- Synthesis and in vitro urease inhibitory activity of 5-nitrofuran-2-yl-thiadiazole linked to different cyclohexyl-2-(phenylamino)acetamides, in silico and kinetic studies
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A series of 5-nitrofuran-2-yl-thiadiazole linked to different cyclohexyl-2-(phenylamino)acetamides were rationally designed and synthesized. All synthetic compounds were evaluated for their urease inhibitory activity and exhibited good inhibitory potential against urease with IC50 values in the range of 0.94 – 6.78 μM as compared to the standard thiourea (IC50 = 22.50 μM). Compound 8g (IC50 = 0.94 μM) with a thiophene substituent at the R2 position was found to be the most active member of the series. Kinetic studies exhibited that the compound 8g was a non-competitive inhibitor. In silico study showed the critical interactions of potent inhibitors with the active site of the enzyme. These newly identified inhibitors of the urease enzyme can serve as leads for further research and development.
- Amanlou, Massoud,Ansari, Shirin,Asadi, Mehdi,Azizian, Homa,Biglar, Mahmood,Dianatpour, Mehdi,Foroumadi, Alireza,Iraji, Aida,Larijani, Bagher,Mahdavi, Mohammad,Mohammadi Khanaposhtani, Maryam,Nazari Montazer, Mohammad,Sherafati, Maede,Tanideh, Nader
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- Synthesis and anti-Helicobacter pylori activity of 5-(nitroaryl)-1,3,4-thiadiazoles with certain sulfur containing alkyl side chain
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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.
- Foroumadi, Alireza,Rineh, Ardeshir,Emami, Saeed,Siavoshi, Farideh,Massarrat, Sadegh,Safari, Fatemeh,Rajabalian, Saeed,Falahati, Mehraban,Lotfali, Ensieh,Shafiee, Abbas
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scheme or table
p. 3315 - 3320
(2009/04/11)
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- Synthesis and antimycobacterial activity of some alkyl [5-(nitroaryl)-1,3, 4-thiadiazol-2-ylthio]propionates
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Two series of 2- and 3-[5-(nitroaryl)-1,3,4-thiadiazol-2-ylthio, sulfinyl and sulfonyl] propionic acid alkyl esters were synthesized and screened for antituberculosis activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system. The MIC values for the compounds showing more than 90% inhibition were determined. The result of comparison between two groups of data exhibited that among the synthesized derivatives, the compound propyl 3-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-ylthio]propionate was the most active one (MIC = 1.56 μg ml-1).
- Foroumadi, Alireza,Kargar, Zahra,Sakhteman, Amirhossein,Sharifzadeh, Zahra,Feyzmohammadi, Robabeh,Kazemi, Mahnoush,Shafiee, Abbas
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p. 1164 - 1167
(2007/10/03)
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- Antituberculosis agents, I: Synthesis and antituberculosis activity of 2-aryl-1,3,4-thiadiazole derivatives
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The design, synthesis and antituberculosis activity of a series of 2-aryl-5-methylthio-1,3,4-thiadiazoles (5a-b), ethyl α-(5aryl)-1,3,4-thiadiazole-2-ylthio)acetates (8a-b) and related compounds are described. All of the compounds were tested against Mycobacterium tuberculosis strain H37Rv in comparison to rifampicin. Six compounds exhibited a very good activity (MIC 6.k25 μ/ml, % Inhibition = 100).
- Foroumadi,Mirzaei,Shafiee
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p. 610 - 612
(2007/10/03)
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- Synthesis and antifungal activity of 2-aryl-1,3,4-thiadiazole-5-sulphides, sulphoxides and sulphones
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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.
- Foroumadi,Daneshtalab,Mahmoudian,Falahati,Nateghian,Shahsavarani,Shafiee
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