlin, Heidelberg : Springer Berlin Heidelberg, 2011. http://dx.doi.org/10.1007/978-3-642-19038-4_23.

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Chattri, GL. « Antitubercular ». Dans Pediatric Drug Doses, 125. Jaypee Brothers Medical Publishers (P) Ltd., 2012. http://dx.doi.org/10.5005/jp/books/11551_21.

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Chattri, GL. « Antitubercular ». Dans Pediatric Drug Doses, 123. Jaypee Brothers Medical Publishers (P) Ltd., 2016. http://dx.doi.org/10.5005/jp/books/12718_22.

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Actes de conférences sur le sujet "Antitubercular"

Laumaillé, Pierre, Alexandra Dassonville-Klimpt et Pascal Sonnet. « Synthesis and study of new antitubercular compounds ». Dans 4th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland : MDPI, 2018. http://dx.doi.org/10.3390/ecmc-4-05578.

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Monteiro, Alex, Marcus Scotti et Luciana Scotti. « MOLECULAR MODELING OF NUCLEOTIDE DERIVATIVES OF 2.5-DIHYDROFURAN-2,5-DIOL FOR EVALUATION OF POTENTIAL ANTITUBERCULAR ACTIVITY ». Dans MOL2NET 2018, International Conference on Multidisciplinary Sciences, 4th edition. Basel, Switzerland : MDPI, 2018. http://dx.doi.org/10.3390/mol2net-04-05917.

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Shaik, Afzal, Kasetti Babu, Indrajeet Singhvi, N. Ravindra et Richie Bhandareh. « Design, synthesis and biological screening of 2,4-dichlorothiazole-5-carboxaldehyde-derived chalcones as potential antitubercular and antiproliferative agents ». Dans 6th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland : MDPI, 2020. http://dx.doi.org/10.3390/ecmc2020-07377.

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Gabrovska, Nataliya, Kaloyan Gabrovski, Krasimir Minkin, Svetlana Velizarova et Petko Minchev. « Severe thoracic tuberculous spondylitis (Pott’s disease) in a 4-year old child treated with antitubercular treatment and surgical decompression, pedicle screw instrumentation and vertebral body reconstruction - a case report ». Dans ERS International Congress 2017 abstracts. European Respiratory Society, 2017. http://dx.doi.org/10.1183/1393003.congress-2017.pa2755.

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Harburn, J. Jonathan, Paul Groundwater, Mark Gray, Sanjib Bhakt, Juan Guzman et Suresh Kottakot. « Synthesis of 20-N-Methylpurpuramine E, an Antitubercural Metabolite from Pseudoceratina sponge ». Dans The 14th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland : MDPI, 2010. http://dx.doi.org/10.3390/ecsoc-14-00430.

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Rapports d'organisations sur le sujet "Antitubercular"

Logan, Isabelle. Mimicking the Bioactivation of the Antitubercular Agent Ethionamide using Peracetic Acid. Portland State University Library, juin 2016. http://dx.doi.org/10.15760/honors.234.

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