Molecules, Vol. 25, Pages 1561: 5-Alkylamino-N-phenylpyrazine-2-carboxamides: Design, Preparation, and Antimycobacterial Evaluation

Molecules, Vol. 25, Pages 1561: 5-Alkylamino-N-phenylpyrazine-2-carboxamides: Design, Preparation, and Antimycobacterial Evaluation Molecules doi: 10.3390/molecules25071561 Authors: Weronika Ambrożkiewicz Marta Kučerová-Chlupáčová Ondřej Janďourek Klára Konečná Pavla Paterová Pavel Bárta Jarmila Vinšová Martin Doležal Jan Zitko According to the World Health Organization, tuberculosis is still in the top ten causes of death from a single infectious agent, killing more than 1.7 million people worldwide each year. The rising resistance developed by Mycobacterium tuberculosis against currently used antituberculars is an imperative to develop new compounds with potential antimycobacterial activity. As a part of our continuous research on structural derivatives of the first-line antitubercular pyrazinamide, we have designed, prepared, and assessed the in vitro whole cell growth inhibition activity of forty-two novel 5-alkylamino-N-phenylpyrazine-2-carboxamides with various length of the alkylamino chain (propylamino to octylamino) and various simple substituents on the benzene ring. Final compounds were tested against Mycobacterium tuberculosis H37Ra and four other mycobacterial strains (M. aurum, M. smegmatis, M. kansasii, M. avium) in a modified Microplate Alamar Blue Assay. We identified several candidate molecules with micromolar MIC against M. tuberculosis H37Ra and low in vitro cytot...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research

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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 causi...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research
Abstract A series of novel alkyl substituted purines were synthesized. 6-(4-(4-propoxyphenyl) piperazin-1-yl)-9 H -purine was used as the key starting material, which was synthesized via a multistep protocol and finally subjected for N-alkylation with various alkyl halides with an aim to get prospective antimicrobial agents. The structures of the novel compounds were established by substantiating them through spectral techniques like 1 H NMR, 13 C NMR, FT-IR and EI-MS. They were explored for antitubercular activity against Mycobacterium tuberculosis H37RV. Furthermore, they were checked for their antimicrobial act...
Source: Chemistry and Biodiversity - Category: Biochemistry Authors: Tags: Chem Biodivers Source Type: research
The World Health Organization (WHO) recommends that all HIV-infected individuals are screened for active tuberculosis (TB) and given isoniazid preventive therapy if active TB is not detected (WHO, 2011). The screening and diagnosis of active TB among HIV-infected individuals is an important issue for HIV care in the countries of Sub-Saharan Africa and other low-income countries. The development of practical algorithms, both for TB screening and active case-finding, is an important aspect, and the WHO TB symptom screening algorithm is recommended for screening.
Source: International Journal of Infectious Diseases - Category: Infectious Diseases Authors: Source Type: research
Authors: Meyer D, Smit DP Abstract Both infective and neoplastic eyelid and orbital conditions in human immunodeficiency virus (HIV) infected patients are often the result of opportunistic or co-infections (OI). In most cases, these clinical findings in younger patients alert the physician to suspected underlying HIV infection. When the eyelids and periorbital skin are primarily involved in OI with varicella-zoster virus it is called Herpes Zoster Ophthalmicus. Co-infection with a Pox virus manifests as molluscum contagiosum eruptions. Orbital cellulitis is secondary to various organisms (Mycobacterium tuberculosis...
Source: Ocular Immunology and Inflammation - Category: Allergy & Immunology Tags: Ocul Immunol Inflamm Source Type: research
Authors: Supriyadi R, Darmawan G, Pranggono EH Abstract Tuberculosis (TB) remains a worldwide scourge and the most common cause of mortality from infectious disease. Around 95% of cases occur in developing country. Renal TB is a rare cases that complicates 3-4% of pulmonary TB patients and commonly overlooked in clinical practice due to its symptoms may mimic other diseases.A-39-year-old man was admitted to our institution due to flank pain. He had history of low grade fever and oligouria since 5 months prior. He had no complaint of cough, dyspnea, or night sweat. He was a non smoker and had no past medical history...
Source: Acta medica Indonesiana - Category: Internal Medicine Tags: Acta Med Indones 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
Journal of Medicinal ChemistryDOI: 10.1021/acs.jmedchem.9b01561
Source: Journal of Medicinal Chemistry - Category: Chemistry Authors: 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 30 November 2019Source: Microbial PathogenesisAuthor(s): Mehdi Hadadi‐Fishani, Ali Shakerimoghaddam, Azad KhalediAbstractDiagnosis of fungal co-infections in patients suffering from pulmonary tuberculosis has critical importance. Therefore, we aimed to determine the prevalence of candida coinfection in patients with pulmonary tuberculosis.The present systematic review of cross-sectional studies was conducted based on the Preferred Reporting Items for Systematic reviews and Meta-analysis (PRISMA) Protocol. Studies published online in English from January 2001 to March 2019 were assessed....
Source: Microbial Pathogenesis - Category: Infectious Diseases Source Type: research
The Bacillus Calmette-Guérin (BCG) is a live attenuated tuberculosis vaccine that has the ability to induce non-specific cross-protection against pathogens that might be unrelated to the target disease. Vaccination with BCG reduces mortality in newborns and induces an improved innate immune response against microorganisms other than Mycobacterium tuberculosis, such as Candida albicans and Staphylococcus aureus. Innate immune cells, including monocytes and natural killer (NK) cells, contribute to this non-specific immune protection in a way that is independent of memory T or B cells. This phenomenon associated with a...
Source: Frontiers in Immunology - Category: Allergy & Immunology Source Type: research
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