Journals / Hittite Journal of Science and Engineering / 2023 / Cilt: 10 Sayı: 2

Novel 1,3,4-Thiadiazole Derivatives as Antibiofilm, Antimicrobial, Efflux Pump Inhibiting Agents and Their ADMET Characterizations

Pages
99–116
Publication Date
2023-06-30
DOI
—
🏛️Bibliographic metadata and full text access for this article are provided via DergiPark.
DergiPark Record ↗
✨

AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

Finally, the electrochemical stabilities of the synthesized molecules have been analyzed by using cyclic voltammetry in 0.1 M TBAPF6 in DMSO as a supporting electrolyte.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:In this study, 1,3,4-thiadiazole derivatives were obtained from the reaction of benzophenone-4,4'-dicarboxylic acid and N-substitute-thiosemicarbazide compounds with each other.
📊
Key Findings & Data:According to the MBC/MFC test, all the activities were found to be bacteriostatic, also, especially the biofilm inhibition activity of C1 against K. pneumoniae is noteworthy.
💡
Conclusion & Impact:Finally, the electrochemical stabilities of the synthesized molecules have been analyzed by using cyclic voltammetry in 0.1 M TBAPF6 in DMSO as a supporting electrolyte.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Efflux pump inhibition · antibiofilm · antibacterial

Abstract

In this study, 1,3,4-thiadiazole derivatives were obtained from the reaction of benzophenone-4,4'-dicarboxylic acid and N-substitute-thiosemicarbazide compounds with each other. After the synthesis of the final products, some biological properties of these compounds such as antibiofilm, antimicrobial and efflux pump inhibiting efficiencies were evaluated. According to the MBC/MFC test, all the activities were found to be bacteriostatic, also, especially the biofilm inhibition activity of C1 against K. pneumoniae is noteworthy. In addition, C4 was observed to exhibit efflux pump inhibition activity in E. coli, whereas C2 and C3 in K. pneumoniae. The absorption and emission values of the molecules were obtained and electrochemical studies were performed. In addition; absorption, metabolism, distribution, excretion and toxicity (ADMET) scores were predicted using the pharmacokinetic properties of all 1,3,4-thiadiazole compounds. Finally, the electrochemical stabilities of the synthesized molecules have been analyzed by using cyclic voltammetry in 0.1 M TBAPF6 in DMSO as a supporting electrolyte.

🔖

Cite This Article

GÜR, M., ZURNACI, M., ALTINÖZ, E., ŞENER, N., ŞAHİN, Ç., ŞENTURAN, M., ŞENER, İ., ÇAVUŞ, M., ALTUNER, E. M. (2023). Novel 1,3,4-Thiadiazole Derivatives as Antibiofilm, Antimicrobial, Efflux Pump Inhibiting Agents and Their ADMET Characterizations. Hittite Journal of Science and Engineering, Cilt: 10 Sayı: 2, 99–116. https://ajindex.com/articles/949692

📄 Full Text PDF Viewer

📄

PDF görüntüleyici hazırlanıyor...

References (12)

  1. S. Janowska, A. Paneth, M. Wujec, Cytotoxic Properties of 1,3,4-Thiadiazole Derivatives—A Review, Molecules. 25 (2020) 4309
  2. R. Ningegowda, N.S. Shivananju, P. Rajendran, Basappa, K.S. Rangappa, A. Chinnathambi, F. Li, R.R. Achar, M.K. Shanmugam, P. Bist, S.A. Alharbi, L.H.K. Lim, G. Sethi, B.S. Priya, A novel 4,6-disubstituted-1,2,4-triazolo-1,3,4-thiadiazole derivative inhibits tumor cell invasion and potentiates the apoptotic effect of TNFα by abrogating NF-κB activation cascade, Apoptosis. 22 (2017) 145–157
  3. G. Lalita, Chauhan; Shalini, Journal of drug delivery and therapeutics (jddt), Journal of Drug Delivery & Therapeutics. 9 (2020) 661–668
  4. D. Disposition, Op Y Ig Ht S Ht S, 46 (2015) 750–756
  5. P.A. Datar, Design and Synthesis of Thiadiazole Derivatives as Antidiabetic Agents, Medicinal Chemistry. 4 (2014)
  6. S. Thrilochana, P., Sahu, C. N., Hazra, K., and Ramachandran, Synthesis and Biological Evaluation of New Thiadiazole Analogs for Anti-diabetic Activity against Alloxan-Induced Diabetes, J. Pharm. Res. 8 (2014) 1–8
  7. A. Cristina, D. Leonte, L. Vlase, L. Bencze, S. Imre, G. Marc, B. Apan, C. Mogoșan, V. Zaharia, Heterocycles 48. Synthesis, Characterization and Biological Evaluation of Imidazo[2,1-b][1,3,4]Thiadiazole Derivatives as Anti-Inflammatory Agents, Molecules. 23 (2018) 2425
  8. S. Schenone, C. Brullo, O. Bruno, F. Bondavalli, A. Ranise, W. Filippelli, B. Rinaldi, A. Capuano, G. Falcone, New 1,3,4-thiadiazole derivatives endowed with analgesic and anti-inflammatory activities, Bioorganic & Medicinal Chemistry. 14 (2006) 1698–1705.
  9. Ö.D. Can, M.D. Altıntop, Ü.D. Özkay, U.İ. Üçel, B. Doğruer, Z.A. Kaplancıklı, Synthesis of thiadiazole derivatives bearing hydrazone moieties and evaluation of their pharmacological effects on anxiety, depression, and nociception parameters in mice, Archives of Pharmacal Research. 35 (2012) 659–669
  10. A.B. Samel, N.R. Pai, Synthesis of Novel Aryloxy Propanoyl Thiadiazoles as Potential Antihypertensive Agents, Journal of the Chinese Chemical Society. 57 (2010) 1327–1330
  11. G. Serban, Synthetic Compounds with 2-Amino-1,3,4-Thiadiazole Moiety Against Viral Infections, Molecules. 25 (2020) 942
  12. Brai, Ronzini, Riva, Botta, Zamperini, Borgini, Trivisani, Garbelli, Pennisi, Boccuto, Saladini, Zazzi, Maga, Botta, Synthesis and Antiviral Activity of Novel 1,3,4-Thiadiazole Inhibitors of DDX3X, Molecules. 24 (2019) 3988. 13. and F.B. Azar Tahghighi, T