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Antitubercular agent

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https://www.readbyqxmd.com/read/29601990/design-synthesis-and-antitubercular-evaluation-of-benzothiazinones-containing-a-piperidine-moiety
#1
Kai Lv, Zeyu Tao, Qian Liu, Lu Yang, Bin Wang, Shuo Wu, Apeng Wang, Menghao Huang, Mingliang Liu, Yu Lu
We herein report the design and synthesis of benzothiazinones containing a piperidine moiety as new antitubercular agents based on the structure feature of IMB-ZR-1 discovered in our lab. Some of them were found to have good in vitro activity (MIC < 1 μg/mL) against drug-susceptible Mycobacterium tuberculosis H37RV strain. After two set of modifications, compound 2i were found to display comparable in vitro anti-TB activity (MIC < 0.016 μg/mL) to PBTZ169 against drug-sensitive and resistant mycobacterium tuberculosis strains...
March 23, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29579424/a-selective-and-sensitive-high-performance-liquid-chromatography-assay-for-the-determination-of-cycloserine-in-human-plasma
#2
A K Hemanth Kumar, Arun Kumar Polisetty, V Sudha, A Vijayakumar, Geetha Ramachandran
BACKGROUND: Cycloserine (CYC) is a second line antitubercular drug that is used for the treatment of multidrug resistant tuberculosis (MDR-TB) along with other antitubercular agents and is often used in developing countries. Monitoring CYC levels in plasma could be useful in the clinical management of patients with MDR-TB. A high performance liquid chromatography method for the determination of CYC in human plasma was developed. METHODS: The method involved extraction of the sample using solid phase extraction cartridges and analysis of the extracted sample using a reverse phase T3 column (150mm) and detection at 240nm with Photo Diode Array (PDA) detector...
April 2018: Indian Journal of Tuberculosis
https://www.readbyqxmd.com/read/29562847/oral-provocation-testing-in-cutaneous-adverse-drug-reactions-to-antiretroviral-and-antitubercular-therapy-a-study-at-a-tertiary-care-hospital-in-south-india
#3
Sowmya Kaimal, Jithendriya Madhukara
AIM: To collect data pertaining to oral drug provocation testing (DPT) in hospitalized patients with antiretroviral (ARV)/antitubercular agent-induced rashes. METHODS: Patients with cutaneous adverse drug reactions (ADRs) to ARV/antitubercular drugs and who underwent oral DPT during a 5-year period were included in this study. RESULTS: Data were collected from the records of 21 patients. Of the 21, 19 had HIV infection. The most commonly implicated drug was nevirapine (NVP), followed by cotrimoxazole and antitubercular agents...
January 2018: Journal of the International Association of Providers of AIDS Care
https://www.readbyqxmd.com/read/29551372/synthesis-evaluation-and-comfa-comsia-study-of-nitrofuranyl-methyl-n-heterocycles-as-novel-antitubercular-agents
#4
Apeng Wang, Yang Yang, Yangsheng Jun, Bin Wang, Kai Lv, Mingliang Liu, Huiyuan Guo, Yu Lu
A series of novel nitrofuranyl methyl N-heterocycles based on the structure of IIIM-MCD-211 were designed and synthesized. Compounds 6d, 8b and 12a show excellent activity against MTB H37Rv strain (MIC: 0.031-0.062 μg/mL) roughly comparable to INH and IIIM-MCD-211. In addition, a three-dimensional quantitative structure-activity relationship (3D-QSAR) study was performed on the above mentioned chemical series employing comparative molecular field analysis (CoMFA) and comparative molecular similarity index analysis (CoMSIA) techniques...
March 3, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29532762/heterocyclic-compounds-2-pyrazolines-are-biological-active-as-well-as-fluorescence-agents-an-overview
#5
Pramod Singh Negi, Jitendra Singh, Geeta Joshi Nee Pant, Msm Rawat
Nitrogen containing five membered heterocyclics play vital role in pharmaceuticals as well as medicinal chemistry. Pyrazolines play a significant role among other heterocycles because of their therapeutic and pharmacological properties. 2-Pyrazolines displayed a wide variety of biological activities such as anticancer, antiepileptic, anti-aids, antimalarial, insecticidal and antitubercular etc. and they are used as pesticides, herbicides, fungicides and also used in agrochemical research and analytical chemistry...
