Abstract:
:Background: A major focus of tuberculosis drug discovery is aimed at the development of novel antibiotics with activity against drug-resistant strains of Mycobacterium tuberculosis. Results: We have synthesized ten isoniazid derivatives and investigated for antibacterial activity toward M. tuberculosis H37Rv and isoniazid-resistant strain SRI 1369. It was revealed that only one compound, isonicotinic acid (1-methyl-1H-pyrrol-2-ylmethylene)-hydrazide (1), is active toward isoniazid-resistant strain with minimum inhibitory concentration value of 0.14 μM. This compound is not cytotoxic toward human liver cells (HepG2; IC50 >100 μM), demonstrates good permeability in Caco-2 cells. Accordingly to the results of plasma protein binding assay, unbound fraction of compound 1, which potentially exhibits pharmacologic effects, is 57.9%. Conclusion: Therefore, isonicotinic acid (1-methyl-1H-pyrrol-2-ylmethylene)-hydrazide is a promising compound for further preclinical studies.
journal_name
Future Microbioljournal_title
Future microbiologyauthors
Volynets GP,Tukalo MA,Bdzhola VG,Derkach NM,Gumeniuk MI,Tarnavskiy SS,Yarmoluk SMdoi
10.2217/fmb-2019-0085subject
Has Abstractpub_date
2020-07-01 00:00:00pages
869-879eissn
1746-0913issn
1746-0921journal_volume
15pub_type
杂志文章abstract::Histoplasma capsulatum, an environmental fungus, is the most common endemic pulmonary mycosis in the USA. Disease is most frequently observed in immunocompromised patients living in endemic areas. We present the mechanisms of fungal recognition, innate immune response and adaptive immune response that lead to protecti...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/fmb.15.25
更新日期:2015-01-01 00:00:00
abstract:AIM:The aim was to evaluate the in vitro activity of fosfomycin against common uropathogens in a fosfomycin-naive population in India. METHODS:The authors prospectively collected and tested all consecutive isolates of Escherichia coli and Enterococcus spp. from urine samples between December 2009 and April 2010. RESU...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb.13.31
更新日期:2013-05-01 00:00:00
abstract::Living organisms adapt to the dynamic external environment for their survival. Environmental adaptation in prokaryotes is thought to be primarily accomplished by signaling events mediated by two-component systems, consisting of histidine kinases and response regulators. However, eukaryotic-like serine/threonine kinase...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/fmb.11.62
更新日期:2011-07-01 00:00:00
abstract:AIM:This study aims to evaluate the genetic and population structure of Vibrio parahaemolyticus in the major coastal regions of China. MATERIALS & METHODS:Multilocus sequence typing was performed. RESULTS:Insertion of large sequence into recA happened in nearly 30 strains, which were untypeable by multilocus sequence...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb-2018-0060
更新日期:2018-09-01 00:00:00
abstract:AIMS:AFN-1252 is a novel inhibitor of FabI, an essential enzyme in Staphylococcus spp. This study was undertaken to assess the safety, tolerability and pharmacokinetic properties of AFN-1252, following oral administration in an ascending dose trial. MATERIALS & METHODS:This was a double-blind, randomized, placebo-cont...
