Mohsen Amini
Associate professor of Medicinal Chemistry Department, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
[ 1 ] - Novel and efficient method for solid phase synthesis of urea-containing peptides targeting prostate specific membrane antigen (PSMA) in comparison with current methods
The basic chemical structure of most prostate specific membrane antigen (PSMA) inhibitors which are now in pre-clinical and clinical studies is Glu-Ureido-based peptides. Synthesis of urea-based PSMA inhibitors includes two steps: 1- isocyanate intermediate formation and 2- urea bond formation. In current methods, isocyanate is formed in liquid phase and then reacts with amine existing in liqui...
[ 2 ] - Nimodipine-Loaded Pluronic Block Copolymer Micelles: Preparation, Characterization, In Vitro and In Vivo Studies
Nimodipine (NM), as a lipophilic calcium channel blocker indicated for the prevention and treatment of neurological disorders, suffers from an extensive first pass metabolism, resulting in low oral bioavailability. Polymeric micelles, self-assembled from amphiphilic polymers, have a core-shell structure which makes them unique nano-carriers with excellent performance as drug delivery. This inve...
[ 3 ] - Preparation of Diaminedicarboxyplatinum (II) Functionalized Single-Wall Carbon Nanotube via Bingel Reaction As a Novel Cytotoxic Agent
Carbon nanotubes have unique properties like high stability, high surface to mass ratio and so on which make them suitable for medicinal purpose applications. Treatment of cancer by organoplatinum agents like Cisplatin has become unresponsive in most cases due to low distribution of drug in biological fluids, inability of drug to cross cellular membranes and low stability in biological environm...
[ 4 ] - Synthesis, Radiolabeling, and Biological Evaluation of Peptide LIKKPF Functionalized with HYNIC as Apoptosis Imaging Agent
Introduction: A noninvasive method of detecting exposure of phosphatidylserine (PS) on the external surface of the plasma membrane such as nuclear imaging could assist the diagnosis and therapy of apoptosis related pathologies. The most studied imaging agent for apoptosis is Annexin V so far. Because of limitations of Annexin V other agents have been introduced such as small peptides and molecu...
[ 5 ] - Design, Synthesis and Evaluation of Antitubercular Activity of Novel Dihydropyridine Containing Imidazolyl Substituent
Recent studies have indicated that 1, 4-dihydropyridine-3, 5-dicarboxamidederivativesshow significant anti-tubercular activity. In this research, new derivatives of 1, 4-dihydropyridine were designed and synthesized using Hantzsch condensation in which dicyclohexyl and different dicyclohexylcarbamoylwere substituted at C-3 and C-5 positions of the DHP ring.In addition, 4 (5)-chloro-2-methyl-5 (...
[ 6 ] - Preparation and Antibacterial Activity Evaluation of 18-β-glycyrrhetinic Acid Loaded PLGA Nanoparticles
AbstractThe aim of the present study was to formulate poly (lactide-co-glycolide) (PLGA) nanoparticles loaded with 18-β-glycyrrhetinic acid (GLA) with appropriate physicochemical properties and antimicrobial activity. GLA loaded PLGA nanoparticles were prepared with different drug to polymer ratios, acetone contents and sonication times and the antibacterial activity of the developed nanopartic...
[ 7 ] - Two Matrix Metalloproteinase Inhibitors from Scrophularia Striata Boiss
Many species belonging to the Scrophularia genus have been used since ancient times as folk remedies for many medical conditions such as scrofulas, scabies, tumors, eczema, psoriasis, inflammations. The aim of this study was to characterize the matrix metalloproteinases (MMPs) inhibitor compounds of the Scrophularia striata extract by bio-guide fractionation. The aerial parts of S. striata were...
[ 8 ] - Synthesis, Evaluation of Anticancer Activity and QSAR Study of Heterocyclic Esters of Caffeic Acid
Caffeic acid phenethyl ester(CAPE) suppresses the growth of transformed cells such as human breast cancer cells, hepatocarcinoma , myeloid leukemia, colorectal cancer cells, fibrosarcoma, glioma and melanoma. A group of heterocyclic esters of caffeic acid was synthesized using Mitsunobu reaction and the esters were subjected to further structural modification by electrooxidation of the catecho...