March 13, 2018: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29527397/wolf-in-sheep-s-clothing-intracranial-actinomycosis-masquerading-as-en-plaque-meningioma
#6
Harsh Deora, Manish Beniwal, Shilpa Rao, K V L N Rao, V Vikas, Sampath Somanna
Background: Actinomycosis israeli is a gram-positive non-acid-fast bacterium and is the most common causative agent of actinomycosis. It usually presents as a brain abscess via a secondary spread from the cervicofacial region or lungs. However, presentation as an en-plaque lesion with bone involvement out of proportion to brain parenchyma is rare and needs to be acknowledged. Case Description: We report a case of intracranial en-plaque lesion in a 47-year-old female with restriction of mouth opening and right third nerve palsy for 1 year...
2018: Surgical Neurology International
https://www.readbyqxmd.com/read/29505613/tnseq-of-mycobacterium-tuberculosis-clinical-isolates-reveals-strain-specific-antibiotic-liabilities
#7
Allison F Carey, Jeremy M Rock, Inna V Krieger, Michael R Chase, Marta Fernandez-Suarez, Sebastien Gagneux, James C Sacchettini, Thomas R Ioerger, Sarah M Fortune
Once considered a phenotypically monomorphic bacterium, there is a growing body of work demonstrating heterogeneity among Mycobacterium tuberculosis (Mtb) strains in clinically relevant characteristics, including virulence and response to antibiotics. However, the genetic and molecular basis for most phenotypic differences among Mtb strains remains unknown. To investigate the basis of strain variation in Mtb, we performed genome-wide transposon mutagenesis coupled with next-generation sequencing (TnSeq) for a panel of Mtb clinical isolates and the reference strain H37Rv to compare genetic requirements for in vitro growth across these strains...
March 2018: PLoS Pathogens
https://www.readbyqxmd.com/read/29475004/novel-compounds-targeting-inha-for-tb-therapy
#8
REVIEW
Manaf AlMatar, Essam A Makky, Işıl Var, Begüm Kayar, Fatih Köksal
Tuberculosis (TB) is described as lethal disease in the world. Resistant to TB drugs is the main reason to have unfavourable outcomes in the treatment of TB. Therefore, new agents to replace existing drugs are urgently needed. Previous reports suggested that InhA inhibitors, an enoyl-ACP-reductase, might provide auspicious candidates which can be developed into novel antitubercular agents. In this review, we explain the role of InhA in the resistance of isoniazid. Furthermore, five classes of InhA inhibitors, which display novel binding modes and deliver evidence of their prosperous target engagement, have been debated...
September 21, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29453370/a-multitarget-approach-to-drug-discovery-inhibiting-mycobacterium-tuberculosis-pyrg-and-pank
#9
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
#10
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-methylerythritol-phosphate-pathway-promising-drug-targets-in-the-fight-against-tuberculosis
#11
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...
March 9, 2018: ACS Infectious Diseases
https://www.readbyqxmd.com/read/29389854/mycobacterium-tuberculosis-molecular-determinants-of-infection-survival-strategies-and-vulnerable-targets
#12
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
#13
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
#14
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
#15
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...
February 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
#16
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
#17
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
#18
Wei Zhang, Shichun Lun, Shu-Huan Wang, Xing-Wu 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 cocrystal 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...
February 8, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29325084/metformin-use-reverses-the-increased-mortality-associated-with-diabetes-mellitus-during-tuberculosis-treatment
#19
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
#20
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 do not show 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, and physiochemical and absorption-distribution-metabolism-excretion properties. Select pyrimidines were then evaluated for their pharmacokinetic profiles in mice...
March 2018: Antimicrobial Agents and Chemotherapy
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