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Antitubercular agent

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https://www.readbyqxmd.com/read/29453370/a-multitarget-approach-to-drug-discovery-inhibiting-mycobacterium-tuberculosis-pyrg-and-pank
#1
Laurent R Chiarelli, Giorgia Mori, Beatrice Silvia Orena, Marta Esposito, Thomas Lane, Ana Luisa de Jesus Lopes Ribeiro, Giulia Degiacomi, Júlia Zemanová, Sára Szádocka, Stanislav Huszár, Zuzana Palčeková, Marcello Manfredi, Fabio Gosetti, Joël Lelièvre, Lluis Ballell, Elena Kazakova, Vadim Makarov, Emilio Marengo, Katarina Mikusova, Stewart T Cole, Giovanna Riccardi, Sean Ekins, Maria Rosalia Pasca
Mycobacterium tuberculosis, the etiological agent of the infectious disease tuberculosis, kills approximately 1.5 million people annually, while the spread of multidrug-resistant strains is of great global concern. Thus, continuous efforts to identify new antitubercular drugs as well as novel targets are crucial. Recently, two prodrugs activated by the monooxygenase EthA, 7947882 and 7904688, which target the CTP synthetase PyrG, were identified and characterized. In this work, microbiological, biochemical, and in silico methodologies were used to demonstrate that both prodrugs possess a second target, the pantothenate kinase PanK...
February 16, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29446718/current-trends-and-future-directions-of-fluoroquinolones
#2
Hamada H H Mohammed, Gamal El-Din A A Abuo-Rahma, Samar H Abbas, El-Shimaa M N Abdelhafez
Fluoroquinolones represent an interesting synthetic class of antimicrobial agents with broad spectrum and potent activity. Since the discovery of nalidixic acid, the prototype of quinolones, several structural modifications to the quinolone nucleus have been carried out for improvement of potency, spectrum of activity, and to understand their structure activity relationship (SAR). The C-7 substituent was reported to have a major impact on the activity. Accordingly, Substitution at C-7 or its N-4-piperazinyl moiety was found to affect potency, bioavailability, and physicochemical properties...
February 14, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29390176/the-mep-pathway-promising-drug-targets-in-the-fight-against-tuberculosis
#3
Xu Wang, Cynthia S Dowd
Tuberculosis (TB), caused by Mycobacterium tuberculosis (Mtb), is a severe infectious disease in need of new chemotherapies especially for drug-resistant cases. To meet the urgent requirement of new TB drugs with novel modes of action, the TB research community has been validating numerous targets from several biosynthetic pathways. The methylerythritol phosphate (MEP) pathway is utilized by Mtb for the biosynthesis of isopentenyl pyrophosphate (IPP) and its isomer dimethylallyl pyrophosphate (DMAPP), the universal five-carbon building blocks of isoprenoids...
February 1, 2018: ACS Infectious Diseases
https://www.readbyqxmd.com/read/29389854/mycobacterium-tuberculosis-molecular-determinants-of-infection-survival-strategies-and-vulnerable-targets
#4
REVIEW
Davide M Ferraris, Riccardo Miggiano, Franca Rossi, Menico Rizzi
Mycobacterium tuberculosis is the causative agent of tuberculosis, an ancient disease which, still today, represents a major threat for the world population. Despite the advances in medicine and the development of effective antitubercular drugs, the cure of tuberculosis involves prolonged therapies which complicate the compliance and monitoring of drug administration and treatment. Moreover, the only available antitubercular vaccine fails to provide an effective shield against adult lung tuberculosis, which is the most prevalent form...
February 1, 2018: Pathogens
https://www.readbyqxmd.com/read/29376495/anti-inflammatory-anti-allergy-agents-in-medicinal-chemistry-formerly-current-medicinal-chemistry-anti-inflammator
#5
Ashwani Kumar Dhingra, Bhawna Chopra, Jagdeep Singh Dua, Deo N Parsad
The search of novel anti-inflammatory agent is not considered as an ending process, since most of the clinically used anti-inflammatory drugs such as NSAIDs, Coxibs and GCs are allied with considerable toxicity. However, numerous approaches were used to overcome the toxicity level such as co-administration with suitable agent/substance which provides protection against toxicity as well to synthesise new potent and safe anti-inflammatory drug. Although the drug treatment has been improved steadily but yet, it is still a challenge for the medicinal chemists to identify more potent therapeutic agents to treat or reduce the symptoms of inflammatory diseases...
January 26, 2018: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29376490/targeting-dna-repair-systems-in-antitubercular-drug-development
#6
Alina Minias, Anna Brzostek, Jaroslaw Dziadek
Infections with Mycobacterium tuberculosis, the causative agent of tuberculosis, are difficult to treat using currently available chemotherapeutics. Clinicians agree on the urgent need for novel drugs to treat tuberculosis. In this mini review, we summarize data that prompts the consideration of DNA repair-associated proteins as targets for the development of new antitubercular compounds. We discuss data, including gene expression data, that highlight the importance of DNA repair genes during the pathogenic cycle as well as after exposure to antimicrobials currently in use...