[ 9 ] - Synthesis and analgesic activity of novel Hydrazide and Hydrazine derivatives
The uses of non-steroidal anti-inflammatory drugs (NSAIDs) are limited by a variety of side effects. So research on preparing new analgesic agents is important. According to some reports about the analgesic activity of hydrazide and hydrazine derivatives a new series of these compounds were synthesized in order to obtain new analgesic compounds. The final compounds 10a-10e and 15a-15d were pre...
[ 10 ] - High Performance Liquid Chromatography Coupled with Pre-column Derivatization for Determination of Oxidized Glutathione Level in Rats Exposed to Paraquat
Glutathione (GSH) is one of the most important antioxidants that plays an essential role in detoxification of reactive oxygen species (ROS) which oxidizes to glutathione disulfide (GSSG). Paraquat (PQ), awidely used herbicide, causes pulmonary injury with the productionof ROS. Excessive ROS accumulation as a consequence of PQ exposure are frequently targeted by GSH thereby oxidative stress lead...
[ 11 ] - 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 ...
[ 12 ] - Comparative Chemical Composition and Antioxidant Properties of the Essential Oils and Aromatic Water from Teucrium persicum Boiss
The essential oils and aromatic water, known as Arak in traditional Iranian medicine, comes from the aerial part of Teucrium persicum Boiss., which is grown in Fars Province located in Iran. The samples were collected in summer and the oils and aromatic water were obtained through steam distillation. The chemical composition of the oils was analyzed using GC-MS. An analysis of the chemical...
[ 13 ] - Rational evaluation of antimicrobial properties of lactobacilli isolates against some pathogenic microorganisms: a new method comparing the susceptibility of indicator microorganisms
BACKGROUND: Lactobacilli are known as a valuable sourceof antimicrobial compounds and have a high potential of use infood biopreservation against food related microorganisms.OBJECTIVES: Antimicrobial potency of 63 dairy lactobacilliisolates against four highly important food-related microorganismswere evaluated. In addition, a new way in data organization wasintroduced, which led to a more info...
[ 14 ] - Novel and efficient method for solid phase synthesis of urea-containing peptides targeting prostate specific membrane antigen (PSMA) in comparison with current methods
The basic chemical structure of most prostate specific membrane antigen (PSMA) inhibitors which are now in pre-clinical and clinical studies is Glu-Ureido-based peptides. Synthesis of urea-based PSMA inhibitors includes two steps: 1- isocyanate intermediate formation and 2- urea bond formation. In current methods, isocyanate is formed in liquid phase and then reacts with amine existing in liqui...
[ 15 ] - Nimodipine-Loaded Pluronic Block Copolymer Micelles: Preparation, Characterization, In Vitro and In Vivo Studies
Nimodipine (NM), as a lipophilic calcium channel blocker indicated for the prevention and treatment of neurological disorders, suffers from an extensive first pass metabolism, resulting in low oral bioavailability. Polymeric micelles, self-assembled from amphiphilic polymers, have a core-shell structure which makes them unique nano-carriers with excellent performance as drug delivery. This inve...
[ 16 ] - Preparation of Diaminedicarboxyplatinum (II) Functionalized Single-Wall Carbon Nanotube via Bingel Reaction As a Novel Cytotoxic Agent
Carbon nanotubes have unique properties like high stability, high surface to mass ratio and so on which make them suitable for medicinal purpose applications. Treatment of cancer by organoplatinum agents like Cisplatin has become unresponsive in most cases due to low distribution of drug in biological fluids, inability of drug to cross cellular membranes and low stability in biological environm...
[ 17 ] - Synthesis, Radiolabeling, and Biological Evaluation of Peptide LIKKPF Functionalized with HYNIC as Apoptosis Imaging Agent
Introduction: A noninvasive method of detecting exposure of phosphatidylserine (PS) on the external surface of the plasma membrane such as nuclear imaging could assist the diagnosis and therapy of apoptosis related pathologies. The most studied imaging agent for apoptosis is Annexin V so far. Because of limitations of Annexin V other agents have been introduced such as small peptides and molecu...
