An Efficient and Mild Method for the Synthesis and Hydrazinolysis of <i>N</i>‐Glyoxylamino Acid Esters

El‐Faham, Ayman; Marhoon, Zainab Al; Abdel-Megeed, Ahmed; Siddiqui, Mohammed Rafiq H.

doi:10.1155/2013/901745

“…The next day, the solvent was removed under reduced pressure and the crude product was washed with ether under stirring to get the products in the pure state. [22] DesigN, syNthesis aND aNtibacterial stuDy of New ageNts haviNg...…”

Section: Compound 3: Synthesis Of 2-((4-(hydroxymethyl) Phenyl) Aminomentioning

confidence: 99%

Design, Synthesis and Antibacterial Study of New Agents Having 4-Thiazolidinone Pharmacophore

Ismaeel

¹

,

Mahdi

²

,

Razik

³

2019

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A New series of compounds containing 4-thiazolidinone pharmacophore 5(a-d) have been synthesized. The chemical structure of the intermediate and final compounds was characterized and confirmed by using FT-IR and 1 H-NMR spectroscopy. All final compounds were tested against gram-positive and gram-negative bacteria using a well-diffusion technique for their ability as antimicrobial agents. The tested compounds 5b and 5c showed comparable antibacterial activity against gram-negative bacteria and gram-positive bacteria like escherichia coli, Acinetobacter bumannii, Staphylococcus aureus, and Streptococcus pyougenes as a standard drug compared with Trimethoprim. Molecular docking simulations were studied to understand the molecular core. The results were achieved by docking, the most active compounds into the active site of protein of the bacteria which completely accorded with in vitro results.

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“…This mixture refluxed for three hours. Then the reaction mixture was cooled, the solid obtained was filtered and recrystallized from ethanol [12] .…”

Section: General Procedures For the Synthesis Of Benzoimidazole Acety...mentioning

confidence: 99%

Design, Synthesis, and Acute Anti-inflammatory Assessment of New 2-methyl Benzoimidazole Derivatives Having 4-Thiazolidinone Nucleus

Adnan,

Mahdi,

Khan

2019

AJPS

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New two derivatives of 2- methyl benzoimidazole were designed, synthesized and evaluated as a potential cyclooxygenase-2 [COX-2] inhibitors. The synthesized compounds have been recognized according to their spectral FT-IR, 1H-NMR data and physical pro- perties. The newly synthesized compounds were investigated in vivo for their anti-inflammatory activities using egg-white stimulated paw edema method with respect to the effect of propylene glycol 50%v/v [control group] and the ibuprofen [10mg/kg i.p.] was selected as a reference ligand. New compounds showed a significantly higher in vivo anti-inflammatory activity compared with ibuprofen as a reference drug. COX-2 selectivity evaluation through molecular docking via GOLD suite [v. 5.6.2.]. The new compounds via molecular docking showed significant higher activities when compared with ibuprofen as referenced drugs because of having hydrogen bonding interaction toward the key amino acids within COX-2 structure and all these results were compatible with the study of in vivo acute anti-inflammatory activities for tested compounds. ADME studies were performed to predict absorption, bioavailability, topological polar surface area, and drug-likeness. The results of ADME studies showed that all synthesized compounds absorbed from the gastrointestinal tract.

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“…This mixture refluxed for three hours. Then the reaction mixture was cooled, the solid obtained was filtered and recrystallized from ethanol [12] . [2][3] drops of glacial acetic acid were added.…”

Section: Generalmentioning

confidence: 99%

Design, Synthesis, and Acute Anti-inflammatory Assessment of New 2-methyl Benzoimidazole Derivatives Having 4-Thiazolidinone Nucleus

Adnan

¹

,

Mahdi

²

,

Khan

³

2019

AJPS

1

0

View full text Add to dashboard Cite

New two derivatives of 2- methyl benzoimidazole were designed, synthesized and evaluated as a potential cyclooxygenase-2 [COX-2] inhibitors. The synthesized compounds have been recognized according to their spectral FT-IR, 1H-NMR data and physical pro- perties. The newly synthesized compounds were investigated in vivo for their anti-inflammatory activities using egg-white stimulated paw edema method with respect to the effect of propylene glycol 50%v/v [control group] and the ibuprofen [10mg/kg i.p.] was selected as a reference ligand. New compounds showed a significantly higher in vivo anti-inflammatory activity compared with ibuprofen as a reference drug. COX-2 selectivity evaluation through molecular docking via GOLD suite [v. 5.6.2.]. The new compounds via molecular docking showed significant higher activities when compared with ibuprofen as referenced drugs because of having hydrogen bonding interaction toward the key amino acids within COX-2 structure and all these results were compatible with the study of in vivo acute anti-inflammatory activities for tested compounds. ADME studies were performed to predict absorption, bioavailability, topological polar surface area, and drug-likeness. The results of ADME studies showed that all synthesized compounds absorbed from the gastrointestinal tract.

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An Efficient and Mild Method for the Synthesis and Hydrazinolysis of N‐Glyoxylamino Acid Esters

Cited by 9 publications

References 46 publications

Design, Synthesis and Antibacterial Study of New Agents Having 4-Thiazolidinone Pharmacophore

Design, Synthesis and Antibacterial Study of New Agents Having 4-Thiazolidinone Pharmacophore

Design, Synthesis, and Acute Anti-inflammatory Assessment of New 2-methyl Benzoimidazole Derivatives Having 4-Thiazolidinone Nucleus

Design, Synthesis, and Acute Anti-inflammatory Assessment of New 2-methyl Benzoimidazole Derivatives Having 4-Thiazolidinone Nucleus

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