Maryam Iman
Department of Pharmaceutics, Faculty of pharmacy, Baqiyatallah University of Medical Sciences, Tehran, Iran|Chemical Injuries Research Center, Baqiyatallah University of Medical Sciences, Tehran, Iran
[ 1 ] - Novel derivatives of phthalimide with potent anticonvulsant activity in PTZ and MES seizure models
Objective(s): Phthalimide-based derivatives have anticonvulsant activity like as phenytoin by inhibition of sodium channel. In our previously research we mentioned about some phthalimide derivatives as potent anticonvulsant agents. Materials and Methods: Fourteen analogs of 2-substituted phthalimide pharmacophore were synthesized and then were evaluated for the anticonvulsant activities in pent...
[ 2 ] - Docking Studies of Phthalimide Pharmacophore as a Sodium Channel Blocker
Objective(s): Recently, phthalimide derivatives were designed based on ameltolide and thalidomide as they possess a similar degree of anticonvulsant potency due to their phenytoin-like profile. The ability of phthalimide pharmacophore to interact with neuronal voltage-dependent sodium channels was studied in the batrachotoxin affinity assay. Therefore, in the present study, a series of 19 com...
[ 3 ] - Design and Synthesis of 4-flurophthalimides as potential anticonvulsant agents
Objective(s): Anticonvulsant activity of phthalimide was discovered in 2000 by molecular hybridization of thalidomide and ameltolide. In our previous research we have reported some new 4-substituted derivatives of phthalimide with good activity against the tonic and clonic seizures Material and Methods: A series of novel 4-flurophthalimides that designed using bioisosteric replacement were synt...
[ 4 ] - Docking Studies, Synthesis, and In-vitro Evaluation of Novel Oximes Based on Nitrones as Reactivators of Inhibited Acetylcholinesterase
Acetylcholinesterase has important role in synaptic cleft. It breaks down the acetylcholineatcholinergic synapsesand terminates the cholinergic effects. Some chemical agents likeorganophosphorus compounds (OPCs) including nerve agents and pesticides react withacetylcholinesteraseirreversibly. They inhibit normal biological enzyme action and resultin accumulation of acetylcholineand show toxic e...
[ 5 ] - Docking, Synthesis and anticonvulsant activity of N-substituted isoindoline-1,3-dione
A series of compounds related to ameltolide were studied for anticonvulsant potential in the subcutaneous pentylenetetrazol (sc Ptz) test in mice. These compounds were synthesized and characterized by TLC followed by IR and H1NMR. In vivo screening data acquired indicate that most of analogs have the ability to protect against PTZ-induced seizure. Phenytoin (PHT) was employed as the reference p...
[ 6 ] - Design, Synthesis and Anti-Tubercular Activity of Novel 1, 4-Dihydropyrine-3, 5-Dicarboxamide Containing 4(5)-Chloro-2-Ethyl-5(4)-Imidazolyl Moiety
Current researches have showed that N3, N5-diaryl-2, 6-dimethyl -1, 4-dihydropyrine-3, 5- dicarboxamide analogues demonstrate notable anti-tubercular activity. In this study, Hantzsch condensation was used to design and synthesize new analogues of dihydropyridine (DHP). Different diary carboxamides were inserted at positions 3 and 5 of the DHP ring. 4(5)-chloro-2-ethyl-5(4)-imidazolyl moiety wa...
[ 7 ] - 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 (...
[ 8 ] - Computational Study of Quinolone Derivatives to Improve their Therapeutic Index as Anti-malaria Agents: QSAR and QSTR
Malaria is a parasitic disease with limited chemotherapy options. Chemotherapy options are limited; moreover, drug resistant frequently occurs. The speed of drug development should be faster to overcome the emerging drug resistance. In the current study, a series of quinolone derivatives were subjected to quantitative structure activity relationship to identify the ideal physicochemical charact...
[ 9 ] - Design and Synthesis of 4-flurophthalimides as potential anticonvulsant agents
Objective(s): Anticonvulsant activity of phthalimide was discovered in 2000 by molecular hybridization of thalidomide and ameltolide. In our previous research we have reported some new 4-substituted derivatives of phthalimide with good activity against the tonic and clonic seizures Material and Methods: A series of novel 4-flurophthalimides that designed using bioisosteric replacement were synt...
[ 10 ] - Docking Studies, Synthesis, and In-vitro Evaluation of Novel Oximes Based on Nitrones as Reactivators of Inhibited Acetylcholinesterase
Acetylcholinesterase has important role in synaptic cleft. It breaks down the acetylcholineatcholinergic synapsesand terminates the cholinergic effects. Some chemical agents likeorganophosphorus compounds (OPCs) including nerve agents and pesticides react withacetylcholinesteraseirreversibly. They inhibit normal biological enzyme action and resultin accumulation of acetylcholineand show toxic e...
[ 11 ] - Docking, Synthesis and anticonvulsant activity of N-substituted isoindoline-1,3-dione
A series of compounds related to ameltolide were studied for anticonvulsant potential in the subcutaneous pentylenetetrazol (sc Ptz) test in mice. These compounds were synthesized and characterized by TLC followed by IR and H1NMR. In vivo screening data acquired indicate that most of analogs have the ability to protect against PTZ-induced seizure. Phenytoin (PHT) was employed as the reference p...
