Alireza Foroumadi
Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
[ 1 ] - N-Phenyl-2-p-tolylthiazole-4-carboxamide derivatives: Syn-thesis and cytotoxicity evaluation as anticancer agents
Objective(s):According to the prevalence of neoplastic diseases, there is a deep necessity for discovery of novel anticancer drugs in the field of medicinal chemistry. In the current study, a new series ofphenylthiazole derivatives(compounds 4a-4f) was synthesizedand theiranticancer activity was assessed in vitro. Materials and Methods:All synthesized derivatives were evaluated towards three h...
[ 2 ] - Synthesis and In Vitro Cytotoxic Activity of Novel Chalcone-Like Agents
Objective(s): Chalcones and their rigid analogues represent an important class of small molecules having anticancer activities. Therefore, in this study the synthesis and cytotoxic activity of new 3-benzylidenchroman-4-ones were described as rigid chalcone analogues. Materials and Methods: The reaction of resorcinol with 3-chloropropionic acid in the presence of CF3SO3H was a...
[ 3 ] - Synthesis and Evaluation of Anti-acetylcholinesterase Activity of 2-(2-(4-(2-Oxo-2-phenylethyl)piperazin-1-yl) ethyl)Isoindoline-1,3-dione Derivatives with Potential Anti-Alzheimer Effects
Objective(s): Alzheimer's disease (AD) is a neurodegenerative disorder in elderly patients. Decrease in cholinergic neurotransmission is the main known cause in the pathophysiology of the disease. Improvement and potentiation of the cholinergic system could be beneficial for treatment of the AD. Acetylcholinesterase inhibitors such as donepezil can enhance the duration of action of a...
[ 4 ] - Brønsted Acidic Phosphonium Based Ionic Liquid Functionalized SBA-15 [HO3S-PhospIL@SBA-15]: Green, Recyclable, and Efficient Catalyst for the Synthesis of Pyrano[3,2-c]Chromenone Derivatives
The surface of SBA-15 was modified by diphenylphosphine; then, it was treated with butane sultone and sulfuric acid to obtain Brønsted acid HO3S-phosphonium based ionic liquid functionalized SBA-15 with HSO4- as a counteranion. It efficiently catalyzed synthesis of pyrano[3,2-c]chromenone derivatives through the reaction of 4-hydroxycoumarin and chalcones at...
[ 5 ] - Synthesis and Leishmanicidal Activity of 1-[5-(5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl]-4-benzoylepiperazines
A series of (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives 6a–6e have been synthesized and screened for in vitro anti-leishmanial activity against the promastigote form of L. major. The structure of Schiff bases were confirmed by 1H NMR, IR. Screening results indicate that all of the designed and synthesized final compounds (6a-6e) significantly reduced the viability of promastigotes ...
[ 6 ] - in silico screening of IL-1β production inhibitors using chemometric tools
The IL-1β play a major role in inflammatory disorders and IL-1β production inhibitors can be used in the treatment of inflammatory and related diseases. In this study, quantitative relationships between the structures of 46 pyridazine derivatives (inhibitors of IL-1β production) and their activities were investigated by Multiple Linear Regression (MLR) technique Stepwise Regression Method (ES-S...
[ 7 ] - Novel N-2-(Furyl)-2-(chlorobenzyloxyimino) ethyl Piperazinyl Quinolones: Synthesis, Cytotoxic Evaluation and Structure-activity Relationship
Quinolone antibacterials are one of the most important classes of pharmacological agents known as potent inhibitors of bacterial DNA gyrase and topoisomerase IV that efficiently inhibit DNA replication and transcription by generating several double-stranded DNA break. Some quinolone derivatives demonstrated inhibitory potential against eukaryote topoismarase II and substantial dose-dependent cy...
[ 8 ] - Synthesis and Biological Investigation of some Novel Sulfonamide and Amide Derivatives Containing Coumarin Moieties
New sulfonamide and amide derivatives containing coumarin moieties; oxo-2H-chromen-sulfamoylphenylacetamides and oxo-2H-chromen-arylacetamides were synthesized starting from diverse 2-chloroacetamide derivatives and a wide range of coumarins. The structures of the obtained compounds were elucidated by IR and NMR spectra and also analytical elemental analysis. In the next step, the above mention...
[ 9 ] - 2-Amino-4-(nitroalkyl)-4H-chromene-3-carbonitriles as New Cytotoxic Agents
A series of 2-amino-4-(nitroalkyl)-4H-chromene-3-carbonitriles were synthesized by an efficient multicomponent reaction in aqueous media using DBU (1,8-diazabicyclo[5.4.0]undec-7-ene) as a catalyst at room temperature. Mild condition, environment friendly procedure and excellent yields are the main advantages of this procedure. The cytotoxic activity of target compounds were evaluated against t...
[ 10 ] - Anti-Helicobacter pylori activity and Structure-Activity Relationship study of 2-Alkylthio-5-(nitroaryl)-1,3,4-thiadiazole Derivatives
Nitro-containing heteroaromatic derivatives structurally related to nitroimidazole (Metronidazole) are being extensively evaluated against Helicobacter pylori isolates. On the other hand, 1,3,4-thiadiazole derivatives have also demonstrated promising antibacterial potential. In present study, we evaluated anti-H. pylori activity of novel hybrid molecules bearing nitroaryl and 1,3,4-thiadiazole ...
