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6 Results Found

  • Article
  • Open Access
13 Citations
8,851 Views
12 Pages

N-Acetyl-l-phenylalanine Racemization during TBTU Amidation: An In-Depth Study for the Synthesis of Anti-Inflammatory 2-(N-Acetyl)-l-phenylalanylamido-2-deoxy-d-glucose (NAPA)

  • Elisa Sturabotti,
  • Fabrizio Vetica,
  • Giorgia Toscano,
  • Andrea Calcaterra and ,
  • Andrea Martinelli,
  • Luisa Maria Migneco and
  • Francesca Leonelli
  • + 2 authors+ 0 author

6 January 2023

A thorough study on the amidation conditions of N-acetyl-l-phenylalanine using TBTU and various bases is reported for the synthesis of 2-(N-acetyl)-l-phenylalanylamido-2-deoxy-d-glucose (NAPA), a promising drug for the treatment of joints diseases. T...

(This article belongs to the Section Organic Chemistry)
  • Article
  • Open Access
10 Citations
3,801 Views
17 Pages

A Convenient One-Pot Synthesis of Novel Benzimidazole–Thiazinone Derivatives and Their Antimicrobial Activity

  • Sabahat Samreen,
  • Asghar Ali,
  • Saiema Ahmedi,
  • Mohammad Raghib and ,
  • Anzarul Haque,
  • Nikhat Manzoor,
  • Afzal Hussain,
  • Mohammad Abid and
  • Afreen Inam
  • + 4 authors+ 0 author

2 December 2024

Background: The increasing prevalence of antimicrobial resistant highlights the urgent need for the new therapeutic agents. This study aimed to design and synthesize fused tricyclic benzimidazole–thiazinone derivatives (CS1–CS10) through...

(This article belongs to the Section Novel Antimicrobial Agents)
  • Short Note
  • Open Access
2,026 Views
5 Pages

2-(2-(Benzylamino)-2-Oxoethyl)-1-Methyl-1H-Pyrrole-3-Carboxylic Acid

  • Monika Fryc,
  • Beata Gryzło,
  • Pravin Kumar and
  • Agnieszka Zagórska

20 June 2025

Here, 2-(2-(Benzylamino)-2-oxoethyl)-1-methyl-1H-pyrrole-3-carboxylic acid was efficiently synthesised in good yield via an amide coupling reaction between 2-carboxymethyl-1-methyl-1H-pyrrole-3-carboxylic acid and benzylamine, employing TBTU as the c...

  • Article
  • Open Access
3 Citations
9,260 Views
17 Pages

A Concise Synthesis of Glycolipids Based on Aspartic Acid Building Blocks

  • Trinidad Velasco-Torrijos,
  • Lorna Abbey and
  • Roisin O’Flaherty

25 September 2012

L-Aspartic acid building blocks bearing galactosyl moieties were used to synthesise glycolipid mimetics of variable hydrocarbon chain length. The glycolipids were readily prepared through amide bond formation using the TBTU/HOBt coupling methodology....

(This article belongs to the Special Issue Advances in Carbohydrate Chemistry 2012)
  • Article
  • Open Access
1 Citations
1,238 Views
19 Pages

Thienyl-Based Amides of M2 and Neuraminidase Inhibitors: Synthesis, Structural Characterization, and In Vitro Antiviral Activity Against Influenza a Viruses

  • Maya Chochkova,
  • Boyka Stoykova,
  • Magdalena Angelova,
  • Hristina Sbirkova-Dimitrova and ,
  • Rusi Rusew,
  • Yuhuan Li,
  • Andrey Popatanasov,
  • Nejc Petek,
  • Martin Štícha and
  • Boris Shivachev
  • + 5 authors+ 0 author

29 August 2025

Influenza A viruses that cause pandemics, as well as other harmful pathogens (e.g., SARS-CoV-2 variants), are known as the ‘silent bioterrorists’ of the 21st century. Due to high mutability, anti-influenza chemotherapeutic treatment is a...

(This article belongs to the Special Issue Celebrating the 10th Anniversary of International Crystallography)
  • Article
  • Open Access
2 Citations
3,439 Views
12 Pages

Synthesis, Molecular Docking, and Neuroprotective Effect of 2-Methylcinnamic Acid Amide in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)—An Induced Parkinson’s Disease Model

  • Maya Chochkova,
  • Rusi Rusew,
  • Reni Kalfin,
  • Lyubka Tancheva and ,
  • Maria Lazarova,
  • Hristina Sbirkova-Dimitrova,
  • Andrey Popatanasov,
  • Krasimira Tasheva,
  • Boris Shivachev and
  • Martin Štícha
  • + 6 authors+ 1 author

26 October 2022

Parkinson’s disease (PD) has emerged as the second most common form of human neurodegenerative disorders. However, due to the severe side effects of the current antiparkinsonian drugs, the design of novel and safe compounds is a hot topic among...

(This article belongs to the Special Issue State-of-the-Art Research in Biomolecular Crystals)