Fariba Peytam

Tehran University of Medical Sciences

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Mehdi Adib

University of Tehran

Loghman Firoozpour

Tehran University of Medical Sciences

Alireza Foroumadi

Tehran University of Medical Sciences

Mohammad Ali Faramarzi

Biotechnology Research Center

Hamid Reza Bijanzadeh

Tarbiat Modares University

Zahra Emamgholipour

Tehran University of Medical Sciences

Mehdi Jahani

Sharif University of Technology

Mahmoud Rahmanian-Jazi

Tehran University of Medical Sciences

Mohammad Mahdavi

Tehran University of Medical Sciences

Bagher Larijani

Tehran University of Medical Sciences

Cooperative Institutions

Tehran University of Medical Sciences

University of Tehran

Kerman University of Medical Sciences

Biotechnology Research Center

Palacký University Olomouc

Shiraz University of Medical Sciences

Chemistry and Chemical Engineering Research Center of Iran

Mazandaran University of Medical Sciences

Iran University of Medical Sciences

Czech Academy of Sciences, Institute of Experimental Botany

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A new synthetic strategy towards 2,4,5-trisubstituted 1H-imidazoles and highly substituted pyrrolo[1,2-c]imidazoles by use of α-azidochalcones via Michael addition-cyclization followed by Wittig reaction

Tetrahedron (2017)

Mehdi Adib Fariba Peytam Mahmoud Rahmanian-Jazi Hamid Reza Bijanzadeh Massoud Amanlou

Wittig reaction

Dichloromethane

Imidazole

Michael reaction

Guanidine

10.1016/j.tet.2017.09.042

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Citations (16)

The possible effect of microRNA-155 (miR-155) and BACE1 inhibitors in the memory of patients with down syndrome and Alzheimer's disease: Design, synthesis, virtual screening, molecular modeling and biological evaluations

Journal of Biomolecular Structure and Dynamics (2021)

Shabnam Mahernia Malihe Hassanzadeh Mehdi Adib Fariba Peytam Zahra Haghighijoo

MiR-155 plays main roles in several physiological and pathological mechanisms, such as Down syndrome (DS), immunity and inflammation and potential anti-AD therapeutic target. The miR-155 is one of the overexpressed miRNAs in DS patients that contribute directly and indirectly to the onset or progression of the DS. Since the miR-155 can simultaneously reduce the translation of several genes at post-transcriptional levels, targeting the miR-155 might set the stage for the treatment of DS. One of the rational strategies in providing therapeutic interventions in this respect is to design and develop novel small molecules inhibiting the miR-155 function or biogenesis or maturation. In the present study, we aim to introduce small molecule compounds with the potential to inhibit the generation of the selectively miR-155 processing by employing computational drug design approaches, as well as in vitro studies. We designed and synthesized a novel series of imidazo[1,2-a]pyridines derivatives as new nonpeptic candidates for the treatment of DS with AD. The designed compounds were investigated for their BACE1 and miR-155 binder inhibitory potential in vitro and in cell. In addition, we present a systematic computational approach that includes 3 D modeling, docking-based virtual screening, and molecular dynamics simulation to identify Small - molecule inhibitors of pre-miR-155 maturation. To confirm the inhibitory potential of compound 8k on miR-155 maturation, qRT- PCR was performed. All our results confirm that compound 8k, in addition to being a good inhibitor of BACE1, can also be a good inhibitor of miR-155.Communicated by Ramaswamy H. Sarma

miR-155

Rational design

10.1080/07391102.2021.1873861

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Citations (11)

An efficient and targeted synthetic approach towards new highly substituted 6-amino-pyrazolo[1,5-a]pyrimidines with α-glucosidase inhibitory activity

Scientific Reports (2020)

Fariba Peytam Mehdi Adib Reihaneh Shourgeshty Loghman Firoozpour Mahmoud Rahmanian-Jazi

Abstract In an attempt to find novel α -glucosidase inhibitors, an efficient, straightforward reaction to synthesize a library of fully substituted 6-amino-pyrazolo[1,5- a ]pyrimidines 3 has been investigated. Heating a mixture of α-azidochalcones 1 and 3-aminopyrazoles 2 under the mild condition afforded desired compounds with a large substrate scope in good to excellent yields. All obtained products were evaluated as α -glucosidase inhibitors and exhibited excellent potency with IC 50 values ranging from 15.2 ± 0.4 µM to 201.3 ± 4.2 µM. Among them, compound 3d was around 50-fold more potent than acarbose (IC 50 = 750.0 ± 1.5 µM) as standard inhibitor. Regarding product structures, kinetic study and molecular docking were carried out for two of the most potent ones.

