Molecules, Vol. 25, Pages 1518: N-Pyrazinoyl Substituted Amino Acids as Potential Antimycobacterial Agents —The Synthesis and Biological Evaluation of Enantiomers

Molecules, Vol. 25, Pages 1518: N-Pyrazinoyl Substituted Amino Acids as Potential Antimycobacterial Agents—The Synthesis and Biological Evaluation of Enantiomers Molecules doi: 10.3390/molecules25071518 Authors: Martin Juhás Lucie Kučerová Ondřej Horáček Ondřej Janďourek Vladimír Kubíček Klára Konečná Radim Kučera Pavel Bárta Jiří Janoušek Pavla Paterová Jiří Kuneš Martin Doležal Jan Zitko Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis (Mtb), each year causing millions of deaths. In this article, we present the synthesis and biological evaluations of new potential antimycobacterial compounds containing a fragment of the first-line antitubercular drug pyrazinamide (PZA), coupled with methyl or ethyl esters of selected amino acids. The antimicrobial activity was evaluated on a variety of (myco)bacterial strains, including Mtb H37Ra, M. smegmatis, M. aurum, Staphylococcus aureus, Pseudomonas aeruginosa, and fungal strains, including Candida albicans and Aspergillus flavus. Emphasis was placed on the comparison of enantiomer activities. None of the synthesized compounds showed any significant activity against fungal strains, and their antibacterial activities were also low, the best minimum inhibitory concentration (MIC) value was 31.25 µM. However, several compounds presented high activity against Mtb. Overa...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research

Related Links:

Authors: Carlos R, Porras L, Sánchez Sánchez R PMID: 32493620 [PubMed - as supplied by publisher]
Source: Medicina Clinica - Category: General Medicine Tags: Med Clin (Barc) Source Type: research
Publication date: Available online 4 June 2020Source: Microbial PathogenesisAuthor(s): K. Raksha Rao, A.V. Vipin, G. Venkateswaran
Source: Microbial Pathogenesis - Category: Infectious Diseases Source Type: research
Authors: Chan ED, Verma D, Ordway DJ Abstract This manuscript describes the infection of mice and guinea pigs with mycobacteria via various routes, as well as necropsy methods for the determination of mycobacterial loads within target organs. Additionally, methods for cultivating mycobacteria and preparing stocks are described. The protocols outlined are primarily used for M. tuberculosis, but can also be used for the study of other non-tuberculosis mycobacterial species. A wide variety of animal models have been used to test new vaccines, drugs, and the impact of cigarette exposure. © 2020 Wiley Periodicals L...
Source: Current Protocols in Immunology - Category: Allergy & Immunology Tags: Curr Protoc Immunol Source Type: research
Publication date: Available online 4 June 2020Source: Colloids and Surfaces B: BiointerfacesAuthor(s): Thomas J. Dauben, Carolin Dewald, Izabela Firkowska-Boden, Christian Helbing, Henrik Peisker, Martin Roth, Jörg Bossert, Klaus D. Jandt
Source: Colloids and Surfaces B: Biointerfaces - Category: Biochemistry Source Type: research
Publication date: Available online 29 January 2020Source: Journal of Molecular StructureAuthor(s): YuA. Kondratenko, A.A. Nikonorova, A.A. Zolotarev, V.L. Ugolkov, T.A. KochinaAbstractTris (hydroxymethyl)methyl ammonium salts, [C(CH2OH)3NH3]X, were obtained for the first time by the interaction of tris(hydroxymethyl)aminomethane (TRIS) with carboxylic acids (cinnamic, benzoic, salicylic, nicotinic, 2-methylphenoxyacetic, succinic, malonic, oxalic, malic and citric). The new compounds (1–15) were characterized by 1H NMR, 13C NMR, FT-IR, elemental analysis and thermal analysis methods. The crystal structures of the tri...
Source: Journal of Molecular Structure - Category: Molecular Biology Source Type: research
This study retrospectively analyzed the clinical data of 411 patients with lung cancer who were hospitalized in the First Affiliated Hospital of Zhejiang University Medical College from January 2017 to December 2018, and counted the incidence of nosocomial lung infection, pathogens, drug resistance and influencing factors. Results There were 184 cases of nosocomial pulmonary infection in 411 lung cancer patients during chemotherapy, the infection rate was 44.77%. The isolated pathogens included Gram-negative bacteria, Gram-positive bacteria, viruses, fungi and tuberculosis, among which Gram-negative bacteria accounted for ...
Source: Chinese Journal of Lung Cancer - Category: Cancer & Oncology Source Type: research
Publication date: Available online 24 September 2019Source: Journal of Molecular StructureAuthor(s): Romana Machníková, Lucie Janovská, Lucie BrulíkováAbstractHerein, we report the polymer-supported synthesis of new pyrimidine derivatives and their antimycobacterial and antimicrobial activity. Our methodology is based on the fast and efficient solid-phase synthesis having the ability to implement structural diversity from the readily available building blocks through minimum synthetic route and with high yields. Our method was validated in the synthesis of a model chemical library prepare...
Source: Journal of Molecular Structure - Category: Molecular Biology Source Type: research
Gulcin Tezcan1, Ekaterina V. Martynova1, Zarema E. Gilazieva1, Alan McIntyre2, Albert A. Rizvanov1 and Svetlana F. Khaiboullina1,3* 1Institute of Fundamental Medicine and Biology, Kazan Federal University, Kazan, Russia 2Centre for Cancer Sciences, Faculty of Medicine and Health Sciences, University of Nottingham, Nottingham, United Kingdom 3Department of Microbiology and Immunology, University of Nevada, Reno, Reno, NV, United States Inflammation has a crucial role in protection against various pathogens. The inflammasome is an intracellular multiprotein signaling complex that is linked to pathogen sensing and...
Source: Frontiers in Pharmacology - Category: Drugs & Pharmacology Source Type: research
In this study they also showed PTX3 localized in NETs formed after neutrophil activation (5). Proteomics analysis revealed that PTX3 forms complexes with two anti-microbial proteins [azurocidin (AZU1) and myeloperoxidase (MPO)] associated to NETs (30). More recently, PTX3 localization in NETs has been confirmed, and the colocalization with AZU1 and MPO has been defined more accurately (31). Further investigation will be needed to understand the involvement of PTX3 interaction with AZU1 and MPO in their antibacterial role during NET formation. Regulation of Complement Activation PTX3 interaction with microorganisms is not...
Source: Frontiers in Immunology - Category: Allergy & Immunology Source Type: research
Publication date: Available online 29 January 2019Source: Journal of Molecular StructureAuthor(s): Veronika Šlachtová, Lucie Janovská, Lucie BrulíkováAbstractThe polymer-supported synthetic protocol for preparation of thiazolidinedione-pyrimidine hybrids was developed and applied for rapid and effective synthesis of a library of variously substituted conjugates. Reported synthetic methodology is based on easy accessible building blocks and very simple chemical operations enabling effective development of potent experimental therapeutics of this type via a combinatorial manner. Synthesized...
Source: Journal of Molecular Structure - Category: Molecular Biology Source Type: research
More News: Aspergillus | Candida | Chemistry | Infectious Diseases | Staphylococcus Aureus | Study | Tuberculosis