FDA’s Limited Population Pathway for Antibacterial and Antifungal Drugs

2021 ◽  
Vol 109 (4) ◽  
pp. 813-815
Author(s):  
Sumathi Nambiar ◽  
Sarah Walinsky ◽  
Katherine Schumann
Keyword(s):  
Antifungal Drugs ◽  
Antibacterial And Antifungal

scholarly journals Ribosomally derived lipopeptides containing distinct fatty acyl moieties

2022 ◽  
Vol 119 (3) ◽  
pp. e2113120119
Author(s):  
Florian Hubrich ◽  
Nina M. Bösch ◽  
Clara Chepkirui ◽  
Brandon I. Morinaka ◽  
Michael Rust ◽  
...  
Keyword(s):  
Natural Products ◽  
Cyclic Peptide ◽  
Fatty Acyl ◽  
Antifungal Drugs ◽  
Guided Discovery ◽  
Bacterial Phyla ◽  
Peptide Synthetases ◽  
Antibacterial And Antifungal ◽  
Microbial Natural Products

Lipopeptides represent a large group of microbial natural products that include important antibacterial and antifungal drugs and some of the most-powerful known biosurfactants. The vast majority of lipopeptides comprise cyclic peptide backbones N-terminally equipped with various fatty acyl moieties. The known compounds of this type are biosynthesized by nonribosomal peptide synthetases, giant enzyme complexes that assemble their products in a non–gene-encoded manner. Here, we report the genome-guided discovery of ribosomally derived, fatty-acylated lipopeptides, termed selidamides. Heterologous reconstitution of three pathways, two from cyanobacteria and one from an arctic, ocean-derived alphaproteobacterium, allowed structural characterization of the probable natural products and suggest that selidamides are widespread over various bacterial phyla. The identified representatives feature cyclic peptide moieties and fatty acyl units attached to (hydroxy)ornithine or lysine side chains by maturases of the GCN5-related N-acetyltransferase superfamily. In contrast to nonribosomal lipopeptides that are usually produced as congener mixtures, the three selidamides are selectively fatty acylated with C10, C12, or C16 fatty acids, respectively. These results highlight the ability of ribosomal pathways to emulate products with diverse, nonribosomal-like features and add to the biocatalytic toolbox for peptide drug improvement and targeted discovery.

scholarly journals Synthesis, Molecular Docking and Evaluation of Library of 3-Mercapto-1,2,4-Triazole Derivatives as Antimicrobial Agents

2021 ◽  
Vol 33 (12) ◽  
pp. 3039-3046
Author(s):  
Swarnagowri Nayak ◽  
Santosh L. Gaonkar ◽  
Sushruta S. Hakkimane ◽  
Swapna B ◽  
Nitinkumar S. Shetty
Keyword(s):  
Antimicrobial Activity ◽  
Molecular Docking ◽  
In Silico ◽  
Structural Modification ◽  
Antimicrobial Agents ◽  
Antifungal Drugs ◽  
Aromatic Acids ◽  
Triazole Derivatives ◽  
In Silico Study ◽  
Antibacterial And Antifungal

Due to the increasing microbial resistance to antibacterial and antifungal drugs, the development of new antimicrobial agents is an urgent priority. In search of newer antimicrobial agents, a series of 4,5-disubstituted-3-mercapto-1,2,4-triazole derivatives were synthesized from aromatic acids and substituted isothiocyanates. The in silico study was performed to study the binding interactions of the synthesized compounds with the active pocket of CYP51. Among the synthesized 3-mercapto-triazole derivatives, compounds 6r, 6s and 6u exhibited promising antimicrobial activity comparable to standard drugs. The results suggested that the structural modification to 3-mercapto-1,2,4-triazole derivatives could lead to promising antimicrobial scaffolds.

scholarly journals Clinical practice of managing corneal ulcer of unknown etiology with pro-tracted course in presence of toxic and allergic component

2021 ◽  
pp. 58-65
Author(s):  
D.Y. Maychuk ◽  
◽  
A. A. Tarkhanova ◽  
A.O. Loshkareva ◽  
I. A. Drozdkov ◽  
...  
Keyword(s):  
Allergic Reaction ◽  
Corneal Ulcer ◽  
Positive Response ◽  
Antifungal Drugs ◽  
Response To Treatment ◽  
Unknown Etiology ◽  
The Subject ◽  
Long Term Observation ◽  
Antibacterial And Antifungal

Purpose. The representation of the clinical case of corneal ulcer course with unknown etiology in presence of patient's acute toxic and allergic reaction. The patient was under long-term observation of the local ophthalmologist and didn't show positive response to treatment. Material and methods. Patient examination on the date of his encounter sug-gested bacterial etiology of the process. However, the etiological factor wasn't re-vealed by laboratory tests. The presence of toxic and allergic components in biomi-croscopy of both eyes, long-term prestudy antibacterial therapy, character of corneal ulcer gave rise to prescription of the therapy. Results. The main areas of the therapy are allergy medications, antibacterial and antifungal drugs. The positive response in the disease course allowed us to be-lieve that the treatment was accurately prescribed Conclusion. Protracted course of the corneal ulcer without positive response is the subject to estimate the presence of toxic and allergic components. Considering the duration of the disease the antifungal drugs were prescribed at the beginning of the therapy, in spite of the assumption that bacterial etiology of the process may take place. Keywords: corneal ulcer, toxic and allergic reaction.