January 28, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29356105/design-synthesis-and-evaluation-of-new-%C3%AE-aminonitrile-based-benzimidazole-biomolecules-as-potent-antimicrobial-and-antitubercular-agents
#7
Irfan N Shaikh, Kallappa M Hosamani, Mahantesh M Kurjogi
The study explores the one-pot synthesis of novel α-aminonitriles by reacting 4-[(1H-benzimidazol-2-yl)methoxy]benzaldehyde, substituted anilines and sodium cyanide using a catalytic amount of copper dipyridine dichloride (CuPy2 Cl2 ) and employing the Strecker reaction under mild conditions. All the synthesized compounds were screened for antimicrobial and antitubercular activity. The promising lead compounds 4d and 4e were identified, with MIC values ranging between 3.9 and 7.8 µg/mL against different bacterial strains...
January 22, 2018: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29342972/the-effect-of-combining-natural-terpenes-and-antituberculous-agents-against-reference-and-clinical-mycobacterium-tuberculosis-strains
#8
Elwira Sieniawska, Rafal Sawicki, Marta Swatko-Ossor, Agnieszka Napiorkowska, Agata Przekora, Grazyna Ginalska, Ewa Augustynowicz-Kopec
Background: On account of emergence of multi- and extensively drug-resistant Mycobacterium tuberculosis (Mtb) strains, combinations of drugs with natural compounds were tested to search for antibiotic activity enhancers. In this work we studied terpenes (α-pinene, bisabolol, β-elemene, (R)-limonene, (S)-limonene, myrcene, sabinene), which are the main constituents of essential oil obtained from Mutellina purpurea L., a plant with described antitubercular activity, to investigate their interactions with antibiotics against reference Mtb strains and multidrug-resistant clinical isolates...
January 15, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29332642/current-affairs-future-perspectives-of-tuberculosis-and-antitubercular-agents
#9
REVIEW
Jineetkumar Gawad, Chandrakant Bonde
Tuberculosis (TB) is the major threat for humans from past several decades. Even after advent of several antitubercular drugs, researchers are still struggling for the mycobacterial infections in humans are TB and leprosy. Chronic infections caused by Mycobacterium tuberculosis and Mycobacterium leprae. A particular problem with both of these organisms is that they can survive inside macrophages after phagocytosis, unless these cells are activated by cytokines produced by T-lymphocytes, because of this researchers are not yet succeeded in finding effective treatment on TB...
January 2018: Indian Journal of Tuberculosis
https://www.readbyqxmd.com/read/29328655/identification-of-novel-coumestan-derivatives-as-polyketide-synthase-13-inhibitors-against-mycobacterium-tuberculosis
#10
Wei Zhang, Shichun Lun, Shu-Huan Wang, Xingwu Jiang, Fan Yang, Jie Tang, Abigail L Manson, Ashlee M Earl, Hendra Gunosewoyo, William R Bishai, Li-Fang Yu
Inhibition of the mycolic acid pathway has proven a viable strategy in antitubercular drug discovery. The AccA3/AccD4/FadD32/Pks13 complex of Mycobacterium tuberculosis constitutes an essential biosynthetic mechanism for mycolic acids. Small molecules targeting the thioesterase domain of Pks13 have been reported, including a benzofuran-based compound, whose X-ray co-crystal structure has been very recently solved. Its initial inactivity in a serum inhibition titration (SIT) assay led us to further probe other structurally-related benzofurans with the aim to improve their potency and bioavailability...
January 12, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29325084/metformin-use-reverses-the-increased-mortality-associated-with-diabetes-mellitus-during-tuberculosis-treatment
#11
Nicholas R Degner, Jann-Yuan Wang, Jonathan E Golub, Petros C Karakousis
Background: The global type 2 diabetes mellitus (DM) epidemic threatens progress made in reducing tuberculosis (TB)-related mortality worldwide. Previous clinical studies have not fully evaluated potential confounding variables in addressing the impact of DM on TB treatment outcomes. The antidiabetic agent metformin regulates autophagy and may play a role as a host-directed therapeutic adjuvant to antitubercular treatment. Methods: We conducted a retrospective cohort study comprising patients aged ≥13 years undergoing treatment for culture-confirmed, drug-susceptible pulmonary TB...
January 6, 2018: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/29311070/novel-pyrimidines-as-antitubercular-agents
#12
Daigo Inoyama, Steven D Paget, Riccardo Russo, Srinivasan Kandasamy, Pradeep Kumar, Eric Singleton, James Occi, Margareta Tuckman, Matthew D Zimmerman, Hsin Pin Ho, Alexander L Perryman, Véronique Dartois, Nancy Connell, Joel S Freundlich
Mycobacterium tuberculosis infection is responsible for a global pandemic. New drugs are needed that lack cross-resistance with the existing front-line therapeutics. A triazine antitubercular hit led to the design of a related pyrimidine family. The synthesis of a focused series of these analogs facilitated exploration of their in vitro activity, in vitro cytotoxicity, physiochemical, and Absorption-Distribution-Metabolism-Excretion properties. Select pyrimidines were then evaluated for their mouse pharmacokinetic profiles...
