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Author Tamer M Ibrahim

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Investigation of the anti-inflammatory and analgesic activities of promising pyrazole derivative.

Adnan A Bekhit, Sherry N Nasralla, Eman J El-Agroudy, Nahla Hamouda, Ahmed Abd El-Fattah, Salma A Bekhit, Kikuko Amagase, Tamer M Ibrahim,

The development of new COX-2 inhibitors with analgesic and anti-inflammatory efficacy as well as minimal gastrointestinal, renal and cardiovascular toxicity, is of vital importance to patients suffering from chronic course pain and inflammatory conditions. This study aims at evaluating the therapeutic activity and adverse drug reactions associated with the use ... Read more >>

Eur J Pharm Sci (European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences)
[2022, 168:106080]

Cited: 0 times

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Development of Novel Quinoline-Based Sulfonamides as Selective Cancer-Associated Carbonic Anhydrase Isoform IX Inhibitors.

Moataz Shaldam, Alessio Nocentini, Zainab M Elsayed, Tamer M Ibrahim, Rofaida Salem, Ramadan A El-Domany, Clemente Capasso, Claudiu T Supuran, Wagdy M Eldehna,

A new series of quinoline-based benzenesulfonamides (<b>QBS</b>) were developed as potential carbonic anhydrase inhibitors (CAIs). The target <b>QBS</b> CAIs is based on the 4-anilinoquinoline scaffold where the primary sulphonamide functionality was grafted at C4 of the anilino moiety as a zinc anchoring group (<b>QBS</b>&nbsp;<b>13a</b>-<b>c</b>); thereafter, the sulphonamide group was switched ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2021, 22(20):]

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Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors.

Moataz Shaldam, Wagdy M Eldehna, Alessio Nocentini, Zainab M Elsayed, Tamer M Ibrahim, Rofaida Salem, Ramadan A El-Domany, Clemente Capasso, Hatem A Abdel-Aziz, Claudiu T Supuran,

In the present study, we describe the design of different series of benzofuran-based derivatives as potential carbonic anhydrase inhibitors (CAIs). The adopted design is based on bioisosteric replacement for the p-fluorophenyl SLC-0111 tail with the lipophilic 2-methylbenzofuran or 5-bromobenzofuran tails to furnish the 2-methylbenzofuran (MBF) sulfonamides (MBFS; 9, 11 and ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2021, 216:113283]

Cited: 4 times

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Design, synthesis, biological evaluation and in silico studies of certain aryl sulfonyl hydrazones conjugated with 1,3-diaryl pyrazoles as potent metallo-β-lactamase inhibitors.

Marwa M Shaaban, Hanan M Ragab, Kenichi Akaji, Ross P McGeary, Alaa-Eldin A Bekhit, Waleed M Hussein, Julia L Kurz, Bassma H Elwakil, Salma A Bekhit, Tamer M Ibrahim, Mona A Mahran, Adnan A Bekhit,

Based on a structure-guided approach, aryl sulfonyl hydrazones conjugated with 1,3-diaryl pyrazoles were designed to target metallo-β-lactamases (MBLs), using Klebsiella pneumoniaeNDM-1 as a model. The in vitro MBLs inhibition showed remarkable inhibition constant for most of the designed compounds at a low micromolar range (1.5-16.4 µM) against NDM-1, IMP-1 and AIM-1 ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2020, 105:104386]

Cited: 1 time

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Synthesis, biological evaluation and modeling of hybrids from tetrahydro-1H-pyrazolo[3,4-b]quinolines as dual cholinestrase and COX-2 inhibitors.

Mohamed Mroueh, Wissam H Faour, Wassim N Shebaby, Costantine F Daher, Tamer M Ibrahim, Hanan M Ragab,

New tetrahydro-1H-pyrazolo[3,4-b]quinoline derivatives were designed, synthesized and characterized as dual anticholinestrase and cyclooxygenase-2 inhibitors. The in vitro and in vivo anti-cholinesterase evaluation exhibited promising activities with lower hepatotoxicity for many candidates compared to tacrine as a reference. Furthermore, their anti-inflammatory activity using in vitro (COX-1/COX-2) inhibitory assay demonstrated superior activity ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2020, 100:103895]

Cited: 2 times

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New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors.