[ 12 ] - Design, Synthesis and Anti-Tubercular Activity of Novel 1, 4-Dihydropyrine-3, 5-Dicarboxamide Containing 4(5)-Chloro-2-Ethyl-5(4)-Imidazolyl Moiety
Current researches have showed that N3, N5-diaryl-2, 6-dimethyl -1, 4-dihydropyrine-3, 5- dicarboxamide analogues demonstrate notable anti-tubercular activity. In this study, Hantzsch condensation was used to design and synthesize new analogues of dihydropyridine (DHP). Different diary carboxamides were inserted at positions 3 and 5 of the DHP ring. 4(5)-chloro-2-ethyl-5(4)-imidazolyl moiety wa...
[ 13 ] - 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 (...
[ 14 ] - Computational Study of Quinolone Derivatives to Improve their Therapeutic Index as Anti-malaria Agents: QSAR and QSTR
Malaria is a parasitic disease with limited chemotherapy options. Chemotherapy options are limited; moreover, drug resistant frequently occurs. The speed of drug development should be faster to overcome the emerging drug resistance. In the current study, a series of quinolone derivatives were subjected to quantitative structure activity relationship to identify the ideal physicochemical charact...
[ 15 ] - طراحی و داکینگ اکسیمهای جدید بهعنوان فعالسازهای استیلکولیناستراز مهارشده با عوامل عصبی
زمینه و هدف: در این مطالعه یک گروه از اکسیم های بر پایه نایترون دارای بخش پیریدینیوم، به عنوان کاندیدهای دارویی جدید در فعالسازی استیل کولین استراز (AChE) مهار شده، با مطالعات داکینگ معرفی شدهاند. روشها: ساختار شیمیایی فعالسازهای جدید با استفاده از برنامه هایپرکم ساخته شدند و مطالعات کانفورماسیونی از طریق روش نیمه تجربی انجام گردید. در محاسبات داکینگ اکسیم های طراحی شده از برنامه AutoDo...
[ 16 ] - بررسی اثر ضدقارچی عصاره های آبی و الکلی گیاه بادرنجبویه روی کاندیدا آلبیکنس، کاندیدا گلابراتا و کاندیدا کروزویی
زمینه و هدف: عفونت های قارچی خصوصا گونه های کاندیدا شایعترین عفونت های فرصت طلب می باشند و درمان با داروهای شیمیایی دارای عوارض بسیاری است. امروزه گیاه بادرنجبویه (Melissa Officinalis) به لحاظ دارا بودن خواص ضدمیکروبی مورد توجه قرار گرفته است. هدف از این بررسی مقایسه اثر بخشی این گیاه بر روی گونه های کاندیدا آلبیکنس، گلابراتا و کروزوئی میباشد. روشها: در این مطالعه آزمایشگاهی، عصاره های آبی و ا...
[ 17 ] - مطالعات داکینگ و QSAR بر روی گروهی از مشتقات تریآزول بهمنظور دستیابی به عوامل ضد قارچ قویتر و مؤثرتر
اهداف: در این مطالعه، بر روی یک دسته از مشتقات تریآزول با اثر مهارکنندگی آنزیم CYP51 مطالعات داکینگ و به دنبال آن آنالیز رابطه فعالیت و ساختار کمی (QSAR) انجام گرفت. روشها: با استفاده از برنامهی Hyperchem ساختار مولکولی آزولهای طراحیشده ساخته شد. برای انجام مطالعات داکینگ از برنامه AutoDock استفاده شد. در مطالعات QSAR، توصیفگرهای مختلفی محاسبه گردیدند. یافتهها: بر اساس نتایج بهدستآمده ...
[ 18 ] - راهبردهای افزایش نفوذ در دارورسانی پوستی
Transdermal drug delivery (TDD) is a non-invasive, topical administration method for therapeutic agents. Transdermal delivery also has advantages including providing release for long periods of time, improving patient compliance, and generally being inexpensive. Despite these advantages, the use of TDD has been limited by innate barrier functions of the skin. Only small (<500 Da), lipophilic mo...
[ 19 ] - Design and Docking Study of Some Pyrimidine derivatives as Antimalarial Agents
Background and Aim: According to the latest estimate published by the World Health Organization in 2017, there are 219 million malaria cases and 435,000 deaths. With the emergence of drug-resistant strains in malaria, there is a need for new drug targets every time. In this study, the design and docking study of the pyrimidine derivatives for inhibiting Methionine aminopeptidase1B enzyme (Metap...
[ 20 ] - The Effect of Descurainia Sophia Seed Extract on Nephrotoxicity Markers Induced by Acetaminophen in Mice
Background & Objective: Acetaminophen is known as the most common agent which causes hepatic and renal toxicity in human and experimental animals at supra-therapeutic doses. The current study investigated the protective effects of Descurainia sophia seed extract on the acetaminophen-induced nephrotoxicity markers in male mice. Materials & Methods: Experimental male mice (n=60, Swiss alb...
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