A5040460713- Synthesis and biological activity
- Computational Drug Discovery Methods
- Cholinesterase and Neurodegenerative Diseases
- Synthesis and Biological Evaluation
- Synthesis of β-Lactam Compounds
- Quinazolinone synthesis and applications
- Synthesis and Characterization of Heterocyclic Compounds
- Natural Antidiabetic Agents Studies
- Chemical synthesis and alkaloids
- Nanomaterials for catalytic reactions
- Click Chemistry and Applications
- melanin and skin pigmentation
- Estrogen and related hormone effects
- Phytochemical compounds biological activities
- Antiplatelet Therapy and Cardiovascular Diseases
- Cancer therapeutics and mechanisms
- Biochemical Analysis and Sensing Techniques
- Multicomponent Synthesis of Heterocycles
- Chemical synthesis and pharmacological studies
- Synthesis of Indole Derivatives
- Phenothiazines and Benzothiazines Synthesis and Activities
- Microwave-Assisted Synthesis and Applications
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Synthesis of heterocyclic compounds
- Nanoparticle-Based Drug Delivery
Iran University of Medical Sciences
2018-2024
Tehran University of Medical Sciences
2013-2015
University of Tehran
2013
Abstract In this article, different s-substituted benzimidazole-thioquinoline derivatives were designed, synthesized, and evaluated for their possible α-glucosidase inhibitory activities. The most active compound in series, 6j (X = 4-bromobenzyl) exhibited significant potency with an IC 50 value of 28.0 ± 0.6 µM compared to acarbose as the positive control 750.0 µM. kinetic study showed a competitive inhibition pattern against derivative. Also, molecular dynamic simulations performed...
In this work, a wide range of novel quinazolin‐4(3 H )‐one linked to 1,2,3‐triazoles was designed, synthesized, and evaluated against panel three human breast ( MDA ‐ MB ‐231, MCF ‐7, T‐47D), lung (A549), prostate PC 3) cancer cell lines. Our results revealed that the anticancer activity synthesized compounds selectively affected by presence methoxy group on linker between quinazolinone 1,2,3‐triazole moieties. According calculated IC 50 values, 6q , 6w 6x showed good cytotoxicity lines even...
Abstract In this work, a novel series of arylisoxazole‐phenylpiperazines were designed, synthesized, and evaluated toward acetylcholinesterase (AChE) butyrylcholinesterase (BChE). Our results revealed that [5‐(2‐chlorophenyl)‐1,2‐oxazol‐3‐yl](4‐phenylpiperazin‐1‐yl)methanone ( 5c ) was the most potent AChE inhibitor with IC 50 21.85 μ m . It should be noted synthesized compounds showed no BChE inhibitory activity [5‐(2‐fluorophenyl)‐1,2‐oxazol‐3‐yl](4‐phenylpiperazin‐1‐yl)methanone 5a active...
Abstract A novel series of hybrid arylisoxazole‐chromenone carboxamides were designed, synthesized, and evaluated for their cholinesterase (ChE) inhibitory activity based on the modified Ellman's method. Among synthesized compounds, 5‐(3‐nitrophenyl)‐ N ‐{4‐[(2‐oxo‐2 H ‐1‐benzopyran‐7‐yl)oxy]phenyl}‐1,2‐oxazole‐3‐carboxamide depicted most acetylcholinesterase (AChE) (IC 50 =1.23 μ m ) 5‐(3‐chlorophenyl)‐ was found to be potent butyrylcholinesterase (BChE) inhibitor =9.71 )....
Abstract In search of safer tacrine analogs, various thieno[2,3‐ b ]pyridine amine derivatives were synthesized and evaluated for their inhibitory activity against cholinesterases (ChEs). Among the compounds, compounds 5e 5d showed highest towards acetylcholinesterase butyrylcholinesterase, with IC 50 values 1.55 0.23 µM, respectively. The most active ChE inhibitors ( ) also candidates further complementary assays, such as kinetic molecular docking studies well on amyloid‐beta (βA)...
Abstract Background Platelet aggregation is one of the most important factors in development thrombotic disorders which plays a central role thrombosis (clot formation). Prophylaxis and treatment arterial are achieved using anti-platelet drugs. In this study, series novel substituted indole carbohydrazide was synthesized evaluated for activity induced by adenosine diphosphate (ADP), arachidonic acid (AA) collagen. Methods Our synthetic route started from methyl 1H-indole-3-carboxylate (1)...
Alzheimer's disease (AD) is a well-known neurodegenerative disorder affecting millions of old people worldwide and the corresponding epidemiological data emphasize importance disease. As AD multifactorial illness, various single target directed drugs that have reached clinical trials failed. Therefore, factors associated with outset been considered in targeted drug discovery. In this work, benzochromenoquinolinones were synthesized evaluated for their cholinesterase BACE1 inhibitory...
