Preparation of New Oxadiazole Acyclic Nucleoside and Thioglycoside Analogs Containing Chromene Moiety with Antimicrobial Evaluation

2017 ◽  
Vol 68 (10) ◽  
pp. 2228-2233
Author(s):  
Mshari A. Alotaibi ◽  
Farag A. El Essawy ◽  
Nader M. Boshta

New sugar hydrazones linked to chroman ring system and their derived oxadiazole acyclic nucleoside analogs were synthesized from the substituted ethyl ester oxime derivative. The 2-sustituted 1,3,4-oxadiazole-5-thione prepared from acid hydrazide was glycosylated to afford the corresponding thioglycosides, not the N-linked glycosides. The novel compounds were evaluated for their antimicrobial activity and showed different degrees of activities.

2012 ◽  
Vol 49 (3) ◽  
pp. 607-612 ◽  
Author(s):  
Wael A. El-Sayed ◽  
Omar M. Ali ◽  
Merfat S. Faheem ◽  
Ibrahim F. Zied ◽  
Adel A.-H. Abdel-Rahman

2012 ◽  
Vol 48 (7) ◽  
pp. 1043-1049 ◽  
Author(s):  
O. M. Ali ◽  
H. H. Amer ◽  
A. A. Mosaad ◽  
A. A.-H. Abdel-Rahman

2012 ◽  
Vol 49 (5) ◽  
pp. 1026-1032 ◽  
Author(s):  
Omar M. Ali ◽  
Wael A. El-Sayed ◽  
Heba A. El-Sayed ◽  
Adel A.-H. Abdel-Rahman

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.


Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3268
Author(s):  
Katja S. Håheim ◽  
Emil Lindbäck ◽  
Kah Ni Tan ◽  
Marte Albrigtsen ◽  
Ida T. Urdal Helgeland ◽  
...  

A series of novel quinoline-based tetracyclic ring-systems were synthesized and evaluated in vitro for their antiplasmodial, antiproliferative and antimicrobial activities. The novel hydroiodide salts 10 and 21 showed the most promising antiplasmodial inhibition, with compound 10 displaying higher selectivity than the employed standards. The antiproliferative assay revealed novel pyridophenanthridine 4b to be significantly more active against human prostate cancer (IC50 = 24 nM) than Puromycin (IC50 = 270 nM) and Doxorubicin (IC50 = 830 nM), which are used for clinical treatment. Pyridocarbazoles 9 was also moderately effective against all the employed cancer cell lines and moreover showed excellent biofilm inhibition (9a: MBIC = 100 µM; 9b: MBIC = 100 µM).


2006 ◽  
Vol 63 (3) ◽  
pp. 316-322 ◽  
Author(s):  
C. Kratzer ◽  
S. Tobudic ◽  
W. Graninger ◽  
A. Buxbaum ◽  
A. Georgopoulos

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