Tamer Nasr, Samir Bondock, Tamer M Ibrahim, Walid Fayad, Ahmed B Ibrahim, Neveen A AbdelAziz, Tamer M Sakr,

New functionalized acrylamide derivatives bearing sulfisoxazole moiety were designed to target bacterial dihydropteroate synthase (DHPS). The in vitro antimicrobial activities of these compounds were assessed. The E-configuration of compound 5b was proved by single crystal X-ray analysis. Compounds 5g and 5h displayed double the activity of ampicillin against B. subtilis. ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2020, 28(9):115444]

Cited: 0 times

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Design and synthesis of phthalazine-based compounds as potent anticancer agents with potential antiangiogenic activity via VEGFR-2 inhibition.

Salwa Elmeligie, Asmaa M Aboul-Magd, Deena S Lasheen, Tamer M Ibrahim, Tamer M Abdelghany, Sohair M Khojah, Khaled A M Abouzid,

In the designed compounds, either a biarylamide or biarylurea moiety or an N-substituted piperazine motif was linked to position 1 of the phthalazine core. The anti-proliferative activity of the synthesised compounds revealed that eight compounds (<b>6b, 6e, 7b, 13a, 13c, 16a, 16d and 17a</b>) exhibited excellent broad spectrum cytotoxic activity ... Read more >>

J Enzyme Inhib Med Chem (Journal of enzyme inhibition and medicinal chemistry)
[2019, 34(1):1347-1367]

Cited: 1 time

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Synthesis, in vitro biological evaluation and in silico studies of certain arylnicotinic acids conjugated with aryl (thio)semicarbazides as a novel class of anti-leishmanial agents.

Wagdy M Eldehna, Hadia Almahli, Tamer M Ibrahim, Mohamed Fares, Tarfah Al-Warhi, Frank M Boeckler, Adnan A Bekhit, Hatem A Abdel-Aziz,

Herein we introduce new compounds as conjugates of arylnicotinic acids with aryl (thio)semicarbazide derivatives. Based on a structure-guided approach, they were designed to possess anti-leishmanial activity through anti-folate mechanism, via targeting Leishmania major pteridine reductase 1 (Lm-PTR1). The in vitro anti-promastigote and anti-amastigote activity were promising for many thiosemicarbazide derivatives and ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 179:335-346]

Cited: 2 times

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Synthesis, modeling and biological evaluation of some pyrazolo[3,4-d]pyrimidinones and pyrazolo[4,3-e][1,2,4]triazolo[4,3-a]pyrimidinones as anti-inflammatory agents.

Gina N Tageldin, Tamer M Ibrahim, Salwa M Fahmy, Hayam M Ashour, Mounir A Khalil, Rasha A Nassra, Ibrahim M Labouta,

New pyrazolo[3,4-d]pyrimidinone and pyrazolo[4,3-e][1,2,4]triazolo[4,3-a]pyrimidinone derivatives were synthesized. They have been evaluated for their anti-inflammatory activity using in vitro (COX-1/COX-2) inhibitory assay. Moreover, compounds with promising in vitro activity and COX-1/COX-2 selectivity indices were subjected for in vivo anti-inflammatory testing using formalin induced paw edema and cotton-pellet induced granuloma assays for ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2019, 90:102844]

Cited: 2 times

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Shooting three inflammatory targets with a single bullet: Novel multi-targeting anti-inflammatory glitazones.

Perihan A Elzahhar, Rana Alaaeddine, Tamer M Ibrahim, Rasha Nassra, Azza Ismail, Benjamin S K Chua, Rebecca L Frkic, John B Bruning, Nadja Wallner, Tilo Knape, Andreas von Knethen, Hala Labib, Ahmed F El-Yazbi, Ahmed S F Belal,

In search for effective multi-targeting drug ligands (MTDLs) to address low-grade inflammatory changes of metabolic disorders, we rationally designed some novel glitazones-like compounds. This was achieved by incorporating prominent pharmacophoric motifs from previously reported COX-2, 15-LOX and PPARγ ligands. Challenging our design with pre-synthetic docking experiments on PPARγ showed encouraging ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 167:562-582]

Cited: 6 times

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Leishmania treatment and prevention: Natural and synthesized drugs.

Adnan A Bekhit, Eman El-Agroudy, Aliaa Helmy, Tamer M Ibrahim, Amin Shavandi, Alaa El-Din A Bekhit,

Leishmaniasis affects over 150 million people all over the world, especially in subtropical regions. Currently used antileishmanial synthesized drugs are associated with some drawbacks such as resistance and cytotoxicity, which hamper the chances of treatment. Furthermore, effective leishmanial vaccines are not well developed. Promising chemotherapy, either from natural or synthetic ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2018, 160:229-244]

Cited: 9 times

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Synthesis, in silico experiments and biological evaluation of 1,3,4-trisubstituted pyrazole derivatives as antimalarial agents.