[ 18 ] - Design, Synthesis and Evaluation of Antitubercular Activity of Novel Dihydropyridine Containing Imidazolyl Substituent
Recent studies have indicated that 1, 4-dihydropyridine-3, 5-dicarboxamidederivativesshow significant anti-tubercular activity. In this research, new derivatives of 1, 4-dihydropyridine were designed and synthesized using Hantzsch condensation in which dicyclohexyl and different dicyclohexylcarbamoylwere substituted at C-3 and C-5 positions of the DHP ring.In addition, 4 (5)-chloro-2-methyl-5 (...
[ 19 ] - Preparation and Antibacterial Activity Evaluation of 18-β-glycyrrhetinic Acid Loaded PLGA Nanoparticles
AbstractThe aim of the present study was to formulate poly (lactide-co-glycolide) (PLGA) nanoparticles loaded with 18-β-glycyrrhetinic acid (GLA) with appropriate physicochemical properties and antimicrobial activity. GLA loaded PLGA nanoparticles were prepared with different drug to polymer ratios, acetone contents and sonication times and the antibacterial activity of the developed nanopartic...
[ 20 ] - Two Matrix Metalloproteinase Inhibitors from Scrophularia Striata Boiss
Many species belonging to the Scrophularia genus have been used since ancient times as folk remedies for many medical conditions such as scrofulas, scabies, tumors, eczema, psoriasis, inflammations. The aim of this study was to characterize the matrix metalloproteinases (MMPs) inhibitor compounds of the Scrophularia striata extract by bio-guide fractionation. The aerial parts of S. striata were...
[ 21 ] - Synthesis, Evaluation of Anticancer Activity and QSAR Study of Heterocyclic Esters of Caffeic Acid
Caffeic acid phenethyl ester(CAPE) suppresses the growth of transformed cells such as human breast cancer cells, hepatocarcinoma , myeloid leukemia, colorectal cancer cells, fibrosarcoma, glioma and melanoma. A group of heterocyclic esters of caffeic acid was synthesized using Mitsunobu reaction and the esters were subjected to further structural modification by electrooxidation of the catecho...
[ 22 ] - Synthesis and analgesic activity of novel Hydrazide and Hydrazine derivatives
The uses of non-steroidal anti-inflammatory drugs (NSAIDs) are limited by a variety of side effects. So research on preparing new analgesic agents is important. According to some reports about the analgesic activity of hydrazide and hydrazine derivatives a new series of these compounds were synthesized in order to obtain new analgesic compounds. The final compounds 10a-10e and 15a-15d were pre...
[ 23 ] - High Performance Liquid Chromatography Coupled with Pre-column Derivatization for Determination of Oxidized Glutathione Level in Rats Exposed to Paraquat
Glutathione (GSH) is one of the most important antioxidants that plays an essential role in detoxification of reactive oxygen species (ROS) which oxidizes to glutathione disulfide (GSSG). Paraquat (PQ), awidely used herbicide, causes pulmonary injury with the productionof ROS. Excessive ROS accumulation as a consequence of PQ exposure are frequently targeted by GSH thereby oxidative stress lead...
[ 24 ] - 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 ...
[ 25 ] - Comparative Chemical Composition and Antioxidant Properties of the Essential Oils and Aromatic Water from Teucrium persicum Boiss
The essential oils and aromatic water, known as Arak in traditional Iranian medicine, comes from the aerial part of Teucrium persicum Boiss., which is grown in Fars Province located in Iran. The samples were collected in summer and the oils and aromatic water were obtained through steam distillation. The chemical composition of the oils was analyzed using GC-MS. An analysis of the chemical...
[ 26 ] - Preclinical study of a new 177Lu-labeled somatostatin receptor antagonist in HT-29 human colorectal cancer cells
Objective(s): Somatostatin receptor-positive neuroendocrine tumors have been targeted using various peptide analogs radiolabeled with therapeutic radionuclides for years. The better biomedical properties of radioantagonists as higher tumor uptake make these radioligands more attractive than agonists for somatostatin receptor-targeted radionuclide therapy. In this study...
نویسندگان همکار