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Your search keyword '"Amer, Mostafa M."' showing total 15 results
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15 results on '"Amer, Mostafa M."'

2. Prediction of Degradation Profiles for Various Sartans under Solvent-Free Mechanochemical Conditions

Author

Amer, Mostafa M., Backer, Laura, Buschmann, Helmut, Handler, Norbert, Scherf-Clavel, Oliver, Holzgrabe, Ulrike, and Bolm, Carsten

Abstract

For the approval of a drug, the stability data must be submitted to regulatory authorities. Such analyses are often time-consuming and cost-intensive. Forced degradation studies are mainly carried out under harsh conditions in the dissolved state, often leading to extraneous degradation profiles for a solid drug. Oxidative mechanochemical degradation offers the possibility of generating realistic degradation profiles. In this study, a sustainable mechanochemical procedure is presented for the degradation of five active pharmaceutical ingredients (APIs) from the sartan family: losartan potassium, irbesartan, valsartan, olmesartan medoxomil, and telmisartan. High-resolution mass spectrometry enabled the detection of impurities already present in untreated APIs and allowed the elucidation of degradation products. Significant degradation profiles could already be obtained after 15–60 min of ball milling time. Many of the identified degradation products are described in the literature and pharmacopoeias, emphasizing the significance of our results and the applicability of this approach to predict degradation profiles for drugs in the solid state.

Published
2024
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9. Stainless steel-initiated chloro sulfoximidations of allenes under solvent-free conditions in a ball mill.

Author

Deshen Kong, Amer, Mostafa M., and Bolm, Carsten

Subjects
*ALLENE, *BALL mills, *RADICALS (Chemistry), *ADDITION reactions, *SULFOXIMINES, *IODIDES
Abstract

We report mechanochemical regioselective chloro sulfoximidations of allenes through stainless steel-initiated radical addition reactions at ambient temperature under solvent-free conditions. The reactions proceed smoothly with a wide range of substrates and do not require an additional catalyst. The resulting vinyl sulfoximines can further be derivatised. Analogous reactions are observed with arylsulfonyl iodides, which add to allenes as well. [ABSTRACT FROM AUTHOR]

Published
2022
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14. A Copper-Catalyzed Interrupted Domino Reaction for the Synthesis of Fused Triazolyl Benzothiadiazine-1-oxides.

Author

Hommelsheim R, Bausch S, Selvakumar A, Amer MM, Truong KN, Rissanen K, and Bolm C

Abstract

Copper(I)-catalyzed domino reactions of 2-azido sulfoximines with 1-iodoalkynes yield fused triazolyl-containing benzothiadiazine-1-oxides. The protocol features the synthesis of two fused heterocyclic rings in one step with good to excellent yields and a broad functional group tolerance. Detailed mechanistic investigations indicate that a copper π-complex initiates a cycloaddition and oxidative C-N coupling reaction sequence. The results suggest an interrupted domino process involving an iodinated triazole as a key intermediate., (© 2022 The Authors. Chemistry - A European Journal published by Wiley-VCH GmbH.)

Published
2023
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15. Synthesis, DFT calculation, pharmacological evaluation, and catalytic application in the synthesis of diverse pyrano[2,3-c]pyrazole derivatives.

Author

Amer MMK, Abdellattif MH, Mouneir SM, Zordok WA, and Shehab WS

Subjects
Anti-Inflammatory Agents, Non-Steroidal chemical synthesis, Anti-Inflammatory Agents, Non-Steroidal chemistry, Antioxidants chemical synthesis, Antioxidants chemistry, Arachidonate 5-Lipoxygenase metabolism, Catalysis, Cyclooxygenase Inhibitors chemical synthesis, Cyclooxygenase Inhibitors chemistry, Dose-Response Relationship, Drug, Humans, Lipoxygenase Inhibitors chemical synthesis, Lipoxygenase Inhibitors chemistry, Molecular Structure, Oxidative Stress drug effects, Prostaglandin-Endoperoxide Synthases metabolism, Pyrans chemical synthesis, Pyrans chemistry, Pyrans pharmacology, Pyrazoles chemical synthesis, Pyrazoles chemistry, Pyrazoles pharmacology, Reactive Oxygen Species metabolism, Structure-Activity Relationship, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Antioxidants pharmacology, Cyclooxygenase Inhibitors pharmacology, Density Functional Theory, Lipoxygenase Inhibitors pharmacology
Abstract

Pyranopyrazole and its derivatives are classified to be a pharmacologically significant active scaffold for almost all modes of biological activities. In this work, An efficient, green, and facile three-component reaction for preparing pyrano[2,3-c]pyrazole derivatives via the condensation reaction of 5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, ethyl acetoacetate, and malononitrile in the presence of ZnO Nanoparticle. The products are produced with high yields and in shorter reaction times. It also is mild, safe, green, and environmentally friendly. The geometric parameters such as dipole moment, bond length, dihedral angles, total energy, heat of formation, atomic charges and energies at a highly accurate for prepared compounds were computed by Denisty Functional Theory along with the B3LYP functional. The newly synthesized compounds were screened for their anti-inflammatory and antioxidant activity. Some of the tested compounds displayed promising activities. The newly prepared compounds were found to be potent towards the antioxidant activity. Results indicated that compounds 11 and 12 exhibited significant (p ≥ 0.05) in vitro total antioxidant activity as 44.93 ± 0.15 and 39.60 ± 0.10 U/ML, respectively higher than standard ascorbic acid (29.40 ± 0.62)., (Copyright © 2021 Elsevier Inc. All rights reserved.)

Published
2021
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