Recent Developments in Azole Compounds as Antitubercular Agent

Tuberculosis (TB) is a global health disaster and is a wide-reaching hitch. The improper use of antibiotics in chemotherapy of TB patients led to the current problem of tuberculosis therapy which gives rise to Multi-Drug Resistant (MDR) strains. Nitrogen heterocycles including azole compounds are an important class of therapeutic agent with electron-rich property. Azole-based derivatives easily bind with the enzymes and receptors in organisms through noncovalent interactions, thereby possessing various applications in medicinal chemistry. Research on azoles derivatives have been expansively carried out and have become one of the extremely active area in recent years and the progress is quite rapid. A genuine attempt to review chemistry of azoles and to describe various azole-based compounds synthesized in the last two decades having promising antitubercular potential is described in the present article. It is hopeful that azole compounds may continue to serve as an important direction for the exploitation of azole-based antitubercular drugs with better curative effect, lower toxicity, less side effects, especially fewer resistances and so on.

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Collaborative Research Funding

Chemistry International ◽

10.1515/ci.2014.36.4.4 ◽

2014 ◽

Vol 36 (4) ◽

Cited By ~ 1

Author(s):

Markus Behnke ◽

Laura McConnell ◽

Chris Ober

Keyword(s):

International Collaboration ◽

Research Funding ◽

International Committee ◽

Research Projects ◽

Scientific Success ◽

Funding Sources ◽

Chemistry Research ◽

National Organizations ◽

Recent Developments ◽

History Of

Within a changing research world, international collaboration has become even more important in achieving scientific success. Given the increased need and desire for multinational research, the actors are forced to identify appropriate funding sources. Whereas, science knows no international boundaries, support for scientific research, including in chemical sciences, is mostly provided by the national funding organizations. This is particularly true for the chemical sciences, where most research projects are relatively small in size and with respect to the number of involved PIs. Traditionally, national organizations are reluctant to provide funds to non-domestic researchers, and in practice, funding truly international research projects can be a real challenge for a variety of technical and bureaucratic reasons. In an effort to change this, an international Committee on Chemistry Research Funding (CCRF)—backed by several leading funding organizations—was established by IUPAC in December 2007 to promote increased international collaboration and networking in the global chemistry community. The following report gives a short overview on the history of IUPAC’s involvement in service for chemistry research funding and on the most recent developments.

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Ribosome Rescue Pathways in Bacteria

Frontiers in Microbiology ◽

10.3389/fmicb.2021.652980 ◽

2021 ◽

Vol 12 ◽

Author(s):

Claudia Müller ◽

Caillan Crowe-McAuliffe ◽

Daniel N. Wilson

Keyword(s):

Messenger Rna ◽

Pathogenic Bacteria ◽

Antimicrobial Agents ◽

Polypeptide Chain ◽

Drug Resistant ◽

Bacterial Survival ◽

Gram Positive Bacteria ◽

Small Protein B ◽

Recent Developments ◽

Rescue System

Ribosomes that become stalled on truncated or damaged mRNAs during protein synthesis must be rescued for the cell to survive. Bacteria have evolved a diverse array of rescue pathways to remove the stalled ribosomes from the aberrant mRNA and return them to the free pool of actively translating ribosomes. In addition, some of these pathways target the damaged mRNA and the incomplete nascent polypeptide chain for degradation. This review highlights the recent developments in our mechanistic understanding of bacterial ribosomal rescue systems, including drop-off, trans-translation mediated by transfer-messenger RNA and small protein B, ribosome rescue by the alternative rescue factors ArfA and ArfB, as well as Bacillus ribosome rescue factor A, an additional rescue system found in some Gram-positive bacteria, such as Bacillus subtilis. Finally, we discuss the recent findings of ribosome-associated quality control in particular bacterial lineages mediated by RqcH and RqcP. The importance of rescue pathways for bacterial survival suggests they may represent novel targets for the development of new antimicrobial agents against multi-drug resistant pathogenic bacteria.

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Antimicrobial Applications of Nanoparticles

10.4018/978-1-7998-8936-6.ch012 ◽

2022 ◽

pp. 269-288

Author(s):

Ayesha Kanwal ◽

Zeeshan Ahmad Bhutta ◽

Ambreen Ashar ◽

Ashar Mahfooz ◽

Rizwan Ahmed ◽

...

