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Antitubercular agent

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
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...
September 28, 2017: Bioorganic & Medicinal Chemistry
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
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
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)...
September 27, 2017: Journal of Medicinal Chemistry
Vania Bernardes Genisson, Julie Laborde, Céline Deraeve
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, namely ethionamide (ETH), prothionamide (PTH), p-aminosalicylic acid (PAS), thiacetazone (TAC), isoxyl (ISO) and the recently approved delamanid. The emergence of mycobacterial strains resistant to one or several antitubercular agents is one of the main issues of the antitubercular therapy...
September 16, 2017: ChemMedChem
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
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
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...
September 4, 2017: Future Medicinal Chemistry
Karen Reyes-Melo, Abraham García, Antonio Romo-Mancillas, Elvira Garza-González, Verónica M Rivas-Galindo, Luis D Miranda, Javier Vargas-Villarreal, Juan Manuel J Favela-Hernández, María Del Rayo Camacho-Corona
Thirty-three meso-dihydroguaiaretic acid (meso-DGA) derivatives bearing esters, ethers, and amino-ethers were synthesized. All derivatives were tested against twelve drug-resistant clinical isolates of Gram-positive and Gram-negative bacteria, including sensitive (H37Rv) and multidrug-resistant Mycobacterium tuberculosis strains. Among the tested compounds, four esters (7, 11, 13, and 17), one ether (23), and three amino-ethers (30, 31, and 33) exhibited moderate activity against methicillin-resistant Staphylococcus aureus, whereas 30 and 31 showed better results than levofloxacin against vancomycin-resistant Enterococcus faecium...
July 29, 2017: Bioorganic & Medicinal Chemistry
Jaroslav Roh, Galina Karabanovich, Hana Vlčková, Alejandro Carazo, Jan Němeček, Pavel Sychra, Lenka Valášková, Oto Pavliš, Jiřina Stolaříková, Věra Klimešová, Kateřina Vávrová, Petr Pávek, Alexandr Hrabálek
In this work, four series of tertiary amine-containing derivatives of 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents were prepared, and their in vitro antimycobacterial effects were evaluated. We found that the studied compounds showed lipophilicity-dependent antimycobacterial activity. The N-benzylpiperazine derivatives, which had the highest lipophilicity among all of the series, showed the highest in vitro antimycobacterial activities against Mycobacterium tuberculosis CNCTC My 331/88 (H37Rv), comparable to those of the first-line drugs isoniazid and rifampicin...
August 8, 2017: Bioorganic & Medicinal Chemistry
Amit S Tapkir, Sohan S Chitlange, Ritesh P Bhole
Fragment based Quantitative structure activity relationship (QSAR) analysis on reported 25 2-(2-(4-aryloxybenzylidene) hydrazinyl) benzothiazole dataset as antitubercular agents were carried out. Molecules in the current dataset were fragmented into six fragments (R1, R2, R3, R4, R5, R6).Group based QSAR Models were derived using Multiple linear regression (MLR) analysis and selected on the basis of various statistical parameters. Dataset of benzothiazole reveled importance of presence of halogen atoms on is essential requirement...
October 2017: Data in Brief
Xu Wang, Yong-Mo Ahn, Adam G Lentscher, Julia S Lister, Robert C Brothers, Malea M Kneen, Barbara Gerratana, Helena I Boshoff, Cynthia S Dowd
Nicotinamide adenine dinucleotide (NAD(+)) synthetase catalyzes the last step in NAD(+) biosynthesis. Depletion of NAD(+) is bactericidal for both active and dormant Mycobacterium tuberculosis (Mtb). By inhibiting NAD(+) synthetase (NadE) from Mtb, we expect to eliminate NAD(+) production which will result in cell death in both growing and nonreplicating Mtb. NadE inhibitors have been investigated against various pathogens, but few have been tested against Mtb. Here, we report on the expansion of a series of urea-sulfonamides, previously reported by Brouillette et al...
September 15, 2017: Bioorganic & Medicinal Chemistry Letters
Vasanthi Natarajan, Kevin John, David Jose, Pradeep Kalaiselvan, Ashok Kumar Das
Vascular thrombosis is one of the complications of tuberculosis. Deep vein thrombosis and pulmonary thrombosis have been reported with pulmonary and extrapulmonary tuberculosis. Splenic involvement in abdominal tuberculosis is among the rarest manifestations. Disseminated tuberculosis is predominantly reported in rheumatoid arthritis following ingestion of biological agents. Here, we report a case of disseminated tuberculosis in a rheumatoid arthritis patient who was on steroids and methotrexate for a long period, presenting with multiple splenic lesion and portal vein thrombosis, which was not reported earlier...
