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https://www.readbyqxmd.com/read/29222671/biological-potential-of-thiazolidinedione-derivatives-of-synthetic-origin
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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/29151986/pyrrolyl-pyrazoline-carbaldehydes-as-enoyl-acp-reductase-inhibitors-design-synthesis-and-antitubercular-activity
#7
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/29110620/vitamins-based-novel-target-pathways-molecules-as-possible-emerging-drug-targets-for-management-of-tuberculosis
#8
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/29093335/novel-6-phenylnicotinohydrazide-derivatives-design-synthesis-and-biological-evaluation-as-a-novel-class-of-antitubercular-and-antimicrobial-agents
#9
Dalia Hussein Soliman, Wagdy Mohamed Eldehna, Hazem Ahmed Ghabbour, Maha Mamdouh Kabil, Marwa Mostafa Abdel-Aziz, Hatem Abdel-Kader Abdel-Aziz
In our ongoing efforts to develop potent antitubercular agents based on the 6-phenylnicotinohydrazide, herein we report the design, synthesis and biological evaluation of three sets of 6-phenylnicotinohydrazide derivatives 8a-g, 12 and 16a, b. The designed compounds were synthesized and in vitro evaluated for their antitubercular activity. In addition, their antifungal and antibacterial activities were evaluated as well. The nicotinohydrazide class displayed different levels of antimicrobial activity and possessed a distinctive pattern of selectivity against the tested microorganisms...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29066301/wild-type-catalase-peroxidase-vs-g279d-mutant-type-molecular-basis-of-isoniazid-drug-resistance-in-mycobacterium-tuberculosis
#10
Aishwarya Singh, Aditi Singh, Sonam Grover, Bharati Pandey, Anchala Kumari, Abhinav Grover
Mycobacterium tuberculosis katG gene is responsible for production of an enzyme catalase peroxidase that peroxidises and activates the prodrug Isoniazid (INH), a first-line antitubercular agent. INH interacts with catalase peroxidase enzyme within its heme pocket and gets converted to an active form. Mutations occurring in katG gene are often linked to reduced conversion rates for INH. This study is focussed on one such mutation occurring at residue 279, where glycine often mutates to aspartic acid (G279D)...
October 21, 2017: Gene
https://www.readbyqxmd.com/read/29064811/-the-risk-of-epileptic-seizures-during-antibiotic-therapy
#11
Ewa Czapińska-Ciepiela
Numerous antibiotics may trigger epileptic seizures or status epilepticus by decreasing inhibitory transmission in the brain, thus lowering the seizure threshold. The most potent seizurogenic effect is exerted by penicillins, cephalosporins, fluorochinolons and carbapenems. Predisposing factors that facilitate development of epileptic seizures in the course of antibiotic therapy comprise all conditions accompanied by damage to the blood-brain barrier (including cerebral trauma and encephalitis), a high dose of an antibiotic or lack of adequate dose adjustment in patients with renal failure...
2017: Wiadomości Lekarskie: Organ Polskiego Towarzystwa Lekarskiego
https://www.readbyqxmd.com/read/29036230/predictors-of-adverse-drug-reaction-related-hospitalisation-in-southwest-ethiopia-a-prospective-cross-sectional-study
#12
Mulugeta Tarekegn Angamo, Colin Michael Curtain, Leanne Chalmers, Daniel Yilma, Luke Bereznicki
BACKGROUND: Adverse drug reactions (ADRs) are important causes of morbidity and mortality in the healthcare system; however, there are no studies reporting on the magnitude and risk factors associated with ADR-related hospitalisation in Ethiopia. OBJECTIVES: To characterise the reaction types and the drugs implicated in admission to Jimma University Specialized Hospital, Southwest Ethiopia, and to identify risk factors associated with ADR-related hospitalisation...
2017: PloS One
https://www.readbyqxmd.com/read/28993106/the-antitubercular-activity-of-various-nitro-triazole-imidazole-based-compounds
#13
Maria V Papadopoulou, William D Bloomer, Howard S Rosenzweig
Twenty three 3-nitrotriazole- and five nitroimidazole-based compounds, mostly amides, were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv (Mtb H37Rv) under aerobic or low oxygen conditions, intracellular activity in murine J774 macrophages or THP-1 cells, activity against resistant Mtb strains as well as cytotoxicity in normal cells. Compounds with a Minimum Inhibitory Concentration (MIC) less than 10μM and 10-50μM were characterized as active and moderately active, respectively, whereas compounds with a MIC >50μM were characterized inactive...
November 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28979312/synthesis-of-some-new-tetrahydropyrimidine-derivatives-as-possible-antibacterial-agents
#14
Naser Foroughifar, Somayeh Karimi Beromi, Hoda Pasdar, Masoumeh Shahi
Heterocyclic compounds containing a pyrimidine nucleus are of special interests thanks to their applications in medicinal chemistry as they are the basic skeleton of several bioactive compounds such as antifungal, antibacterial, antitumor and antitubercular. As a part of our research in the synthesis of pyrimidine derivatives containing biological activities, some new tetrahydropyrimidine derivatives (1-10) were synthesized via Biginelli reaction using HCl or DABCO as a catalyst with good yields. All structures of products were confirmed by IR, (1)H NMR and (13)C NMR spectroscopy...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/28961440/chemical-synthesis-and-in-silico-molecular-modeling-of-novel-pyrrolyl-benzohydrazide-derivatives-their-biological-evaluation-against-enoyl-acp-reductase-inha-and-mycobacterium-tuberculosis
#15
Shrinivas D Joshi, Uttam A More, Sheshagiri R Dixit, Sunil V Balmi, Basavaraj G Kulkarni, Geeta Ullagaddi, Christian Lherbet, Tejraj M Aminabhavi
In efforts to develop new antitubercular agents, we report here the synthesis of a series of novel pyrrole hydrazine derivatives. The molecules were evaluated against inhibitors of InhA, which is one of the key enzymes involved in type II fatty acid biosynthetic pathway of the mycobacterial cell wall as well as inhibitors of Mycobacterium tuberculosis H37Rv. The binding mode of compounds at the active site of enoyl-ACP reductase was explored using the surflex-docking method. The model suggests one or two H-bonding interactions between the compounds and the InhA enzyme...
