ChemInform Abstract: Synthesis, Biological Activities and Chemistry of Thiadiazole Derivatives and Schiff Bases

ChemInform ◽  
2013 ◽  
Vol 44 (16) ◽  
pp. no-no
Author(s):  
Sunny Jalhan ◽  
Anil Jindal ◽  
Avneet Gupta ◽  
Hemraj Hemraj
2020 ◽  
Vol 26 (1) ◽  
pp. 6-13 ◽  
Author(s):  
Ulviye Acar Çevik ◽  
Derya Osmaniye ◽  
Serkan Levent ◽  
Begüm Nurpelin Sağlik ◽  
Betül Kaya Çavuşoğlu ◽  
...  

AbstractCancer is one of the most common causes of death in the world. Despite the importance of combating cancer in healthcare systems and research centers, toxicity in normal tissues and the low efficiency of anticancer drugs are major problems in chemotherapy. Nowadays the aim of many medical research projects is to discover new safer and more effective anticancer agents. 1,3,4-Thiadiazole compounds are important fragments in medicinal chemistry because of their wide range of biological activities, including anticancer activities. The aim of this study was to determine the capacity of newly synthesized 1,3,4-thiadiazole compounds as chemotherapeutic agents. The structures of the obtained compounds were elucidated using 1H-NMR, 13C-NMR and mass spectrometry. Although the thiadiazole derivatives did not prove to be significantly cytotoxic to the tumour tissue cultures, compound 4i showed activity against the C6 rat brain cancer cell line (IC50 0.097 mM) at the tested concentrations.


2021 ◽  
Vol 17 ◽  
Author(s):  
Em Canh Pham ◽  
Tuyen Ngoc Truong ◽  
Nguyen Hanh Dong ◽  
Duy Duc Vo ◽  
Tuoi Thi Hong Do

Background: Many compounds containing a five-membered heterocyclic ring display exceptional chemical properties and versatile biological activities. Objective: The objective of the present study was the desire to prepare the 5-substituted 2-amino-1,3,4-oxadiazole and 2-amino-1,3,4-thiadiazole derivatives and evaluate their potential anticancer, antibacterial and antifungal activities. Methods: Twenty-seven derivatives were synthesized by iodine-mediated cyclization of semicarbazones or thiosemicarbazones obtained from condensation of semicarbazide or thiosemicarbazide and aldehydes. The structures were confirmed by 1H-NMR, 13C-NMR and MS spectra. The antibacterial and antifungal activities were evaluated by diffusion method and the anticancer activities were evaluated by MTT assay. Results: Twenty-seven derivatives have been synthesized in moderate to good yields. A number of derivatives exhibited potential antibacterial, antifungal and anticancer activities. Conclusion: Compounds (1b, 1e and 1g) showed antibacterial activity against Streptococcus faecalis, MSSA and MRSA with MIC ranging between 4 to 64 µg/mL. Compound (2g) showed antifungal activity against Candida albicans (8 µg/mL) and Aspergillus niger (64 µg/mL). Compound (1o) exhibited high cytotoxic activity against HepG2 cell line (IC50 value 8.6 µM), which is comparable to the activity of paclitaxel, and is non-toxic on LLC-PK1 normal cell line. The structure activity relationship and molecular docking study of the synthesized compounds are also reported.


Author(s):  
Ebuka Leonard Onyeyilim ◽  
Mercy Amarachi Ezeokonkwo ◽  
David Izuchukwu Ugwu ◽  
Chiamaka Peace Uzoewulu ◽  
Florence Uchenna Eze ◽  
...  

: Carbohydrazides and their Schiff bases are important class of heterocycles that are not only employed in the area of organic chemistry, but also have tremendous applications in physical and inorganic chemistry. A series of potential bioactive compounds, containing carbohydrazide functionality and their hydrazone derivatives have been synthesized and screened for antibacterial, anticancer, antifungal and anti-inflammatory etc. This brief review discloses some synthetic route to so many reported carbohydrazides, their Schiff bases, their biological activities and their structure activity relationship.


2016 ◽  
Vol 20 ◽  
pp. S463-S475 ◽  
Author(s):  
Bhoomendra A. Bhongade ◽  
Sirajunisa Talath ◽  
Ravikiran A. Gadad ◽  
Andanappa K. Gadad

2021 ◽  
Vol 0 (0) ◽  
pp. 0-0
Author(s):  
Shorouk Mukhtar ◽  
Ashraf Hassan ◽  
Nesrin Morsy ◽  
Taghrid Hafez ◽  
Hamdi Hassaneen ◽  
...  

1968 ◽  
Vol 88 (11) ◽  
pp. 1437-1449 ◽  
Author(s):  
TERUHISA NOGUCHI ◽  
YOSHINOBU HASHIMOTO ◽  
TOSHIRO MORI ◽  
SABURO KANO ◽  
KOOSHIN MIYAZAKI

2018 ◽  
Vol 42 (11) ◽  
pp. 8851-8863 ◽  
Author(s):  
Alexander Carreño ◽  
César Zúñiga ◽  
Dayán Páez-Hernández ◽  
Manuel Gacitúa ◽  
Rubén Polanco ◽  
...  

Schiff bases exhibit a broad range of applications, including their use as catalysts, stabilizers, dyes, and intermediates in organic synthesis; and biological activities, such as antifungal properties.


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