June 2017: Journal of Clinical and Diagnostic Research: JCDR
Maria V Papadopoulou, William D Bloomer, Howard S Rosenzweig, Marcel Kaiser
A limited number of novel 3-nitrotriazole- and 2-nitroimidazole-linked quinolines and quinazolines were synthesized and screened for in vitro antitrypanosomal and antitubercular activities as well as cytotoxicity in normal cells. All compounds were active against T. cruzi amastigotes, while all but one were active or moderately active against T. b. rhodesiense. However, only two chloroquinolines exhibited satisfactory selectivity indices (SI) against T. cruzi and only one of them demonstrated a satisfactory SI against T...
September 29, 2017: European Journal of Medicinal Chemistry
Elisa Azzali, Diana Machado, Amit Kaushik, Federica Vacondio, Sara Flisi, Clotilde Silvia Cabassi, Gyanu Lamichhane, Miguel Viveiros, Gabriele Costantino, Marco Pieroni
Tuberculosis remains one of the deadliest infectious diseases in the world, and the increased number of multidrug-resistant and extremely drug-resistant strains is a significant reason for concern. This makes the discovery of novel antitubercular agents a cogent priority. We have previously addressed this need by reporting a series of substituted 2-aminothiazoles capable to inhibit the growth of actively replicating, nonreplicating persistent, and resistant Mycobacterium tuberculosis strains. Clues from the structure-activity relationships lining up the antitubercular activity were exploited for the rational design of improved analogues...
August 24, 2017: Journal of Medicinal Chemistry
Rosalba Perrone, Enrico Lavezzo, Erika Riello, Riccardo Manganelli, Giorgio Palù, Stefano Toppo, Roberta Provvedi, Sara N Richter
Mycobacterium tuberculosis is the causative agent of tuberculosis (TB), one of the top 10 causes of death worldwide in 2015. The recent emergence of strains resistant to all current drugs urges the development of compounds with new mechanisms of action. G-quadruplexes are nucleic acids secondary structures that may form in G-rich regions to epigenetically regulate cellular functions. Here we implemented a computational tool to scan the presence of putative G-quadruplex forming sequences in the genome of Mycobacterium tuberculosis and analyse their association to transcription start sites...
July 18, 2017: Scientific Reports
Mohamed A Abdelrahman, Ismail Salama, Mohamed S Gomaa, Mahmoud M Elaasser, Marwa M Abdel-Aziz, Dalia H Soliman
The increased development of highly resistant bacterial strains and tuberculosis, constitute a serious public health threat, highlighting the urgent need of novel antibacterial agents. In this work, two novel series of nicotinic acid hydrazone derivatives (6a-r) and quinolone hydrazide derivatives (12a-l) were synthesized and evaluated as antimicrobial and antitubercular agents. The synthesized compounds were evaluated in vitro for their antibacterial, antifungal and antimycobacterial activities. Compounds 6f and 6p bearing the 3,4,5- (OCH3)3 and 2,5-(OCH3)2 benzylidene motifs were the most potent and as antibacterial, antifungal (MIC: 0...
September 29, 2017: European Journal of Medicinal Chemistry
S Anuradha, K Shravan Kumar, S Bhama, V Kishan
Tuberculosis, caused by Mycobacterium tuberculosis, continues to be a serious public health problem around the world, and it urges the need for development of new antitubercular drugs. An antibiotic producing strain, Streptomyces luridus (MTCC 4402) was earlier isolated from soil by our group. In this work, the phylogenic status was established by 16S rRNA gene sequence analysis. The strain was found to be active against clinically resistant strains. The culture was grown in shake flasks in a medium containing cornsteep liquor, glucose, CaCO(3), soyabean meal and starch...
September 2016: Indian Journal of Experimental Biology
Neeraj Jaryal, Harpreet Kaur
In the present work, silver nanoparticles have been biosynthesized by utilizing the alcoholic extract of Plumbago auriculata. The optimization of reaction conditions was carried out by monitoring the reactions with the help of UV-Visible absorption spectroscopy. The characterization of AgNP was carried out by infrared spectroscopy, transmission electron microscopy and X-Ray diffraction (XRD) studies. The biogenic AgNPs were tested against Mycobacterium tuberculosis using Microplate Almar Blue assay (MABA) and their antioxidant activity was also evaluated...
July 20, 2017: Journal of Biomaterials Science. Polymer Edition
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