September 12, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28953378/discovery-of-a-potent-and-specific-m-tuberculosis-leucyl-trna-synthetase-inhibitor-s-3-aminomethyl-4-chloro-7-2-hydroxyethoxy-benzo-c-1-2-oxaborol-1-3h-ol-gsk656
#16
Xianfeng Li, Vincent Hernandez, Fernando L Rock, Wai Choi, Yvonne S L Mak, Manisha Mohan, Weimin Mao, Yasheen Zhou, Eric E Easom, Jacob J Plattner, Wuxin Zou, Esther Pérez-Herrán, Ilaria Giordano, Alfonso Mendoza-Losana, Carlos Alemparte, Joaquín Rullas, Iñigo Angulo-Barturen, Sabrinia Crouch, Fátima Ortega, David Barros, M R K Alley
There is an urgent need to develop new and safer antitubercular agents that possess a novel mode of action. We synthesized and evaluated a novel series of 3-aminomethyl 4-halogen benzoxaboroles as Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS) inhibitors. A number of Mtb LeuRS inhibitors were identified that demonstrated good antitubercular activity with high selectivity over human mitochondrial and cytoplasmic LeuRS. Further evaluation of these Mtb LeuRS inhibitors by in vivo pharmacokinetics (PK) and murine tuberculosis (TB) efficacy models led to the discovery of GSK3036656 (abbreviated as GSK656)...
October 12, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28921911/update-of-antitubercular-prodrugs-from-a-molecular-perspective-mechanisms-of-action-bioactivation-pathways-and-associated-resistance
#17
REVIEW
Julie Laborde, Céline Deraeve, Vania Bernardes-Génisson
The place of prodrugs in the current antitubercular therapeutic arsenal is preponderant, since two of the four first-line antitubercular agents, isoniazid (INH) and pyrazinamide (PZA), need to be activated by Mycobacterium tuberculosis before exerting their activity. In addition, six other prodrugs can be found in the second- and third-line therapeutic regimens. The emergence of mycobacterial strains resistant to one or several antitubercular agents is one of the main issues of the antitubercular therapy. In the case of prodrugs, the resistance phenomenon is often related to a mutation in the gene encoding for the activation enzymes, resulting thus in a default of these enzymes that are no more able to activate prodrugs...
October 20, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28911608/effect-of-goat-milk-on-hepatotoxicity-induced-by-antitubercular-drugs-in-rats
#18
Sonam Miglani, Rakesh Raman Patyar, Sazal Patyar, Mohammad Rafi Reshi
Aim of the present study was to assess the hepatoprotective activity of goat milk on antitubercular drug-induced hepatotoxicity in rats. Hepatotoxicity was induced in rats using a combination of isoniazid, rifampicin, and pyrazinamide given orally as a suspension for 30 days. Treatment groups received goat milk along with antitubercular drugs. Liver damage was assessed using biochemical and histological parameters. Administration of goat milk (20 mL/kg) along with antitubercular drugs (Group III) reversed the levels of serum alanine aminotransferase (82 ± 25...
October 2016: Journal of Food and Drug Analysis
https://www.readbyqxmd.com/read/28895161/therapeutic-drug-monitoring-of-antitubercular-agents-for-disseminated-mycobacterium-tuberculosis-during-intermittent-haemodialysis-and-continuous-venovenous-haemofiltration
#19
J H Sin, R H Elshaboury, R M Hurtado, A R Letourneau, R G Gandhi
WHAT IS KNOWN AND OBJECTIVE: There is a lack of data regarding therapeutic drug monitoring (TDM) of antitubercular agents in the setting of continuous venovenous haemofiltration (CVVH). We describe TDM results of numerous antitubercular agents in a critically ill patient during CVVH and haemodialysis. CASE SUMMARY: A 49-year-old man was initiated on treatment for disseminated Mycobacterium tuberculosis. During hospital admission, the patient developed critical illness and required renal replacement therapy...
September 11, 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28869400/azide-alkyne-cycloaddition-en-route-to-4-aminoquinoline-ferrocenylchalcone-conjugates-synthesis-and-anti-tb-evaluation
#20
Amandeep Singh, Albertus Viljoen, Laurent Kremer, Vipan Kumar
AIM: Tuberculosis is responsible for 9.6 million infections and 1.5 million deaths in 2015. The development of multidrug-resistant and extensively drug-resistant strains has impeded the development of effective antitubercular therapy. Results/methodology: The present manuscript describes the synthesis of a series of 4-aminoquinoline-ferrocenylchalcone conjugates via Cu-promoted Huisgen's azide-alkyne cycloaddition reaction and evaluation of their antitubercular activities against mc(2)6230 strain of Mycobacterium tuberculosis...
October 2017: Future Medicinal Chemistry
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