Keyword(s):

Antibacterial Activity ◽

Side Effects ◽

Antibacterial Agent ◽

Antibacterial Agents ◽

The Other ◽

Drug Resistant ◽

Short Term ◽

Human Mortality ◽

Recent Developments

Human mortality due to drug-resistant infections is becoming more prevalent in our society. Antibiotics are impotent due to abuse and/or misuse, leading to new, more expensive, and more effective medicines and treatments. Therefore, it causes many short-term and long-term side effects in the patient. On the other hand, nanoparticles have exhibited antibacterial activity against various pathogens due to their small size and ability to destroy cells by various mechanisms. Unlike antibiotics for the treatment of patients' diseases and infections, nanomaterials provide an exciting way to limit the growth of microorganisms due to infections in humans. This has led to the development of a number of nanoparticles as active antibacterial agents. Therefore, the authors have carefully reviewed the recent developments in the use of nanomaterials for antibacterial applications and the mechanisms that make them an effective alternate antibacterial agent.

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DRUG-RESISTANT TUBERCULOSIS: RECENT APPROACH IN POLYMER BASED NANOMEDICINE

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2016v8i10.11295 ◽

2016 ◽

Vol 8 (10) ◽

pp. 1 ◽

Cited By ~ 1

Author(s):

Jessy Shaji ◽

Mahmood Shaikh

Keyword(s):

Drug Delivery ◽

Side Effects ◽

Pulmonary Drug Delivery ◽

Symbiotic Association ◽

Drug Resistant ◽

Second Line ◽

Antitubercular Drugs ◽

Recent Approach ◽

Mdr Tb ◽

High Doses

<p>Tuberculosis (TB) had been a leading chronic bacterial infection since decades. Current therapeutic management of Mycobacterium tuberculosis (MTB) is inadequate due to the lengthy course of treatment, drug-related side effects and ill-planned therapy, and these factors can lead to therapeutic failure and the emergence of drug-resistant TB. The Multi-drug-resistant (MDR) TB needs a lengthy course of treatment with second-line antitubercular drugs (ATDs) having higher side effects and cost. The misuse of second-line ATDs may result in extremely drug-resistant (XDR) strain which is very difficult to treat and require high doses of drugs resulting in more toxicity and side effects. This review highlights the need for novel drug delivery for the treatment of drug-susceptible and resistant TB. The characteristics of the nanoparticulate system in ATDs delivery and its approach in the MDR and XDR TB are discussed. The lung is the site of infection in pulmonary TB and the targeted drug delivery to the site of infection helps in achieving increased efficacy with less dose further reducing the side effects and toxicity. The symbiotic association of nanotechnology and pulmonary drug delivery give rise to an efficient inhalable polymer based nanoparticulate system containing ATDs for the better management of drug-susceptible and resistant TB. Various ATDs loaded polymer based nanocarrier systems like Alginate, PLGA, Chitosan and Gelatin nanocarriers are discussed in detail. Thus, this review highlights the current research in pulmonary drug delivery of polymer based ATDs nanomedicine and their importance in control of drug-resistant TB.</p>

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Physics Comes to the Aid of Medicine—Clinically-Relevant Microorganisms through the Eyes of Atomic Force Microscope

Pathogens ◽

10.3390/pathogens9110969 ◽

2020 ◽

Vol 9 (11) ◽

pp. 969

Author(s):

Mateusz Cieśluk ◽

Piotr Deptuła ◽

Ewelina Piktel ◽

Krzysztof Fiedoruk ◽

Łukasz Suprewicz ◽

...

Keyword(s):

Mammalian Cells ◽

Antimicrobial Agents ◽

Antimicrobial Treatment ◽

Point Of View ◽

Diagnostic Methods ◽

Drug Resistant ◽

Bacterial Strains ◽

Force Microscopy ◽

Atomic Force ◽

Recent Developments

Despite the hope that was raised with the implementation of antibiotics to the treatment of infections in medical practice, the initial enthusiasm has substantially faded due to increasing drug resistance in pathogenic microorganisms. Therefore, there is a need for novel analytical and diagnostic methods in order to extend our knowledge regarding the mode of action of the conventional and novel antimicrobial agents from a perspective of single microbial cells as well as their communities growing in infected sites, i.e., biofilms. In recent years, atomic force microscopy (AFM) has been mostly used to study different aspects of the pathophysiology of noninfectious conditions with attempts to characterize morphological and rheological properties of tissues, individual mammalian cells as well as their organelles and extracellular matrix, and cells’ mechanical changes upon exposure to different stimuli. At the same time, an ever-growing number of studies have demonstrated AFM as a valuable approach in studying microorganisms in regard to changes in their morphology and nanomechanical properties, e.g., stiffness in response to antimicrobial treatment or interaction with a substrate as well as the mechanisms behind their virulence. This review summarizes recent developments and the authors’ point of view on AFM-based evaluation of microorganisms’ response to applied antimicrobial treatment within a group of selected bacteria, fungi, and viruses. The AFM potential in development of modern diagnostic and therapeutic methods for combating of infections caused by drug-resistant bacterial strains is also discussed.

