Amr Sonousi
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View article: Combating oxi-inflamm-aging: Passerini adducts tethered with 1,2,3-triazoles for enhanced antioxidant defense and 5-LOX inhibition
Combating oxi-inflamm-aging: Passerini adducts tethered with 1,2,3-triazoles for enhanced antioxidant defense and 5-LOX inhibition Open
Design and synthesis of novel hybrids of Passerini adducts tethered with 1,2,3-triazoles as promising dual anti-inflammatory and antioxidant agents.
View article: Impact of trifluoromethyl Ugi adducts as anticancer agents: EGFR inhibition, apoptosis induction and miRNA up-regulation
Impact of trifluoromethyl Ugi adducts as anticancer agents: EGFR inhibition, apoptosis induction and miRNA up-regulation Open
A series of novel bis-amide Ugi adducts with a Y-shaped configuration imitating the thematic feature of fourth-generation EGFR inhibitors was designed and synthesized with potent cytotoxicity against breast and lung cancer cells.
View article: Novel sulfonamide derivatives as multitarget antidiabetic agents: design, synthesis, and biological evaluation
Novel sulfonamide derivatives as multitarget antidiabetic agents: design, synthesis, and biological evaluation Open
A series of new sulfonamide derivatives connected through an imine linker to five or seven membered heterocycles were designed and synthesized.
View article: Design, synthesis, and biological evaluation of novel thiazole derivatives as PI3K/mTOR dual inhibitors
Design, synthesis, and biological evaluation of novel thiazole derivatives as PI3K/mTOR dual inhibitors Open
A series of new thiazole derivatives 3a–q were synthesized and tested against 60 cancer cell lines at the NCI, USA. Compound 3b showed the highest activity against PI3Kα with IC 50 = 0.086 ± 0.005 μM and IC 50 of 0.221 ± 0.014 μM against m…
View article: Design, synthesis, and biological evaluation of 1,2,4-oxadiazole-based derivatives as multitarget anti-Alzheimer agents
Design, synthesis, and biological evaluation of 1,2,4-oxadiazole-based derivatives as multitarget anti-Alzheimer agents Open
A series of novel 1,2,4-oxadiazole-based derivatives were synthesized and evaluated for their potential anti-Alzheimer disease activity.
View article: Novel sofosbuvir derivatives against SARS-CoV-2 RNA-dependent RNA polymerase: an in silico perspective
Novel sofosbuvir derivatives against SARS-CoV-2 RNA-dependent RNA polymerase: an in silico perspective Open
The human coronavirus, SARS-CoV-2, had a negative impact on both the economy and human health, and the emerging resistant variants are an ongoing threat. One essential protein to target to prevent virus replication is the viral RNA-depende…
View article: Design, synthesis, anticancer, and antibacterial evaluation of some quinazolinone‐based derivatives as DHFR inhibitors
Design, synthesis, anticancer, and antibacterial evaluation of some quinazolinone‐based derivatives as DHFR inhibitors Open
Two series of quinazolinone derivatives were designed and synthesized as dihydrofolate reductase (DHFR) inhibitors. All compounds were evaluated for their antibacterial and antitumor activities. Antibacterial activity was evaluated against…
View article: Design and synthesis of novel quinazolinone-based derivatives as EGFR inhibitors with antitumor activity
Design and synthesis of novel quinazolinone-based derivatives as EGFR inhibitors with antitumor activity Open
Nineteen new quinazolin-4(3H)-one derivatives 3a–g and 6a–l were designed and synthesised to inhibit EGFR. The antiproliferative activity of the synthesised compounds was tested in vitro against 60 different human cell lines. The most pote…
View article: Structure‐Activity Relationships for 5′′ Modifications of 4,5‐Aminoglycoside Antibiotics
Structure‐Activity Relationships for 5′′ Modifications of 4,5‐Aminoglycoside Antibiotics Open
Modification at the 5’’‐position of 4,5‐disubstituted aminoglycoside antibiotics (AGAs) to circumvent inactivation by aminoglycoside modifying enzymes (AMEs) is well known. Such modifications, however, unpredictably impact activity and aff…
View article: An Advanced Apralog with Increased in vitro and in vivo Activity toward Gram‐negative Pathogens and Reduced ex vivo Cochleotoxicity
An Advanced Apralog with Increased in vitro and in vivo Activity toward Gram‐negative Pathogens and Reduced ex vivo Cochleotoxicity Open
We describe the convergent synthesis of a 5‐ O ‐β‐D‐ribofuranosyl‐based apramycin derivative (apralog) that displays significantly improved antibacterial activity over the parent apramycin against wild‐type ESKAPE pathogens. In addition, t…
View article: Synthesis of a Pseudodisaccharide Suitable for Synthesis of Ring I Modified 4,5-2-Deoxystreptamine Type Aminoglycoside Antibiotics
Synthesis of a Pseudodisaccharide Suitable for Synthesis of Ring I Modified 4,5-2-Deoxystreptamine Type Aminoglycoside Antibiotics Open
To facilitate the synthesis of paromomycin and/or neomycin analogues, we describe a cleavage of ring I from paromomycin that proceeds in the presence of azides and affords a glycosyl acceptor for the installation of a modified ring I. A pa…
View article: Apralogs: Apramycin 5-<i>O</i>-Glycosides and Ethers with Improved Antibacterial Activity and Ribosomal Selectivity and Reduced Susceptibility to the Aminoacyltransferase (3)-IV Resistance Determinant
Apralogs: Apramycin 5-<i>O</i>-Glycosides and Ethers with Improved Antibacterial Activity and Ribosomal Selectivity and Reduced Susceptibility to the Aminoacyltransferase (3)-IV Resistance Determinant Open
Apramycin is a structurally unique member of the 2-deoxystreptamine class of aminoglycoside antibiotics characterized by a monosubstituted 2-deoxystreptamine ring that carries an unusual bicyclic eight-carbon dialdose moiety. Because of it…
View article: Synthesis, ribosomal selectivity, and antibacterial activity of netilmicin 4′-derivatives
Synthesis, ribosomal selectivity, and antibacterial activity of netilmicin 4′-derivatives Open
We describe the synthesis and evaluation of 4′-subsituted netilmicin derivatives by selective functionalization at the 4′-position of the endocyclic enolether function.
View article: Synthesis of Netilmicin and Apramycin Derivatives for the Treatment of Multidrug-Resistant Infectious Diseases
Synthesis of Netilmicin and Apramycin Derivatives for the Treatment of Multidrug-Resistant Infectious Diseases Open
The ever-growing bacterial resistance to existing antibiotics is alarming to humanity. Many researchers decided to revisit aminoglycosides with renewed emphasis on chemical modification as they have long been used as highly potent antibiot…
View article: Selective Protection of Secondary Amines as the <i>N</i>-Phenyltriazenes. Application to Aminoglycoside Antibiotics
Selective Protection of Secondary Amines as the <i>N</i>-Phenyltriazenes. Application to Aminoglycoside Antibiotics Open
Selective protection of secondary amines as triazenes in the presence of multiple primary amines is demonstrated, with subsequent protection of the primary amines as either azides or carbamates in the same pot. Aminoglycoside antibiotic ex…