Abstract The complex pathophysiology of Alzheimer's disease (AD) has prompted researchers to develop multitarget‐directed molecules find an effective therapy against the disease. In this context, a novel series N ‐(1‐benzylpiperidin‐4‐yl)‐5‐arylisoxazole‐3‐carboxamide derivatives were designed, synthesized, and evaluated acetylcholinesterase (AChE) butyrylcholinesterase (BuChE). vitro biological evaluation demonstrated that compound 4e was best AChE (IC 50 = 16.07 μM) BuChE inhibitor 15.16...
Abstract A series of new boron-containing quinazolinones, benzo[d][1,3,2]diazaborinin-4(1H)-one derivatives, were synthesized by the sequential one-pot reaction isatoic anhydride, amines, and arylboronic acids in absence a catalyst solvent. Heating isotoic anhydride amines led to formation 2-aminobenzamide intermediates, which reacted easily with boronic obtain title compounds good yields. Solvent-free conditions provided unique procedure because corresponding products not obtained using...
Tamoxifen (TAM), the most widely used anti-estrogenic drug, inhibits progression of breast cancer through competing with estrogen for binding to receptor (ER). has been first-line adjuvant endocrine therapy in pre- and postmenopausal patients ER + two decades. However, due its side effects, interest using anticancer agents derived from natural foods increased. It recently stated that some probiotics can improve efficacy drugs via synergistic effects. Here, Local Probiotic Lactobacillus...
Abstract In this work, an efficient, user‐friendly, and simple procedure was reported for the preparation of indole derivatives catalyzed by heterogeneous SBA‐15‐Pr‐SO 3 H via Fischer pathway. The title compounds were synthesized from various arylhydrazines ketones in presence mol% catalyst refluxing ethanol.
Background: α-Glucosidase inhibitors have occupied a significant position in the treatment of type 2 diabetes. In this respect, development novel and efficient non-sugar-based is high demand. Objective: Design synthesis new 5-arylisoxazole-1,3,4-thiadiazole hybrids possessing α- glucosidase inhibitory activity were developed. Methods: Different derivatives synthesized by reaction various 5-arylisoxazole-3- carboxylic acids ethyl 2-((5-amino-1,3,4-thiadiazol-2-yl)thio)acetate. Finally, they...
Abstract Herein, a straightforward synthetic strategy mediated by Ugi reaction was developed to synthesize novel series of compounds as tyrosinase inhibitors. The structures all were confirmed FT‐IR, 1 H‐NMR, 13 C‐NMR, and CHNOS techniques. inhibitory activities synthesized derivatives 5a – m determined against mushroom it found that derivative 5c possesses the best inhibition with an IC 50 value 69.53±0.042 μM compared rest derivatives. Structure–activity relationships (SARs) showed...
Abstract Ring closure reactions of diaminomaleonitrile (DAMN) with electrophilic aryl isocyanates and isothiocyanates lead to the formation target 5,5′-diimino-1,1′-diaryl-4,4′-biimidazolidinylidene-2,2′-diones 2a,b 2,2′-diarylimino-4,4′-bithiazolidinylidenes 4a–e , respectively. The protocol provides a new strategy for synthesis wide range alkenes two electron-donating withdrawing substituents DAMN in moderate good yields.
In this study, a new series of N-(di or trimethoxyaryl)-5-arylisoxazole-3-carboxamide derivatives were synthesized and evaluated against human breast cancer cell lines including MCF-7, MDA-MB-231, T-47D. Among the compounds, 5-(m-tolyl)-N-(3,4,5-trimethoxyphenyl)isoxazole-3-carboxamide (8f) showed significant cytotoxicity all three comparing with etoposide as reference drug. Also, Annexin V-FITC/propidium iodide acridine orange/ethidium bromide staining assay performed to validate apoptotic...
Abstract In recent years, focusing on new potent anticancer agents with selective activity is one of the greatest challenges in cancer therapy. Breast most common and main cause deaths women. The sulfatase enzyme plays an important role converting sulfated steroids into non-sulfate steroid hormones, which increases growth development many hormone-dependent cancers, such as breast cancer. this regard, structure-based optimization was conducted to design novel flavone-sulfonates pharmacophore...
In this study, an attempt was made to synthesize, characterize, and develop many applications of functionalized rare metal oxide nanoparticles. Herein, a new strategy for drug delivery is developed functionalize magnetite nanoparticles improve their performances in the celecoxib.Magnetite Fe3O4@SiO2 are synthesized by sol-gel method. The surface hydroxyl groups extended treating with cerium nitrate salt; finally, sodium hydroxide anchored produce oxidefunctionalized Fe3O4@SiO2@CeO2 magnetic...