Acarbose

Docking (animal)

10.1038/s41598-020-59079-z

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Citations (33)

Imidazopyridine-based kinase inhibitors as potential anticancer agents: A review

Bioorganic Chemistry (2023)

Fariba Peytam Zahra Emamgholipour Ali Mousavi Mahfam Moradi Roham Foroumadi

Imidazopyridine

Kinome

10.1016/j.bioorg.2023.106831

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Citations (12)

A one-pot, three-component and solvent-free synthesis of 2,3-disubstituted isoindolin-1-ones

Tetrahedron Letters (2015)

Mehdi Adib Fariba Peytam Mohsen Zainali Long‐Guan Zhu Jing Wu

Benzylamine

Dimedone

Component (thermodynamics)

Meldrum's acid

10.1016/j.tetlet.2015.06.020

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Citations (19)

Imidazo[1,2-c]quinazolines as a novel and potent scaffold of α-glucosidase inhibitors: design, synthesis, biological evaluations, and in silico studies

Scientific Reports (2023)

Fariba Peytam Faezeh Sadat Hosseini Malak Hekmati Bahareh Bayati Mahdis Sadeghi Moghadam

α-Glucosidase inhibition is an approved treatment for type 2 diabetes mellitus (T2DM). In an attempt to develop novel anti-α-glucosidase agents, two series of substituted imidazo[1,2-c]quinazolines, namely 6a-c and 11a-o, were synthesized using a simple, straightforward synthetic routes. These compounds were thoroughly characterized by IR, 1H and 13C NMR spectroscopy, as well as mass spectrometry and elemental analysis. Subsequently, the inhibitory activities of these compounds were evaluated against Saccharomyces cerevisiae α-glucosidase. In present study, acarbose was utilized as a positive control. These imidazoquinazolines exhibited excellent to great inhibitory potencies with IC50 values ranging from 12.44 ± 0.38 μM to 308.33 ± 0.06 μM, which were several times more potent than standard drug with IC50 value of 750.0 ± 1.5 μM. Representatively, compound 11j showed remarkable anti-α-glucosidase potency with IC50 = 12.44 ± 0.38 μM, which was 60.3 times more potent than positive control acarbose. To explore the potential inhibition mechanism, further evaluations including kinetic analysis, circular dichroism, fluorescence spectroscopy, and thermodynamic profile were carried out for the most potent compound 11j. Moreover, molecular docking studies and in silico ADME prediction for all imidazoquinazolines 6a-c and 11a-o were performed to reveal their important binding interactions, as well as their physicochemical and drug-likeness properties, respectively.

Acarbose

ADME

IC50

10.1038/s41598-023-42549-5

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Citations (6)

Quinazoline-based VEGFR-2 inhibitors as potential anti-angiogenic agents: A contemporary perspective of SAR and molecular docking studies

European Journal of Medicinal Chemistry (2023)

Mahfam Moradi Ali Mousavi Zahra Emamgholipour Johanna Giovannini Setareh Moghimi

Vandetanib

Quinazoline

10.1016/j.ejmech.2023.115626

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Citations (26)

ChemInform Abstract: A One‐Pot, Three‐Component and Solvent‐Free Synthesis of 2,3‐Disubstituted Isoindolin‐1‐ones.

ChemInform (2015)

Mehdi Adib Fariba Peytam Mohsen Zainali Long‐Guan Zhu Jing Wu

Abstract Simply heating a mixture of β‐dicarbonyl compounds, benzylamines, and acid (II) under solvent‐free conditions gives isoindolines in good to excellent yields.

Component (thermodynamics)

10.1002/chin.201547130

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Citations (0)

Imidazo[1,2-a]quinazolines as novel, potent EGFR-TK inhibitors: Design, synthesis, bioactivity evaluation, and in silico studies

Bioorganic Chemistry (2023)

Zaman Hasanvand Tayebeh Oghabi Bakhshaiesh Fariba Peytam Loghman Firoozpour Elaheh Hosseinzadeh

EGFR Inhibitors

10.1016/j.bioorg.2023.106383

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Citations (8)

Identification of furo[2,3-d]pyrimidin-4-ylsulfanyl-1,3,4-thiadiazole derivatives as novel FLT3-ITD inhibitors