scholarly journals Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening

2021 ◽  
Vol 11 (3) ◽  
pp. 1180
Author(s):  
Kinga Paruch ◽  
Łukasz Popiołek ◽  
Anna Biernasiuk ◽  
Anna Berecka-Rycerz ◽  
Anna Malm ◽  
...  

Bacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present the synthesis and evaluation of the in vitro antimicrobial activity of a series of 15 new derivatives of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid. The potential antimicrobial effect of the new compounds was observed mainly against Gram-positive bacteria. Compound 15, with the 5-nitro-2-furoyl moiety, showed the highest bioactivity: minimum inhibitory concentration (MIC) = 1.95–15.62 µg/mL and minimum bactericidal concentration (MBC)/MIC = 1–4 µg/mL.

2022 ◽  
Vol 8 (1) ◽  
Author(s):  
Shailesh Mistry ◽  
Akhilesh Kumar Singh

Abstract Background For many years, various drugs have been used for the treatment of infectious diseases but some bacterial microorganisms have induced resistance to several drugs. In a search of new antimicrobial agents, a series of new steroidal hydrazones were designed and synthesized. Result The structures of the compounds were established based on the spectral data. The in vitro antimicrobial activity of some newly synthesized compounds against bacteria and fungi was studied. Conclusion New compounds showed better or similar antimicrobial activity. Designing more efficient steroidal hydrazones from ketosteroid based on the current study may successfully lead to the development of antimicrobial agent. Graphical abstract


2016 ◽  
Vol 24 (4) ◽  
pp. 219-230 ◽  
Author(s):  
Halyna Tkachenko ◽  
Lyudmyla Buyun ◽  
Elżbieta Terech-Majewska ◽  
Zbigniew Osadowski

Abstract The main goal of this study was to determine in vitro antimicrobial activity of ethanolic extracts obtained from the leaves of various Ficus species against Aeromonas hydrophila isolated locally from infected rainbow trout (Oncorhynchus mykiss Walbaum) with the aim of providing scientific rationale for the use of the plant in the treatment of bacterial infections induced by Aeromonas spp. in fish. Antimicrobial susceptibility testing was done on Muller-Hinton agar with the disc diffusion method. In the present study, most ethanolic extracts proved effective against the A. hydrophila tested, with 10-12 mm inhibition zones observed. A. hydrophila demonstrated the highest susceptibility to F. pumila. Among various species of Ficus with moderate activity against A. hydrophila, the highest antibacterial activities were noted for F. benghalensis, F. benjamina, F. deltoidea, F. hispida, and F. lyrata. Thus, Ficus can be used as a natural antiseptic and antimicrobial agent in veterinary practice. Further investigations need to be conducted to isolate and identify the bioactive compounds that can then be subjected to detailed pharmacological studies and the development of clinical applications. The alarming rate of increasing resistance in bacterial pathogens in aquaculture environments means that medicinal plants with antibacterial properties are very important as natural resources of new active compounds.


2017 ◽  
Vol 11 (1) ◽  
pp. 38-53 ◽  
Author(s):  
Ola H. Rizk ◽  
Omaima G. Shaaban ◽  
Abeer E. Abdel Wahab

Introduction: Three series of pyrazole, thiazole and 1,3,4-oxadiazole, derivatives were synthesized starting from 5-amino-4-(hydrazinocarbonyl)-3-methylthiophene-2-carboxamide (2). Methods: All compounds were investigated for their preliminary antimicrobial activity. They were proved to exhibit remarkable antimicrobial activity against Pseudomonas aeruginosa with insignificant activity towards Gram positive bacterial strains and fungi. Results: In-vitro testing of the new compounds on hepatitis-C virus (HCV) replication in hepatocellular carcinoma cell line HepG2 infected with the virus utilizing the reverse transcription polymerase chain reaction technique (RT-PCR) generally showed inhibition of the replication of HCV RNA (–) strands at low concentration, while, eight compounds; 3a, 6, 7a, 7b, 9a, 9b, 10a and 11b proved to inhibit the replication of HCV RNA (+) and (–) strands at very low concentration range 0.08-0.36 μg/mL. Conclusion: Compounds 7b and 11b displayed the highest anti-HCV and antimicrobial activities in this study.


1965 ◽  
Vol 11 (4) ◽  
pp. 637-640
Author(s):  
Alfred A. Richtarik ◽  
Klaus Lindemulder ◽  
B. De Boer

The in vitro antimicrobial activity of selected pharmacological agents was studied against five strains of staphylococci (phage types 7 US, 54, 71, 80, 81). At the concentrations used (maximal 0.125 μg/ml) chlorothiazide, acetazolamide, FeCl3, SnCl2, stilbamine urea, quinacrine, antimony Na thioglycollate, antimony thioglycollamide, and sulfisoxazole were found to have no antimicrobial effect against these strains of staphylococci, whereas HgCl2, AgNO3, meralluride sodium, stilbamidine, pentamidine, and propamidine did show activity. When effective agents were combined with potassium phenoxymethyl penicillin, the bacteriostatic action of the antibiotic was inhibited in some cases and markedly potentiated in others. Consideration should be given to the possible incorporation of effective agents into the structure of synthetic antibiotics as a means of combating resistant staphylococci.


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