Adnan A Bekhit, Manal N Saudi, Ahmed M M Hassan, Salwa M Fahmy, Tamer M Ibrahim, Doaa Ghareeb, Aya M El-Seidy, Sherry N Nasralla, Alaa El-Din A Bekhit,

New 1,3,4-trisubstituted pyrazole derivatives were synthesized and evaluated for their antiplasmodial activity. Compounds 4b, 4c, 7a and 7d were the most potent antiplasmodial agents against P. berghei with percent of suppression ranging from 90 to 100%. They were also screened for their in vitro antimalarial activity against the chloroquine resistant strain P. falciparum, ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2019, 163:353-366]

Cited: 4 times

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Synthesis, molecular modeling and biological screening of some pyrazole derivatives as antileishmanial agents.

Adnan A Bekhit, Manal N Saudi, Ahmed Mm Hassan, Salwa M Fahmy, Tamer M Ibrahim, Doaa Ghareeb, Aya M El-Seidy, Sayed M Al-Qallaf, Huda J Habib, Alaa El-Din A Bekhit,

<h4>Aim</h4>Novel open chain and cyclized derivatives containing pyrazole scaffold were designed, synthesized and evaluated as antileishmanial compounds. Methodology & results: In silico reverse docking experiment suggested Leishmania major pteridine reductase (Lm-PTR1) as a putative target for the synthesized compounds. In vitro antileishmanial screening against L. major promastigotes and amastigotes using miltefosine ... Read more >>

Future Med Chem (Future medicinal chemistry)
[2018, 10(19):2325-2344]

Cited: 1 time

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Synthesis, anti-inflammatory screening, molecular docking, and COX-1,2/-5-LOX inhibition profile of some novel quinoline derivatives.

Ibrahim Chaaban, Ola H Rizk, Tamer M Ibrahim, Shery S Henen, El-Sayeda M El-Khawass, Aida E Bayad, Ibrahim M El-Ashmawy, Hisham A Nematalla,

New quinoline compounds comprising pyrazole scaffold through different amide linkages were synthesized. The synthesized compounds were evaluated for their anti-inflammatory activity. Eight compounds (5c, 11b,c, 12c, 14a,b, 20a and 21a) were found to exhibit promising anti-inflammatory profiles in acute and sub-acute inflammatory models. They were screened for their ulcerogenic activity ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2018, 78:220-235]

Cited: 3 times

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Synthesis, biological evaluation and molecular modeling of novel thienopyrimidinone and triazolothienopyrimidinone derivatives as dual anti-inflammatory antimicrobial agents.

Adnan A Bekhit, Ahmed M Farghaly, Ragab M Shafik, Mona M A Elsemary, Alaa El-Din A Bekhit, Aida A Guemei, Mai S El-Shoukrofy, Tamer M Ibrahim,

New thienopyrimidinone and triazolothienopyrimidinone derivatives have been synthesized. These compounds were subjected to anti-inflammatory and antimicrobial activity screening aiming to identify new candidates that have dual anti-inflammatory and antimicrobial activities. Compounds 5, 7 and 10a showed minimal ulcerogenic effect and high selectivity towards human recombinant COX-2 over COX-1 enzyme. Their ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2018, 77:38-46]

Cited: 0 times

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Synthesis, evaluation and modeling of some triazolothienopyrimidinones as anti-inflammatory and antimicrobial agents.

Adnan A Bekhit, Ahmed M Farghaly, Ragab M Shafik, Mona Ma Elsemary, Mai S El-Shoukrofy, Alaa El-Din A Bekhit, Tamer M Ibrahim,

<h4>Aim</h4>New triazolotetrahydrobenzothienopyrimidinone derivatives were synthesized.<h4>Experimental</h4>Their structures were confirmed, and their anti-inflammatory, antimicrobial activities and ulcerogenic potentials were evaluated.<h4>Results</h4>Compounds 7a, 10a and 11a showed minimal ulcerogenic effect and high selectivity toward human recombinant COX-2 over COX-1 enzyme with IC<sub>50</sub> values of 1.39, 1.22 and 0.56 μM, respectively. Their docking outcome correlated ... Read more >>

Future Med Chem (Future medicinal chemistry)
[2017, 9(9):881-897]

Cited: 3 times

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Mining ZINC Database to Discover Potential Phosphodiesterase 9 Inhibitors Using Structure-Based Drug Design Approach.

