Seyedeh Sara Mirfazli

Iran University of Medical Sciences · Medicinal Chemistry

Fluorine-containing small molecules have occupied a special position in drug discovery research. The successful clinical use of fluorinated corticosteroids in the 1950s and fluoroquinolones in the 1980s led to an ever-increasing number of approved fluorinated compounds over the last 50 years. They have shown various biological properties such as an...

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 this series, 6j (X = 4-bromobenzyl) exhibited significant potency with an IC50 value of 28.0 ± 0.6 µM compared to acarbose as the positive cont...

Skin and hair pigmentation, skin cancer, and enzymatic browning of plants and fruits are caused by tyrosinase, a di‐copper oxidase. In the present work, we developed a novel series of substituted benzyl‐1,2,3‐triazole derivatives linked to hydrazinecarbothiamide via methoxyphenyl linker and assessed them for their tyrosinase inhibitory effects in t...

Herein, a straightforward synthetic strategy mediated by Ugi reaction was developed to synthesize novel series of compounds as tyrosinase inhibitors. The structures of all compounds were confirmed by FT‐IR, 1H‐NMR, 13C‐NMR, and CHNOS techniques. The tyrosinase inhibitory activities of all synthesized derivatives 5a–m were determined against mushroo...

In the current study, twenty-five indole-carbohydrazide derivatives linked to different aryl substitutions were rationally designed and synthesized. The structures of all derivatives were confirmed using different spectroscopic techniques including ¹H-NMR, ¹³C-NMR, Mass spectrometry, and elemental analysis. The tyrosinase inhibitory activities of a...

In this work, various imidazo[1,2-a]pyridines linked to carbamate moiety were designed, synthesized, and evaluated for their α-glucosidase inhibitory activity. Among synthesized compounds, 4-(3-(tert-Butylamino)imidazo[1,2-a]pyridin-2-yl)phenyl p-tolylcarbamate (6d) was the most potent compound (IC50 = 75.6 µM) compared with acarbose as the referen...

Aims and objectives 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 to functionalize magnetite nanoparticles to improve their performances in the delivery of celecoxib. Materials and methods Magnetit...

In recent years, focusing on new potent anticancer agents with selective activity is one of the greatest challenges in cancer therapy. Breast cancer is the most common cancer and the main cause of cancer deaths in women. The sulfatase enzyme plays an important role in converting the sulfated steroids into non-sulfate steroid hormones, which increas...

In recent years, focusing on new potent anticancer agents with selective activity is one of the greatest challenges in cancer therapy. Breast cancer is the most common cancer and the main cause of cancer deaths in women. The sulfatase enzyme plays an important role in converting the sulfated steroids into non-sulfate steroid hormones, which increas...

In view of the multifactorial nature of Alzheimer's disease, a new series of methylindolinone-1,2,3-triazole derivatives (7a-n) were efficiently prepared and evaluated for their in vitro cholinesterase inhibitory activity. Although most synthesized compounds showed weak acetylcholinesterase inhibitory activity, they depicted moderate to good activi...

Background α-Glucosidase inhibitors have occupied a significant position in the treatment of type 2 diabetes. In this respect, development of novel and efficient non sugar-based inhibitors are highly in demand. Objective Design and synthesis of new 5-arylisoxazole-1,3,4-thiadiazole hybrids possessing α-glucosidase inhibitory activity was developed...

The complex pathophysiology of Alzheimer's disease (AD) has prompted researchers to develop multitarget‐directed molecules to find an effective therapy against the disease. In this context, a novel series of N‐(1‐benzylpiperidin‐4‐yl)‐5‐arylisoxazole‐3‐carboxamide derivatives were designed, synthesized, and evaluated against acetylcholinesterase (A...

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 synthesized compounds, compounds 5e and 5d showed the highest activity towards acetylcholinesterase and butyrylcholinesterase, with IC50 values of 1.55 and 0.23 µM...

Tamoxifen (TAM), the most widely used anti-estrogenic drug, inhibits the progression of breast cancer through competing with estrogen for binding to the estrogen receptor (ER). Tamoxifen has been the first-line adjuvant endocrine therapy in pre- and postmenopausal patients with ER + breast cancer for two decades. However, due to its side effects, i...

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-2H-chromen-7-yl)oxy)phenyl)isoxazole-3-carboxamide (11h) depicted the most acetylcholinesterase...

In this work, an efficient, user‐friendly, and simple procedure was reported for the preparation of indole derivatives catalyzed by the heterogeneous SBA‐15‐Pr‐SO3H via Fischer indole pathway. The title compounds were synthesized from various arylhydrazines and ketones in the presence of 3 mol% of the catalyst in the refluxing ethanol.

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, and T-47D. Among the synthesized compounds, 5-(m-tolyl)-N-(3,4,5-trimethoxyphenyl)isoxazole-3-carboxamide (8f) showed significant cytotoxicity against al...

Alzheimer’s disease (AD) is a well‐known neurodegenerative disorder affecting millions of old people worldwide and the corresponding epidemiological data emphasize the importance of the disease. As AD is a multifactorial illness, various single‐target directed drugs that have reached clinical trials have failed. Therefore, various factors associate...

In this work, a novel series of arylisoxazole‐phenylpiperazines 5a‐k were designed, synthesized, and evaluated toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Our results revealed that (5‐(2‐chlorophenyl)isoxazol‐3‐yl)(4‐phenylpiperazin‐1‐yl)methanone (5c) was the most potent AChE inhibitor with IC50 of 21.85 µM. It should be n...

Ring closure reactions of diaminomaleonitrile (DAMN) with electrophilic aryl isocyanates and aryl isothiocyanates lead to the formation of the target 5,5′-diimino-1,1′-diaryl-4,4′-biimidazolidinylidene-2,2′-diones 2a,b and 2,2′-diarylimino-4,4′-bithiazolidinylidenes 4a–e , respectively. The protocol provides a new strategy for the synthesis of a wi...

Alzheimer's disease (AD) is a well-known neurodegenerative disorder affecting millions of old people worldwide and the corresponding epidemiological data highlights the significance of the disease. As AD is a multifactorial illness, various single-target directed drugs that have reached clinical trials have failed. Therefore, various factors associ...

In this work, a wide range of novel quinazolin‐4(3H)‐one linked to 1,2,3‐triazoles were designed, synthesized, and evaluated against a panel of three human breast (MDA‐MB‐231, MCF‐7, T‐47D), lung (A549), and prostate (PC3) cancer cell lines. Our results revealed that the anticancer activity of the synthesized compounds was selectively affected by t...

A series of novel substituted indole carbohydrazide was synthesized and evaluated for anti-platelet aggregation activity. The structures of the synthesized compounds were confirmed by spectral data and elemental analysis and were evaluated for their ability to inhibit platelet aggregation induced by adenosine diphosphate, arachidonic acid (AA) and...

Background Platelet aggregation is one of the most important factors in the development of thrombotic disorders which plays a central role in thrombosis (clot formation). Prophylaxis and treatment of arterial thrombosis are achieved using anti-platelet drugs. In this study, a series of novel substituted indole carbohydrazide was synthesized and eva...

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 of isatoic anhydride, amines, and arylboronic acids in the absence of a catalyst and solvent. Heating isotoic anhydride and amines led to the formation of 2-aminobenzamide intermediates, which react...