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Inhalable Spray-Dried Chondroitin Sulphate Microparticles: Effect of Different Solvents on Particle Properties and Drug Activity

Polymers ◽

10.3390/polym12020425 ◽

2020 ◽

Vol 12 (2) ◽

pp. 425 ◽

Cited By ~ 3

Author(s):

Susana Rodrigues ◽

Ana da Costa ◽

Noelia Flórez-Fernández ◽

María Torres ◽

Maria Faleiro ◽

...

Keyword(s):

Spray Drying ◽

Chondroitin Sulphate ◽

Antitubercular Activity ◽

Particle Fraction ◽

First Line ◽

Antitubercular Drugs ◽

Particle Properties ◽

Aerodynamic Properties ◽

Tuberculosis Therapy ◽

Spray Dried

Spray-drying stands as one of the most used techniques to produce inhalable microparticles, but several parameters from both the process and the used materials affect the properties of the resulting microparticles. In this work, we describe the production of drug-loaded chondroitin sulphate microparticles by spray-drying, testing the effect of using different solvents during the process. Full characterisation of the polymer and of the aerodynamic properties of the obtained microparticles are provided envisaging an application in inhalable tuberculosis therapy. The spray-dried microparticles successfully associated two first-line antitubercular drugs (isoniazid and rifabutin) with satisfactory production yield (up to 85%) and drug association efficiency (60%–95%). Ethanol and HCl were tested as co-solvents to aid the solubilisation of rifabutin and microparticles produced with the former generally revealed the best features, presenting a better ability to sustainably release rifabutin. Moreover, these presented aerodynamic properties compatible with deep lung deposition, with an aerodynamic diameter around 4 μm and fine particle fraction of approximately 44%. Finally, it was further demonstrated that the antitubercular activity of the drugs remained unchanged after encapsulation independently of the used solvent.

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Biomolecular Simulations: Recent Developments in Force Fields, Simulations of Enzyme Catalysis, Protein-Ligand, Protein-Protein, and Protein-Nucleic Acid Noncovalent Interactions

Annual Review of Biophysics and Biomolecular Structure ◽

10.1146/annurev.biophys.30.1.211 ◽

2001 ◽

Vol 30 (1) ◽

pp. 211-243 ◽

Cited By ~ 355

Author(s):

Wei Wang ◽

Oreola Donini ◽

Carolina M. Reyes ◽

Peter A. Kollman

Keyword(s):

Nucleic Acid ◽

Enzyme Catalysis ◽

Force Fields ◽

Noncovalent Interactions ◽

Recent Developments ◽

Biomolecular Simulations ◽

Protein Nucleic Acid

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Discovery of Low-Molecular Weight Antagonists of Substance P: Recent Developments and Prospects as a Therapeutic Agent.

Journal of Synthetic Organic Chemistry Japan ◽

10.5059/yukigoseikyokaishi.52.445 ◽

1994 ◽

Vol 52 (5) ◽

pp. 445-452

Author(s):

Daijiro HAGIWARA

Keyword(s):

Molecular Weight ◽

Substance P ◽

Therapeutic Agent ◽

Low Molecular Weight ◽

Recent Developments

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RECENT ADVANCES IN ELECTRONIC STRUCTURE THEORY

Journal of Theoretical and Computational Chemistry ◽

10.1142/s0219633602000105 ◽

2002 ◽

Vol 01 (01) ◽

pp. 109-136 ◽

Cited By ~ 6

Author(s):

TAKAHITO NAKAJIMA ◽

TAKAO TSUNEDA ◽

HARUYUKI NAKANO ◽

KIMIHIKO HIRAO

Keyword(s):

Computational Chemistry ◽

Density Functional ◽

Relativistic Effects ◽

Molecular Theory ◽

Structure Theory ◽

Functional Theory ◽

Molecular Systems ◽

Chemistry Research ◽

Ab Initio Theory ◽

Recent Developments

Accurate quantum computational chemistry has evolved dramatically. The size of molecular systems, which can be studied accurately using molecular theory is increasing very rapidly. Theoretical chemistry has opened up a world of new possibilities. It can treat real systems with predictable accuracy. Computational chemistry is becoming an integral part of chemistry research. Theory can now make very significant contribution to chemistry. This review will focus on our recent developments in the theoretical and computational methodology for the study of molecular structure and molecular interactions. We are aiming at developing accurate molecular theory on systems containing hundreds of atoms. We continue our research in the following three directions: (i) development of new ab initio theory, particularly multireference-based perturbation theory, (ii) development of exchange and correlation functionals in density functional theory, and (iii) development of molecular theory including relativistic effects. We have enjoyed good progress in each of the above areas. We are very excited about our discoveries of new theory and new algorithms and would like to share this enthusiasm with readers.

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