Engi A Hassaan, Sara C Sigler, Tamer M Ibrahim, Kevin J Lee, Lauren K Cichon, Bernard D Gary, Joshua C Canzoneri, Gary A Piazza, Ashraf H Abadi,

In view of the emerging clinical indications for Phosphodiesterase 9 inhibitors e.g. treatment of Alzheimer, diabetes, cancer, and the limited number of its selective inhibitors which possess a single chemical scaffolds, a structure-based approach was undertaken to mine the ZINC database by virtual screening to identify novel PDE9 inhibitors. The ... Read more >>

Med Chem (Medicinal chemistry (Shariqah (United Arab Emirates)))
[2016, 12(5):472-477]

Cited: 1 time

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pROC-Chemotype Plots Enhance the Interpretability of Benchmarking Results in Structure-Based Virtual Screening.

Tamer M Ibrahim, Matthias R Bauer, Alexander Dörr, Erdem Veyisoglu, Frank M Boeckler,

Recently, we have reported a systematic comparison of molecular preparation protocols (using MOE or Maestro) in combination with two docking tools (GOLD or Glide), employing our DEKOIS 2.0 benchmark sets. Herein, we demonstrate how comparable settings of data preparation protocols can affect the profile and AUC of pROC curves based ... Read more >>

J Chem Inf Model (Journal of chemical information and modeling)
[2015, 55(11):2297-2307]

Cited: 4 times

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Applying DEKOIS 2.0 in structure-based virtual screening to probe the impact of preparation procedures and score normalization.

Tamer M Ibrahim, Matthias R Bauer, Frank M Boeckler,

BACKGROUND:Structure-based virtual screening techniques can help to identify new lead structures and complement other screening approaches in drug discovery. Prior to docking, the data (protein crystal structures and ligands) should be prepared with great attention to molecular and chemical details. RESULTS:Using a subset of 18 diverse targets from the recently ... Read more >>

J Cheminform (Journal of cheminformatics)
[2015, 7:21]

Cited: 7 times

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Use of DEKOIS 2.0 to gain insights for virtual screening.

Frank M Boeckler, Matthias R Bauer, Tamer M Ibrahim, Simon M Vogel,

J Cheminform (Journal of cheminformatics)
[2014, 6(Suppl 1):O24]

Cited: 4 times

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Probing the impact of protein and ligand preparation procedures on chemotype enrichment in structure-based virtual screening using DEKOIS 2.0 benchmark sets

Tamer M Ibrahim, Matthias R Bauer, Frank M Boeckler,

J Cheminform (Journal of cheminformatics)
[2014, 6(Suppl 1):P19-P19]

Cited: 0 times

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Evaluation and optimization of virtual screening workflows with DEKOIS 2.0--a public library of challenging docking benchmark sets.

Matthias R Bauer, Tamer M Ibrahim, Simon M Vogel, Frank M Boeckler,

The application of molecular benchmarking sets helps to assess the actual performance of virtual screening (VS) workflows. To improve the efficiency of structure-based VS approaches, the selection and optimization of various parameters can be guided by benchmarking. With the DEKOIS 2.0 library, we aim to further extend and complement the ... Read more >>

J Chem Inf Model (Journal of chemical information and modeling)
[2013, 53(6):1447-1462]

Cited: 37 times

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Design, synthesis and biological evaluation of novel pyridine derivatives as anticancer agents and phosphodiesterase 3 inhibitors.

Ashraf H Abadi, Tamer M Ibrahim, Khaled M Abouzid, Jochen Lehmann, Heather N Tinsley, Bernard D Gary, Gary A Piazza,

Two series of 4,6-diaryl-2-imino-1,2-dihydropyridine-3-carbonitriles and their isosteric 4,6-diaryl-2-oxo-1,2-dihydropyridine-3-carbonitriles were synthesized through a combinatorial approach. The prepared analogues were evaluated for their in vitro capacity to inhibit PDE3A and the growth of the human HT-29 colon adenocarcinoma tumor cell line. Compound 6-(4-bromophenyl)-4-(2-ethoxyphenyl)-2-imino-1,2-dihydropyridine-3-carbonitrile (Id) exhibited the strongest PDE3 inhibition when cGMP but ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2009, 17(16):5974-5982]

Cited: 16 times

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