[ 11 ] - Synthesis and Antidiabetic Evaluation of Benzenesulfonamide Derivatives
The complex metabolic syndrome, diabetes mellitus, is a major human health concern in the world and is estimated to affect 300 million people by the year 2025. Several drugs such as sulfonylureas and biguanides are presently available to reduce hyperglycemia in diabetes mellitus. These drugs have side effects and thus searching for a new class of compounds is essential to overcome this problems...
[ 12 ] - PEGylation of Octreotide Using an α,β-unsaturated-β′-mono-sulfone Functionalized PEG Reagent
PEGylation is a well-established technique utilized to overcome the problems related to the therapeutic applications of peptides and proteins. Reasons for the PEGylation of these biological macromolecules include reducing immunogenicity, proteolytic degradation and rapid clearance from blood circulation. Octreotide is an octapeptide analogue of naturally-occurred somatostatin. This peptide has ...
[ 13 ] - Synthesis and In-vitro Antibacterial Activities of Acetylanthracene and Acetylphenanthrene Derivatives of Some Fluoroquinolones
Novel analogues of N-piperazinyl fluoroquinolones were prepared and evaluated against a panel of Gram-positive and Gram-negative bacteria, to study the effect of introducing bulky anthracene and phenanthrene moieties on the antibacterial effects of norfloxacin, ciprofloxacin and gatifloxacin. Although most of the novel synthesized compounds had lower antibacterial effects, some derivatives show...
[ 14 ] - Synthesis and Leishmanicidal Activity of 1-[5-(5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl]-4-benzoylepiperazines
A series of (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives 6a–6e have been synthesized and screened for in vitro anti-leishmanial activity against the promastigote form of L. major. The structure of Schiff bases were confirmed by 1H NMR, IR. Screening results indicate that all of the designed and synthesized final compounds (6a-6e) significantly reduced the viability of promastigotes ...
[ 15 ] - in silico screening of IL-1β production inhibitors using chemometric tools
The IL-1β play a major role in inflammatory disorders and IL-1β production inhibitors can be used in the treatment of inflammatory and related diseases. In this study, quantitative relationships between the structures of 46 pyridazine derivatives (inhibitors of IL-1β production) and their activities were investigated by Multiple Linear Regression (MLR) technique Stepwise Regression Method (ES-S...
[ 16 ] - Novel N-2-(Furyl)-2-(chlorobenzyloxyimino) ethyl Piperazinyl Quinolones: Synthesis, Cytotoxic Evaluation and Structure-activity Relationship
Quinolone antibacterials are one of the most important classes of pharmacological agents known as potent inhibitors of bacterial DNA gyrase and topoisomerase IV that efficiently inhibit DNA replication and transcription by generating several double-stranded DNA break. Some quinolone derivatives demonstrated inhibitory potential against eukaryote topoismarase II and substantial dose-dependent cy...
[ 17 ] - Synthesis and Biological Investigation of some Novel Sulfonamide and Amide Derivatives Containing Coumarin Moieties
New sulfonamide and amide derivatives containing coumarin moieties; oxo-2H-chromen-sulfamoylphenylacetamides and oxo-2H-chromen-arylacetamides were synthesized starting from diverse 2-chloroacetamide derivatives and a wide range of coumarins. The structures of the obtained compounds were elucidated by IR and NMR spectra and also analytical elemental analysis. In the next step, the above mention...
[ 18 ] - 2-Amino-4-(nitroalkyl)-4H-chromene-3-carbonitriles as New Cytotoxic Agents
A series of 2-amino-4-(nitroalkyl)-4H-chromene-3-carbonitriles were synthesized by an efficient multicomponent reaction in aqueous media using DBU (1,8-diazabicyclo[5.4.0]undec-7-ene) as a catalyst at room temperature. Mild condition, environment friendly procedure and excellent yields are the main advantages of this procedure. The cytotoxic activity of target compounds were evaluated against t...
[ 19 ] - Anti-Helicobacter pylori activity and Structure-Activity Relationship study of 2-Alkylthio-5-(nitroaryl)-1,3,4-thiadiazole Derivatives
Nitro-containing heteroaromatic derivatives structurally related to nitroimidazole (Metronidazole) are being extensively evaluated against Helicobacter pylori isolates. On the other hand, 1,3,4-thiadiazole derivatives have also demonstrated promising antibacterial potential. In present study, we evaluated anti-H. pylori activity of novel hybrid molecules bearing nitroaryl and 1,3,4-thiadiazole ...
[ 20 ] - Synthesis and Antidiabetic Evaluation of Benzenesulfonamide Derivatives
The complex metabolic syndrome, diabetes mellitus, is a major human health concern in the world and is estimated to affect 300 million people by the year 2025. Several drugs such as sulfonylureas and biguanides are presently available to reduce hyperglycemia in diabetes mellitus. These drugs have side effects and thus searching for a new class of compounds is essential to overcome this problems...