journal_title:Future microbiology
pub_type: 杂志文章,随机对照试验
doi:10.2217/fmb.15.101
更新日期:2015-01-01 00:00:00
abstract::Background: Sporotrichosis occurs through contact with contaminated soil and plant. However, the incidence of sporotrichosis as a zoonotic epidemic has increased, particularly in Rio de Janeiro. Aim: In this work, we decided to evaluate some T-cell phenotypes involved in the immune response. Materials & methods: We us...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb-2020-0046
更新日期:2020-09-01 00:00:00
abstract::Salmonella enterica serovars Typhi and Paratyphi are the causative agents of human typhoid fever. Current typhoid vaccines are ineffective and are not widely used in endemic areas. Greater understanding of host-pathogen interactions during Salmonella infection should facilitate the development of improved vaccines to ...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/fmb.14.98
更新日期:2015-01-01 00:00:00
abstract::Group A Streptococcus (GAS) is a leading human bacterial pathogen with diverse clinical manifestations. Macrophages constitute a critical first line of host defense against GAS infection, using numerous surface and intracellular receptors such as Toll-like receptors and inflammasomes for pathogen recognition and activ...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/fmb-2017-0142
更新日期:2018-01-01 00:00:00
abstract::Atomic force microscopy (AFM) has recently opened a variety of novel possibilities for imaging and manipulating microbial surfaces in their native environment. While AFM imaging offers a means to visualize surface structures at high resolution and in physiological conditions, AFM force spectroscopy enables researchers...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/17460913.1.4.387
更新日期:2006-12-01 00:00:00
abstract::Background: There is increasing evidence of the association between microbiome dysfunction and Parkinson's disease (PD). Moreover, some PD patients suffer from unintentional weight loss (WL) which may precede the motor manifestations of the disease. Materials & methods: Gut microbiota profiling by 16S rRNA gene sequen...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb-2019-0336
更新日期:2020-09-01 00:00:00
abstract::Report from the 28th European Congress of Clinical Microbiology and Infectious Diseases (ECCMID 2018), Madrid, Spain, 21-24 April 2018 Gram-negative bacteria such as Klebsiella, Acinetobacter and Pseudomonas cause some of the most serious infections and are increasingly resistant to multiple drugs and in some cases, t...
journal_title:Future microbiology
pub_type:
doi:10.2217/fmb-2018-0202
更新日期:2018-10-01 00:00:00
abstract:AIM:Presenting the first clinical case of Wickerhamomyces myanmarensis. PATIENTS & METHODS:Yeast cells were isolated from blood and central venous catheter of a 5.5-year-old male subject. API 20C AUX, MALDI-TOF MS, ITS and LSU rDNA sequencing, and our qPCR assay were used for identification and the MIC values were det...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb-2018-0253
更新日期:2019-03-01 00:00:00
abstract::Traditionally, the patients believed to be at highest risk of invasive aspergillosis (IA) are those who are neutropenic due to chemotherapy for hematological malignancy or those undergoing allogeneic hematopoietic stem cell transplantation. However, emerging data show that other patients are vulnerable to IA, even tho...
journal_title:Future microbiology
pub_type:
doi:10.2217/fmb.10.73
更新日期:2010-07-01 00:00:00
abstract::Evaluation of: Mowat E, Butcher J, Lang S, Williams C, Ramage G: Development of a simple model for studying the effects of antifungal agents on multicellular communities of Aspergillus fumigatus. J. Med. Microbiol. 56, 1205-1212 (2007). Many microorganisms possess the innate ability for adhering to biotic and abiotic ...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/17460913.3.1.19
更新日期:2008-02-01 00:00:00
abstract::The obligate intracellular bacterial pathogen Chlamydia trachomatis is a major cause of blindness and sexually transmitted diseases. Like the enteric pathogens Salmonella and Shigella, Chlamydia injects effector proteins into epithelial cells to initiate extensive remodeling of the actin cytoskeleton at the bacterial ...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/fmb.10.77
更新日期:2010-08-01 00:00:00
abstract::Cooling towers provide a favorable environment for the proliferation of microorganisms. Cooling towers generate a biofilm and often aerosolize contaminated water, thereby increasing the risk of microorganism dissemination by human inhalation. This pathogen dissemination was first revealed by the epidemics of Legionnai...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/fmb.09.25
更新日期:2009-06-01 00:00:00
abstract::Streptococcus pneumoniae (the pneumococcus) is a major global cause of human disease. Since the publication of the entire sequence of TIGR4 in 2001, our understanding of this human pathogen has increased significantly. Genetic studies, and the use of mutant strains have refined our understanding of the pathogenic mech...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/17460913.3.2.205
更新日期:2008-04-01 00:00:00
