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Articles by Mohamed M. Abdalla
Total Records ( 7 ) for Mohamed M. Abdalla
  Suzan Khayyat , Abd El-Galil E. Amr , Osama I. Abd El- Salam , Mohamed A. Al-Omar and Mohamed M. Abdalla
  A series of bis-schiff base candidates 5a-l, 6a-c and 7a-c were synthesized by using N2, N2`-(pyridine-3,5-dicarbonyl)-di-L-lucylhydrazide (4) as starting material which was synthesized from 3,5-pyridinedicarboxylic acid (1) and screening for their analgesic and anti-inflammatory. Bis-ester 3 was prepared from 3,5-pyridinedi-carboxylic acid 1 and L-lucine methyl ester, which was hydrazonolysis with hydrazine hydrate afforded compounds 4. Treatment of acid hydrazide 4 with aromatic aldehydes afforded the corresponding bis-dipeptide Schiff bases 5a-l, respectively. Compounds 6a-c and 7a-c were synthesized by reacting of hydrazide 4 with cycloalkanone and acetyl pyridine derivatives. Some of the newly synthesized compounds exhibited better analgesic and anti-inflammatory activities than the reference controls. The structures of newly synthesized compounds were confirmed by IR, NMR, MS spectral data and elemental analysis. The detailed synthesis, spectroscopic data, pharmacological activities of the synthesized compounds was reported.
  Said A. Said , Abd El-Galil E. Amr , Hassan A. El- Sayed , Mohamed A. Al- Omar and Mohamed M. Abdalla
  Some of synthesized heterocyclic pyrimidine, pyrimidine, furopyridine derivatives and their nucleoside candidates (2-14) were previously prepared and were founded to have some aspects of structural similarity with many anti-inflammatory agents. Therefore, these agents were screened for this property. The evaluation of the anti-inflammatory activities was based on evaluation of the abilities of these compounds in protection against carrageenan-induced edema. The anti-inflammatory activities of the tested compounds further confirmed based on evaluation of the abilities of these compounds to inhibit plasma PGE2. These compounds showed potent anti-inflammatory activity with low toxicity (LD50) comparable to Valdicoxib® as reference anti-inflammatory drugs.
  Said A. Said , Hassan A. El-Sayed , Abd El-Galil E. Amr and Mohamed M. Abdalla
  A series of the newly substituted thienopyrimidine derivatives 2-13 were synthesized by using 3-amino-6-(4-chlorophenyl)-4-(4-isopropylphenyl) thieno[2,3-b]pyridine-2-carbohydrazide 1 as starting material. Reaction of compound 1 with p-nitrobenzaldehyde in refluxing ethanol afforded the corresponding Shiff base 2, which was cyclized with triethyl orthoformate to give thienopyrimidine derivative 3. Compound 1 was treated with formic acid or acetic anhydride to afford the corresponding thienopyrimidines 4 and 5, respectively. Treatment of 1 with acetylacetone afforded pyrazolothienopyrimidine 6. Treatment of 1 with triethyl orthoformate, carbon disulfide, dimethylformamide and ethyl acetoacetate or diethyl malonate gave compounds 7-11, respectively. Cyclization of 1 with m-nitrophthalic anhydride or formaldehyde afforded thienopyrimidines 12 and 13, respectively. The newly synthesized compounds were found to be potent selective and orally bioavailable CHK1 inhibitors. This elucidated and confirmed via determination of checkpoint abrogation, antiproliferative activity and potentiation of genotoxic drug efficacy in cancer cell lines and also determination of compound concentrations in vivo at selected time points following i.v. and oral dosing.
  Abd El-Galil E. Amr , Mohamed A. Al- Omar and Mohamed M. Abdalla
  Here the report antiulcer activity of some 2,6-bis substituted pyrimidothienopyridine (1-9). Eighteen pyrimidothienopyridine derivatives were synthesized and screened as analgesic, anticonvulsant and antiparkinsonian agent before. Many pyrimidines derivatives were synthesized and showed wide diversity of excellent biological activities, the most interesting one amongest these activities the antiulcer activates. It was proven that the antiulcer activities of many pyrimidines derivatives were due to their proton Pump Inhibitor Activities (PPI). Herein and due to structure similarity between the compounds in study and some pyrimidines derivatives showed potent antiulcer activities, the antiulcer activities of these compounds were evaluated using pyloric ligation ulcer model. All the tested compounds showed potent antiulcerogenic activities and the potency descending order was 6b, 6a, 5b, 5a, 7b, 7a, 9b, 9a, 8b, 8a, 2b, 2a, 3b, 3a, 4b, 4a, 1b and 1a. To specify the accurate mechanism of antiulcer activity, many animal models were used the only one that give fruit results was H+/K+-ATPase inhibition in membrane vesicles of stomach mucosa that proved all antiulcer activities of the tested compounds accomplished via H+/K+-ATPase (proton pump) inhibition activities.
  Abd El-Galil E Amr , Mohamed A. Al- Omar and Mohamed M. Abdalla
  A series of chiral linear and macrocyclic bridged pyridines (1-8) has been prepared starting from pyridine-2,6-dicarbonyl dichloride and they screened as antimicrobial agents before. Screening of the compounds for their Inhibition of type A and type B monoamine oxidase activities in mitochondria preparation revealed that the tested compounds showed selective inhibition of type A monoamine oxidase activities in the following order 4a, 6, 5a, 3, 4b, 5b, 1, 4c, 7, 8 and 2, this confirmed by the in vivo tryptamine seizure potentiation model in rats. The tested compounds showed in vivo good pharmacokinetic and pharmacodynamic profiles.
  Abd El-Galil E Amr , Mohamed A. Al- Omar and Mohamed M. Abdalla
  A series of synthesized 2,6-bis(tetracarboxamide)-pyridine and macrocyclic tripeptide derivatives 1-6 were previously prepared and screened as antimicrobial, anti-inflammatory and anticancer agents. The compounds for evaluation of analgesic, anticonvulsant and antiparkinsonian activities were used. Analgesic activities of selected compounds determined by hot plate assay, all tested compounds showed this property. Anticonvulsant activities of selected compounds measured their abilities to antagonize yohimbine-induced clonic seizure, all tested compounds showed this property. The antiparkinsonian activity measured by the ability of compounds to protect animals against the parkinsonian like signs induced by agonists, all tested compounds showed this property. All tested compounds showed analgesic, antipakinsonian and anticonvulsant activities and the order for these activities were 5b, 6a, 3, 5a, 5c, 4, 6c, 2, 6b and 1.
  Abd El-Galil E. Amr , Mohamed A. Al-Omar and Mohamed M. Abdalla
  Ten pyridine and pyrimidine and thiazolopyrimidine derivatives (1-10) were synthesized and screened as analgesic, anticonvulsant and antiparkinsonian agent beforeTen pyridine and pyrimidine and thiazolopyrimidine derivatives (1-10) were synthesized and screened as analgesic, anticonvulsant and antiparkinsonian agent before. Herein, all the target compounds showed anti-inflammatory activity. The active compounds showed selective inhibitory activity towards COX-2 enzyme as revealed by the in vitro enzymatic assay. All the tested compounds proved to have superior gastrointestinal (GI) safety profiles as compared to indomethacin, when tested for their ulcerogenic effects.

 
 
 
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