January 8, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29288945/recent-advance-in-oxazole-based-medicinal-chemistry
#13
REVIEW
Hui-Zhen Zhang, Zhi-Long Zhao, Cheng-He Zhou
Oxazole compounds containing nitrogen and oxygen atoms in the five-membered aromatic ring are readily able to bind with a variety of enzymes and receptors in biological systems via diverse non-covalent interactions, and thus display versatile biological activities. The related researches in oxazole-based derivatives including oxazoles, isoxazoles, oxazolines, oxadiazoles, oxazolidones, benzoxazoles and so on, as medicinal drugs have been an extremely active topic, and numerous excellent achievements have been acquired...
December 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29226732/pharmacokinetics-and-pharmacogenetics-of-anti-tubercular-drugs-a-tool-for-treatment-optimization
#14
Ilaria Motta, Andrea Calcagno, Stefano Bonora
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...
January 2018: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29222671/biological-potential-of-thiazolidinedione-derivatives-of-synthetic-origin
#15
REVIEW
Sucheta, Sumit Tahlan, Prabhakar Kumar Verma
Thiazolidinediones are sulfur containing pentacyclic compounds that are widely found throughout nature in various forms. Thiazolidinedione nucleus is present in numerous biological compounds, e.g., anti-malarial, antimicrobial, anti-mycobacterium, anticonvulsant, antiviral, anticancer, anti-inflammatory, antioxidant, anti-HIV (human immunodeficiency virus) and antitubercular agent. However, owing to the swift development of new molecules containing this nucleus, many research reports have been generated in a brief span of time...
December 8, 2017: Chemistry Central Journal
https://www.readbyqxmd.com/read/29220797/primaquine-hybrids-as-promising-antimycobacterial-and-antimalarial-agents
#16
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/29202408/synthesis-and-antimycobacterial-activity-of-triterpeni%C3%A2-a-ring-azepanes
#17
Natalya I Medvedeva, Oxana B Kazakova, Tatyana V Lopatina, Irina E Smirnova, Gul'nara V Giniyatullina, Irina P Baikova, Vladimir E Kataev
A series of A-ring azepanones and azepanes derived from betulonic, oleanonic and ursonic acids was synthesized and evaluated for their in vitro antimycobacterial activities against M. tuberculosis (MTB) H37Rv and SDR-TB in the National Institute of Allergy and Infectious Diseases. Triterpenic A-azepano-28-hydroxy-derivatives were synthesized by the reduction with LiAlH4 of triterpenic azepanones available from the Beckmann rearrangement of the corresponding C3-oximes. Modification of azepanes at NH-group and atoms С12, C20, C28 and C29 of triterpenic core led to the derivatives with oxo, epoxy, aminopropyl, oximino and acyl substituents...
November 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29201084/design-and-synthesis-of-some-novel-fluorobenzimidazoles-substituted-with-structural-motifs-present-in-physiologically-active-natural-products-for-antitubercular-activity
#18
Bangalore Nandha, Laxmivenkatesh Gurachar Nargund, Shachindra Laxmivenkatesh Nargund, Kishore Bhat
Keeping in view the drawbacks associated with research on anti-TB drugs based on plant extracts and the non-availability of fluorinated natural products with antitubercular activity has prompted us to make an effort towards the synthesis and characterization of a novel series of fifteen substituted fluorobenzimidazoles. The newly synthesized compounds were characterized by I.R, 1H-NMR, 13C-NMR, Mass, and elemental analysis. The synthesized compounds 4(a-f) and 5(b-j) have been evaluated for their in-vitro antimycobacterial activity against H37Rv strain (ATCC 27294) by MABA method...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/29188778/cytotoxic-and-acute-toxicity-studies-of-isoniazid-derivatives
#19
Sabahat Naeem, Shamim Akhtar, Zi-Ning Lei, Kimberly Lu, Shaista Zafar, Ahsaan Ahmed, Mohsin Ali, Mansoor Ahmed, Zhe-Sheng Chen
Cancer is ultimately the result of cells that hysterically grow and do not die. Cells can experience uncontrolled growth if there are mutations to DNA, and therefore, alterations to the genes involved in cell division. Cancer occurs when a cell's gene mutations make the cell unable to correct DNA damage and is unable to destroy itself. There are over 100 different types of cancer each classified by the type of initially affected cell. Isoniazid, a well-known antitubercular agent has been reported to exhibit some cytotoxic activity...
November 2017: Pakistan Journal of Pharmaceutical Sciences
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
#20
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
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