abstract::Helicobacter pylori is arguably one of the most successful pathogens; it colonizes the stomachs of more than half of the human population. Colonization and persistence in such an inhospitable niche requires the presence of exquisite adaptive mechanisms. One of the proteins that contributes significantly to the remarka...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/fmb.13.43
更新日期:2013-06-01 00:00:00
abstract::Surgical procedures for the symptomatic removal of the gallbladder and the vermiform appendix have been posited to adversely shift the assemblage of the intestinal microbiome increasing the risk of disease. The associated mechanisms have been linked with dysbiosis of the gut microbiota. Cholecystectomy causes changes ...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb-2019-0325
更新日期:2020-05-01 00:00:00
abstract::Aim: Face masks are an important addition to our arsenal in the fight against COVID-19. The aim of this study is to present a novel method of measuring mask performance which can simultaneously assess both fabric penetration and leakage due to poor fit. Materials & methods: A synthetic aerosol is introduced into the l...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb-2020-0292
更新日期:2021-01-01 00:00:00
abstract::Staphylococcus aureus is a major human pathogen responsible for a wide diversity of infections ranging from localized to life threatening diseases. From 1961 and the emergence of methicillin-resistant S. aureus (MRSA), this bacterium has shown a particular capacity to survive and adapt to drastic environmental changes...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb.11.38
更新日期:2011-05-01 00:00:00
abstract::Currently, there is growing interest in the identification and purification of microbial lectins due to their involvement in the pathogenicity mechanisms of pathogens, such as Entamoeba histolytica and free-living amoebae. The Gal/GalNAc lectin from E. histolytica participates in adhesion, cytotoxicity and regulation ...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb-2019-0275
更新日期:2020-07-01 00:00:00
abstract:AIMS:To investigate whether Cek2 (as Cek1) is involved in the biogenesis of the fungal cell wall and to uncover differences and similitudes between both proteins. MATERIALS & METHODS:We used molecular genetics to characterize the role of Cek2 in MTL-heterozygous cells. RESULTS:Deletion of CEK2 (similar to CEK1) rende...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb.15.127
更新日期:2016-01-01 00:00:00
abstract::Aim: Bile salts promote the specific autolysis of pneumococcal cells, allowing the differentiation between Streptococcus pneumoniae and other viridans group streptococci (VGS). Material & methods: One hundred clinical VGS isolates identified by amplification and sequencing of 16S rRNA, groEL and sodA genes were analyz...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb-2019-0073
更新日期:2019-07-01 00:00:00
abstract::In this Phase I study, healthy volunteers (n = 24) were randomly allocated to receive either one or two 0.2-g applications per day (12 h apart) of ozenoxacin 2% cream on three different areas of the back for 3 consecutive days. Ozenoxacin concentrations were measured in tape stripping samples (from the stratum corneum...
journal_title:Future microbiology
pub_type: 杂志文章,随机对照试验
doi:10.2217/fmb.14.83
更新日期:2014-01-01 00:00:00
abstract::The Enterococcus species is the third main cause of infective endocarditis (IE) worldwide, and it is gaining relevance, especially among healthcare-associated cases. Patients with enterococcal IE are older and have more comorbidities than other types of IE. Classical treatment options are limited due to the emergence ...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/fmb.15.46
更新日期:2015-01-01 00:00:00
abstract::Most humans are infected with herpes simplex virus (HSV) type 1 in early childhood and remain latently infected throughout life. While most individuals have mild or no symptoms, some will develop destructive HSV keratitis. Ocular infection with HSV-1 and its associated sequelae account for the majority of corneal blin...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/fmb.11.73
更新日期:2011-08-01 00:00:00
abstract::Cytomegalovirus (CMV) manifestations remain important complications after allogeneic hematopoietic stem cell transplantation (HSCT), even in the current era. Unfortunately, available anti-CMV agents, mainly viral polymerase inhibitors, have a substantial risk of myelosuppression and nephrotoxicity. Letermovir, a novel...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb-2018-0250
更新日期:2019-02-01 00:00:00
abstract:AIM:The purpose of current study is to find out relationship between cas9 gene and antimicrobial resistance in Campylobacter jejuni NCTC11168. MATERIALS & METHODS:The involvement of the cas9 gene in antimicrobial resistance of C. jejuni was determined by assessment of minimum inhibitory concentration, clustered regula...
journal_title:Future microbiology
pub_type: 杂志文章
doi:10.2217/fmb-2018-0234
更新日期:2018-12-01 00:00:00
abstract::Mycobacterium tuberculosis is included among a select group of bacteria possessing the capacity for de novo biosynthesis of vitamin B12, the largest and most complex natural organometallic cofactor. The bacillus is also able to scavenge B12 and related corrinoids utilizing an ATP-binding cassette-type protein that is ...
journal_title:Future microbiology
pub_type: 杂志文章,评审
doi:10.2217/fmb.13.113
更新日期:2013-11-01 00:00:00