Alessandra Ammazzalorso

Synthesis, Antibacterial Evaluation, and Chemometric Profiling of a Vanilloid-Based Compounds Library Active Against Helicobacter pylori

Ilaria D’Agostino, Strahinja Z. Kovačević, Moataz Ahmed Shaldam, Alessandra Ammazzalorso et autres

Background: Among natural products, vanillin (Van), a major component of Vanilla planifolia, exhibits multiple bioactivities, including antimicrobial effects. Methods: In this study, Van, its analogues o-vanillin (oVan), iso-vanillin (iVan), ethylvanillin (eVan), and a library of newly synthesized derivatives were evaluated against Helicobacter …

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Synthesis, Biological Evaluation, and Computational Study of Pyridine- and Indazole-Based Inhibitors of the Inducible Nitric Oxide Synthase as Promising Antipsoriatic Agents

Pasquale Amoia, Marialucia Gallorini, Claudia Scarponi, Francisco Franco-Montalbán et autres

High Resolution Image Download MS PowerPoint Slide The dysregulation of inducible nitric oxide synthase (iNOS) is linked to various diseases, including psoriasis, where it contributes to imbalanced nitro-oxidative stress. iNOS is primarily produced in the skin’s epidermal layer and can be activated …

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Sulfonamides as Aromatase Inhibitors: Nimesulide Analogues, N-cyclic- and Aryl-Sulfonamides

Cristina Maccallini, Alessandra Ammazzalorso, Barbara De Filippis, Marialuigia Fantacuzzi et autres

Aromatase catalyzes the final and rate-limiting step in the biosynthesis of estrogens. Inhibitors of this key enzyme are used to treat hormone receptor-positive early, locally advanced, and metastatic breast cancers and are classified by structure into steroidal and nonsteroidal classes. Non-steroidal inhibitors, …

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Discovery and Evaluation of Novel Sulfonamide Derivatives Targeting Aromatase in ER+ Breast Cancer

Barbara De Filippis, Mariangela Agamennone, Alessandra Ammazzalorso, Rosa Vitale Amoroso et autres

Background: Third-generation aromatase inhibitors (CYP19A1) are the mainstay of treatment for estrogen-receptor-positive breast cancer. This is because estrogen is required for cancer growth in approximately 70% of patients with this condition. Although potent and effective, aromatase inhibitors induce resistance and secondary effects, …

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Targeting PPARs in the Brain: From Old Knowledge to Emerging Therapeutic Roles

Alessandra Ammazzalorso

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Azobenzene as Multi-Targeted Scaffold in Medicinal Chemistry

Barbara De Filippis, Alice Della Valle, Alessandra Ammazzalorso, Cristina Maccallini et autres

The discovery of a multi-target scaffold in medicinal chemistry is an important goal for the development of new drugs with different biological effects. Azobenzene is one of the frameworks in medicinal chemistry used for its simple synthetic methods and for the possibility …

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A sulfonimide derivative of bezafibrate as a dual inhibitor of cyclooxygenase-2 and PPARα

Alessandra Ammazzalorso, Stefania Tacconelli, Annalisa Contursi, Ulrika Hofling et autres

Background PPARα and cyclooxygenase (COX)-2 are overexpressed in certain types of cancer. Thus, developing a dual inhibitor that targets both could be more effective as an anticancer agent than single inhibitors. We have previously shown that an analog of the bezafibrate named …

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A novel life for antitumor combretastatins: Recent developments of hybrids, prodrugs, combination therapies, and antibody-drug conjugates

Marialuigia Fantacuzzi, Simone Carradori, Letizia Giampietro, Cristina Maccallini et autres

Since their discovery from natural sources, the potent cytotoxic effects of combretastatins were widely studied for the application in antitumor therapy. However, major pharmacokinetic issues as low water solubility and chemical instability of the double bond configuration prevented their use in therapy. …

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Azo derivatives of monoterpenes as anti- Helicobacter pylori agents: from synthesis to structure-based target investigation

Francesco Melfi, Marialuigia Fantacuzzi, Simone Carradori, Ilaria D’Agostino et autres

Monoterpene-derived azo benzenes showed selective antibacterial activity against Helicobacter pylori with a safe profile. An in silico investigation highlighted the inosine 5′-monophosphate dehydrogenase enzyme as the putative target.

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Azobenzenesulfonamide Carbonic Anhydrase Inhibitors as New Weapons to Fight Helicobacter pylori: Synthesis, Bioactivity Evaluation, In Vivo Toxicity, and Computational Studies

Letizia Giampietro, Beatrice Marinacci, Alice Della Valle, Ilaria D’Agostino et autres

Research into novel anti-Helicobacter pylori agents represents an important approach for the identification of new treatments for chronic gastritis and peptic ulcers, which are associated with a high risk of developing gastric carcinoma. In this respect, two series of azobenzenesulfonamides were designed, …

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CAPE derivatives: Multifaceted agents for chronic wound healing

Marwa F. Balaha, Amelia Cataldi, Alessandra Ammazzalorso, Ivana Cacciatore et autres

Chronic wounds significantly impact the patients' quality of life, creating an urgent interdisciplinary clinical challenge. The development of novel agents capable of accelerating the healing process is essential. Caffeic acid phenethyl ester (CAPE) has demonstrated positive effects on skin regeneration. However, its …

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Synthesis and in vitro cytotoxicity of benzoxazole‐based PPARα/γ antagonists in colorectal cancer cell lines

Nazaret Moreno‐Rodríguez, Antonio Laghezza, Carmen Cerchia, Darina V. Sokolova et autres

A series of benzoxazole-based amides and sulfonamides were synthesized and evaluated for their human peroxisome proliferator-activated receptor (PPAR)α and PPARγ activity. All tested compounds showed a dual antagonist profile on both PPAR subtypes; based on transactivation results, seven compounds were selected to …

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