[ 21 ] - PEGylation of Octreotide Using an α,β-unsaturated-β′-mono-sulfone Functionalized PEG Reagent
PEGylation is a well-established technique utilized to overcome the problems related to the therapeutic applications of peptides and proteins. Reasons for the PEGylation of these biological macromolecules include reducing immunogenicity, proteolytic degradation and rapid clearance from blood circulation. Octreotide is an octapeptide analogue of naturally-occurred somatostatin. This peptide has ...
[ 22 ] - Synthesis and In-vitro Antibacterial Activities of Acetylanthracene and Acetylphenanthrene Derivatives of Some Fluoroquinolones
Novel analogues of N-piperazinyl fluoroquinolones were prepared and evaluated against a panel of Gram-positive and Gram-negative bacteria, to study the effect of introducing bulky anthracene and phenanthrene moieties on the antibacterial effects of norfloxacin, ciprofloxacin and gatifloxacin. Although most of the novel synthesized compounds had lower antibacterial effects, some derivatives show...
[ 23 ] - اثرات ضدهلیکوباکترپیلوری عصاره متانولی برخی گونههای جنس Stachys و Melia
مقدمه: باکتری گرم منفی هلیکوباکترپیلوری که اولین بار در سال 1982 میلادی شناسایی شده است، امروزه به عنوان مهمترین عامل التهاب معده و زخمهای گوارشی مطرح است. با افزایش مقاومت باکتریها به آنتیبیوتیکهای موجود، لزوم مطالعه برای یافتن داروهایی با منشای گیاهی ضروری به نظر میرسد. هدف: هدف از مطالعه حاضر، بررسی خواص ضدهلیکوباکترپیلوری عصاره 10 گیاه موجود در ایران بر علیه سوشهای بالینی هلیکوباکت...
[ 25 ] - Cholinesterase Inhibition Activity and Docking Simulation Study of Coumarin Mannich Base Derivatives
Inhibition of acetylcholinesterase and butyrylcholinesterase (AChE and BuChE) as two major forms of cholinesterases (ChEs) is considered as the common approach for the treatment of Alzheimer's disease (AD). The present study was done to explore the anticholinesterase inhibition property of coumarin Mannich base derivatives. A series of cumarin Manich bases were synthesized (4a-h) through one-po...
[ 26 ] - Novel 5-(nitrothiophene-2-yl)-1,3,4-Thiadiazole Derivatives: Synthesis and Antileishmanial Activity against promastigote stage of Leishmania major
In this study, a series of novel compounds based on 5-(5-nitrothiophene-2-yl)-1,3,4-thiadiazole possessing (het)aryl thio pendant at C-2 position of thiadiazole ring is developed and evaluated as antileishmanial agents using MTT colorimetric assay. 10 New compounds containing aryl and hetero aryl derivatives, started from thiophene-2-carbaldehyde in five steps, were synthesized in good to excel...
[ 27 ] - Novel 5-(nitrothiophene-2-yl)-1,3,4-Thiadiazole Derivatives: Synthesis and Antileishmanial Activity against promastigote stage of Leishmania major
In this study, a series of novel compounds based on 5-(5-nitrothiophene-2-yl)-1,3,4-thiadiazole possessing (het)aryl thio pendant at C-2 position of thiadiazole ring is developed and evaluated as antileishmanial agents using MTT colorimetric assay. 10 New compounds containing aryl and hetero aryl derivatives, started from thiophene-2-carbaldehyde in five steps, were synthesized in good to excel...
[ 28 ] - Synthesis and in vitro Anti-Bacterial Activity of 2-(5-Nitro-2-heteroaryl)-1,3,4-Thiadiazole Derivatives
A new series of 2-(5-nitro-2-heteroaryl)-1,3,4-thiadiazole derivatives, including nitro furan, nitro thiophene and nitro imidazole, were synthesized and screened in vitro for their inhibitory activity against eight bacterial strains. The results showed that most of the synthesized compounds were active against Gram-positive bacteria, determined by MIC method. Among them, compounds <str...
[ 29 ] - Effect of 3,4-Methylenedioxymethamphetamine on Liver CYP2C19 Enzyme Activity in Isolated Perfused Rat Liver Using Omeprazole Probe
Background and purpose: This study aimed at investigating the effects of 3,4-Methylenedioxymethamphetamine (MDMA) on liver cytochrome 2C19 enzyme activity, which is a major liver enzyme in the metabolism of a wide range of drugs, using omeprazole as a probe of the CYP2C19 activity in isolated perfused rat liver. Materials and methods: This experimental study was done in 20 male Sprague–Da...
[ 30 ] - Synthesis and DFT Calculation of a New Series of Enaminones based on 3-amino Coumarin
In this paper, the synthesis of various enaminones from the reaction of 3-aminocoumarin and ethyl-2,4-dioxo-4-arylbutanoate in the presence of p-toluene sulfonic acid is reported. The reaction was examined under different solvents and catalytic systems, which clearly proved the importance of acidic catalyst in this organic transformation. This work was also accompanied by density functional the...