Publications by authors named "Yousef Valizadeh"

4 Publications

  • Page 1 of 1

Novel Coumarin Containing Dithiocarbamate Derivatives as Potent α-Glucosidase Inhibitors for Management of Type 2 Diabetes.

Med Chem 2021 ;17(3):264-272

Nano Alvand Company, Avicenna Tech Park, Tehran University of Medical Sciences, Tehran, Iran.

Background: α-Glucosidase is a hydrolyzing enzyme that plays a crucial role in the degradation of carbohydrates and starch to glucose. Hence, α-glucosidase is an important target in carbohydrate mediated diseases such as diabetes mellitus.

Objective: In this study, novel coumarin containing dithiocarbamate derivatives 4a-n were synthesized and evaluated against α-glucosidase in vitro and in silico.

Methods: These compounds were obtained from the reaction between 4-(bromomethyl)-7- methoxy-2H-chromen-2-one 1, carbon disulfide 2, and primary or secondary amines 3a-n in the presence of potassium hydroxide and ethanol at room temperature. In vitro α-glucosidase inhibition and kinetic study of these compounds were performed. Furthermore, a docking study of the most potent compounds was also performed by Auto Dock Tools (version 1.5.6).

Results: Obtained results showed that all the synthesized compounds exhibited prominent inhibitory activities (IC50 = 85.0 ± 4.0-566.6 ± 8.6 μM) in comparison to acarbose as a standard inhibitor (IC50 = 750.0 ± 9.0 μM). Among them, the secondary amine derivative 4d with pendant indole group was the most potent inhibitor. Enzyme kinetic study of the compound 4d revealed that this compound competes with a substrate to connect to the active site of α-glucosidase and therefore is a competitive inhibitor. Moreover, a molecular docking study predicted that this compound interacted with the α-glucosidase active site pocket.

Conclusion: Our results suggest that the coumarin-dithiocarbamate scaffold can be a promising lead structure for designing potent α-glucosidase inhibitors for the treatment of type 2 diabetes.
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http://dx.doi.org/10.2174/1573406416666200826101205DOI Listing
January 2021

Novel N,N-dimethylbarbituric-pyridinium derivatives as potent urease inhibitors: Synthesis, in vitro, and in silico studies.

Bioorg Chem 2020 01 20;95:103529. Epub 2019 Dec 20.

Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran. Electronic address:

A new series of N,N-dimethylbarbituric-pyridinium derivatives 7a-n was synthesized and evaluated as Helicobacter pylori urease inhibitors. All the synthesized compounds (IC = 10.37 ± 1.0-77.52 ± 2.7 μM) were more potent than standard inhibitor hydroxyurea against urease (IC = 100.00 ± 0.2 μM). Furthermore, comparison of IC values of the synthesized compounds with the second standard inhibitor thiourea (IC = 22.0 ± 0.03 µM) revealed that compounds 7a-b and 7f-h were more potent than thiourea. Molecular modeling study of the most potent compounds 7a, 7b, 7f, and 7g was also conducted. Additionally, the drug-likeness properties of the synthesized compounds, based on Lipinski rule and other filters, were evaluated.
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http://dx.doi.org/10.1016/j.bioorg.2019.103529DOI Listing
January 2020

Effects of Guajol ointment synthesized from medicinal smoke condensate of jennet feces on burn wound healing on Wistar rat.

Vet Res Forum 2017 15;8(3):215-221. Epub 2017 Sep 15.

Young Researchers and Elites Club, Shahrekord Branch, Islamic Azad University, Shahrekord, Iran.

Application of smoke condensate derived from an indirect heating of jennet feces (Sargin) had been recommended by Iranian ancient scientists as a therapeutic agent. The present study was done to evaluate the healing effects of Guajol ointment on burn wound in rat. The Guajol ointment was prepared from the smoke condensate of Sargin samples. Wistar Rats (n = 50) were randomized into six groups including normal saline, silver sulfadiazine and 1.25%, 2.50%, 5.00% and 10.00% concentrations of Guajol ointment. Under general anesthesia, dorsum of the rats were shaved and burn wounds were created using hot plate. Area of wounds and percent of healing were measured. Normal saline had the highest area of wound, followed by 1.25% Guajol and silver-sulfadiazine groups. The group treated with 5.00% Guajol showed the highest percent of healing. Percent of healing in NS, SSD and 5.00% Guajol ointment groups on day 21 were 38.47%, 75.00% and 98.51%, respectively. Microscopic examination of wounds sections of rats treated with 5.00% Guajol showed more collagen fibers and fibroblasts cells on day 7. Wounds of 5.00% Guajol treated group was covered with healthy epithelial and epidermis tissues and hair follicles on day 21. This was the first report of using Sargin to heal the burn wound of rat. Further studies are recommended for investigation of the other effects of Guajol ointment and its possible application in medicine.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5653885PMC
September 2017

Virulence factors, serogroups and antimicrobial resistance properties of Escherichia coli strains in fermented dairy products.

BMC Res Notes 2014 Apr 7;7:217. Epub 2014 Apr 7.

Young Researchers Club and Elite, ShahreKord Branch, Islamic Azad University, P,O, Box 166, ShahreKord, Iran.

Background: From a clinical perspective, it is essential to know the microbial safety of fermented dairy products. Doogh and kashk are fermented dairies. These products are used by millions of people but their microbial qualities are unknown. Shiga toxin producing Escherichia coli (STEC) is one of the most commonly detected pathogens in the cases of food poisoning and food-borne illnesses. The present investigation was carried out in order to study the molecular characterization and antimicrobial resistance properties of STEC strains isolated from fermented dairy products.

Methods: Six hundred fermented dairy samples were collected and immediately transferred to the laboratory. All samples were cultured immediately and those that were E. coli-positive were analyzed for the presence of O157 , O26, O103, O111, O145, O45, O91, O113, O121 and O128 STEC serogroups, tetA, tetB, blaSHV, CITM, cmlA, cat1, aadA1, dfrA1, qnr, aac (3)-IV, sul1 and ereA antibiotic resistance genes and stx1, stx2, eaeA, ehly, cnf1, cnf2, iutA, cdtB, papA, traT, sfaS and fyuA virulence factors using PCR. Antimicrobial susceptibility testing was performed also using disk diffusion methodology with Mueller-Hinton agar.

Results: Fifty out of 600 (8.33%) dairy samples harbored E. coli. In addition, yoghurt was the most commonly contaminated dairy. O157 (26%) and O26 (12%) were the most commonly detected serogroups. A significant difference was found between the frequency of Attaching and Effacing E. coli and Enterohaemorrhagic E. coli (P <0.05). Stx1 (44%), eae (36%), papA (32%) stx2 (30%), and ehly (28%) were the most commonly detected virulence factors. The genes encode resistance against tetracycline (tetA and tetB) (76% and 70%, respectively), cephalothin (blaSHV) (38%), ampicillin (CITM) (36%) and gentamicin (aac (3)-IV) (32%) were the most commonly detected. High resistance levels to tetracycline (84%), penicillin (46%), ampicillin (38%) and streptomycin (36%) were observed.

Conclusion: Fermented dairy products can easily become contaminated by antibiotic resistant STEC strains. Our findings should raise awareness about antibiotic resistance in Iran. Clinicians should exercise caution when prescribing antibiotics, especially in veterinary treatments.
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http://dx.doi.org/10.1186/1756-0500-7-217DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3983858PMC
April 2014