88541-06-4Relevant academic research and scientific papers
Synthesis and anti-Helicobacter pylori activity of 5-(nitroaryl)-1,3,4-thiadiazoles with certain sulfur containing alkyl side chain
Foroumadi, Alireza,Rineh, Ardeshir,Emami, Saeed,Siavoshi, Farideh,Massarrat, Sadegh,Safari, Fatemeh,Rajabalian, Saeed,Falahati, Mehraban,Lotfali, Ensieh,Shafiee, Abbas
scheme or table, p. 3315 - 3320 (2009/04/11)
A series of 5-(nitroaryl)-1,3,4-thiadiazoles bearing certain sulfur containing alkyl side chain similar to pendent residue in tinidazole molecule were synthesized and evaluated against Helicobacter pylori using disk diffusion method. The synthesized compounds were also evaluated for their antibacterial, antifungal and cytotoxic effects. Study of the structure-activity relationships of this series of compounds indicated that both the structure of the nitroaryl unit and the pendent group on 2-position of 1,3,4-thiadiazole ring dramatically impact the anti-H. pylori activity. While compound 7a containing 2-[2-(ethylsulfonyl)ethylthio]-side chain from nitrothiophene series was the most potent compound tested against clinical isolates of H. pylori, however, nitroimidazoles 6c and 7c were found to be more promising compounds because of their respectable anti-H. pylori activity besides less cytotoxic effects.
Synthesis and in vitro antibacterial activity of some N-(5-aryl-1,3,4-thiadiazole-2-yl)piperazinyl quinolone derivatives
Foroumadi, Alireza,Soltani, Fatemeh,Moshafi, Mohammad Hasan,Ashraf-Askari, Rogheeyeh
, p. 1023 - 1028 (2007/10/03)
A series of N-[5-(1-methyl-5-nitro-2-imidazolyl)-1,3,4-thiadiazole-2-yl] and N-[5-(nitrophenyl)-1,3,4-thiadiazole-2-yl] piperazinyl quinolone derivatives (5a-c and 5d-l) were synthesized and evaluated for in vitro antibacterial activity against some Gram-positive and Gram-negative bacteria. The antibacterial data revealed that all nitroimidazole derivatives (5a-c) showed interesting activity against tested Gram-positive bacteria (minimum inhibitory concentration, MIC=0.008-0.03 μg/ml) while they did not show good activity against Gram-negative organisms. Despite the significant activity of nitroimidazole series, all nitrophenyl analogues (5d-l) were inactive against both Gram-positive and Gram-negative bacteria. Among all of the tested compounds, 5a (ciprofloxacin derivative in nitroimidazole series) exhibited excellent activity against Staphylococcus aureus and Staphylococcus epidermidis (MIC=0.008 μg/ml).
Synthesis and in vitro antifungal activity of 2-aryl-5-phenylsulfonyl- 1,3,4-thiadiazole derivatives
Foroumadi, Alireza,Daneshtalab, Mohsen,Shafiee, Abbas
, p. 1035 - 1038 (2007/10/03)
The synthesis and antifungal activity of a series of 2-nitroaryl-5- phenylsulfonyl-1,3,4-thiadiazoles (5a-e) are described. The in vitro antifungal activity of the compounds was determined against a variety of fungal strains in comparison to miconazole (CAS 22916-47-8) and fluconazole (CAS 86386-73-4). Two derivatives (5d, 5e) showed high activity against Candida albicans and Candida spp. having MIC values ranging from 0.048-3.12 μg/ml, providing higher potencies than the reference drug fluconazole. Compound 5a also showed high activity against Cryptococcus neoformans (MIC 0.048 μg/ml). The activity of this compound against Aspergillus niger and Aspergillus fumigatus was moderate (MIC = 1.56-6.25 μg/ml), while fluconazole was inactive. Moreover, the nitroimidazole derivative 5d possessed good activity against most fungal strains in comparison to fluconazole.
Synthesis and antifungal activity of 2-aryl-1,3,4-thiadiazole-5-sulphides, sulphoxides and sulphones
Foroumadi,Daneshtalab,Mahmoudian,Falahati,Nateghian,Shahsavarani,Shafiee
, p. 95 - 98 (2007/10/03)
2-Aryl-1,3,4-thiadiazole-5-sulphides, sulphoxides and sulphones were synthesized and tested against a variety of fungal strains, Miconazole and fluconazole were used as reference drugs. The most active compounds against Candida albicans, Candida spp., Cryptococcus neoformans and Aspergillus niger were 2-(1-methyl-5-nitro-2-imidazolyl)-5-methylsulphonyl-1 ,3,4-thiadiazole (8h) and 2-(5-nitro-2-furyl)-5-methylsulphonyl-1,3,4-thiadiazole (8f). Our results showed that compounds 8h and 8f were several times more active than fluconazole in most fungal strains.
SYNTHESIS AND MASS-SPECTROMETRIC STUDY OF 2-AMINO- AND 2-CHLORO-5-ARYL-1,3,4-THIADIAZOLES
Zubets, I. V.,Boikov, Yu. A.,Viktorovskii, I. V.,V'yunov, K. A.
, p. 1148 - 1152 (2007/10/02)
The cyclization of aldehyde thiosemicarbazones with ferric chloride yielded 2-amino-5-aryl-1,3,4-thiadiazoles, forming 2-chloro-5-aryl-1,3,4-thiadiazoles in the Sandmeyer reaction.The mass-spectrometric behavior of the 2-amino- and 2-chloro-5-aryl-1,3,4-t
Guanidino-heterocyclyl-phenyl-amidines and salts thereof
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, (2008/06/13)
Compounds of the tautomeric formula STR1 wherein R, R1 and R2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms; R3 is straight or branched alkyl, optionally interru