Integration of Bioinformatics and in vitro Analysis Reveal Anti-leishmanial Effects of Azithromycin and Nystatin

2019 ◽  
Vol 14 (5) ◽  
pp. 450-459
Author(s):  
Irum Jehangir ◽  
Syed Farhan Ahmad ◽  
Maryam Jehangir ◽  
Anwar Jamal ◽  
Momin Khan
Keyword(s):  
In Silico ◽  
Dosage Form ◽  
Antifungal Drugs ◽  
Pure Form ◽  
Potential Candidate ◽  
Leishmania Tropica ◽  
Ic50 Value ◽  
Antibacterial And Antifungal ◽  
Better Than

Background: Leishmaniasis is the major cause of mortality in under-developed countries. One of the main problems in leishmaniasis is the limited number of drug options, resistance and side effects. Such a situation requires to study the new chemical series with anti-leishmanial activity. Objective: To assess the anti-leishmanial activity of antibacterial and antifungal drugs. Methods: We have applied an integrative approach based on computational and in vitro methods to elucidate the efficacy of different antibacterial and antifungal drugs against Leishmania tropica (KWH23). Firstly these compounds were analyzed using in silico molecular docking. This analysis showed that the nystatin and azithromycin interacted with the active site amino acids of the target protein leishmanolysin. The nystatin, followed by azithromycin, produced the lowest binding energies indicating their inhibitive activity against the target. The efficacy of the docked drugs was further validated in vitro which showed that our bioinformatics based predictions completely agreed with experimental results. Stock solutions of drugs, media preparation and parasites cultures were performed according to the standard in-vitro protocol. Results: We found that the half maximal inhibitory concentration (IC50) value of dosage form of nystatin (10,000,00 U) and pure nystatin was 0.05701 µM and 0.00324 µM respectively. The IC50 value of combined azithromycin and nystatin (dosage and pure form) was 0.156 µg/ml and 0.0023 µg /ml (0.00248 µM) respectively. It was observed that IC50 value of nystatin is better than azithromycin and pure form of drugs had significant activity than the dosage form of drugs. Conclusion: From these results, it was also proven that pure drugs combination result is much better than all tested drugs results. The results of both in vitro and in silico studies clearly indicated that comparatively, nystatin is the potential candidate drug in combat against Leishmania tropica.

scholarly journals New Insights into theIn VitroSusceptibility of Pythium insidiosum

2014 ◽  
Vol 58 (12) ◽  
pp. 7534-7537 ◽  
Author(s):  
Érico S. Loreto ◽  
Juliana S. M. Tondolo ◽  
Maiara B. Pilotto ◽  
Sydney H. Alves ◽  
Janio M. Santurio
Keyword(s):  
Protein Synthesis ◽  
Antifungal Drugs ◽  
Disk Diffusion ◽  
Broth Microdilution ◽  
Promising Candidate ◽  
Pythium Insidiosum ◽  
Content Type ◽  
Zones Of Inhibition ◽  
Antibacterial And Antifungal

ABSTRACTWe have determined thein vitroactivity of several antibacterial and antifungal drugs againstPythium insidiosumusing broth microdilution (BMD), disk diffusion, and Etest methods. The largest zones of inhibition (disk diffusion) and the lowest BMD and Etest MICs were observed for azithromycin, clarithromycin, linezolid, mupirocin, doxycycline, minocycline, and tigecycline. Thein vitroactivities observed suggest that antibacterials, which act by inhibiting protein synthesis, are promising candidate therapies for the treatment of pythiosis.

scholarly journals Financial accounts reports

2005 ◽  
Vol 11 (4) ◽  
Author(s):  
Colin Aaronson
Keyword(s):  
Stock Exchange ◽  
Antifungal Drugs ◽  
Biotechnology Company ◽  
Wholly Owned Subsidiary ◽  
Antibacterial And Antifungal ◽  
Swiss Stock Exchange

Basilea Pharmaceutica AG is a Swiss-based biotechnology company whose shares are traded on the Swiss Stock Exchange. It is developing antibacterial and antifungal drugs along with dermatology treatments. The company was founded in October 2000 as a wholly owned subsidiary of F. Hoffmann-La Roche, which subsequently sold over half of the company's shares to other investors but retained approximately 33 per cent of the company at 31st December, 2004. The company's pipeline consists of the following compounds:

scholarly journals SYNTHESIS AND INVESTIGATION OF ANTIMICROBIAL ACTIVITY OF THE NEW CLASS OF ACYLHYDROSONES (QUINOLIN-8-YL) OF GLYCOLIC ACID

2021 ◽  
Vol 19 (4) ◽  
Author(s):  
V.O. Chornous ◽  
A.M. Grosav ◽  
M.K. Bratenko ◽  
S.Ye. Deineka ◽  
О.І. Gavrilyuk
Keyword(s):  
Antimicrobial Activity ◽  
Glycolic Acid ◽  
Wide Spectrum ◽  
Research Synthesis ◽  
Modern Medicine ◽  
Antifungal Drugs ◽  
Antibacterial And Antifungal Activity ◽  
Antimicrobial Drugs ◽  
New Class ◽  
Antibacterial And Antifungal

Antibiotic resistance of pathogenic strains of microorganisms is one of the most difficultproblems of modern medicine. An effective way to solve it is the synthesis of new classesof antibacterial and antifungal drugs with a wide spectrum of antiseptic action.Purpose of the research – synthesis of the new types of glycolic acid acylhydrazones(quinolin-8-yl)and investigation of their antimicrobe activity.Material and methods. The analysis of their antibacterial and antifungal activity wascarried out and the dependence of the antimicrobial action of the synthesized drugson the structure of the molecule, the type of heterocyclic fragment and the type ofmicroorganisms was investigated.Results. It was proposed a convenient method for the synthesis of new types of acylhydrosones (quinolin-8-yl) glycolic acid, which is realized by condensation ofhydrozides (quinolin-8-yl) of glycolic acid with a series of heterocyclic aldehydes.Conclusion. The results obtained indicate that this class of compounds is promising aspotential antimicrobial drugs.

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