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Pharmaceuticals, Volume 15, Issue 12

December 2022 - 147 articles

Cover Story: The design of drugs for multifactorial diseases is one of the most significant challenges for medicinal chemistry today. In this scenario, multitarget drugs appear attractive as they can simultaneously affect several biological mechanisms. In this work, we present the molecular docking-directed optimization of 5-aminoanthranilic acid derivatives, their in vitro evaluation, and the determination of their effects in an in vivo model of metabolic syndrome induced by a hypercaloric diet. The optimized compound simultaneously lowered glucose, triglyceride, and cholesterol levels after 14 days of oral administration. The evidence suggests that the mechanisms related to the biological effects of these new compounds result from an orchestrated and balanced activation between different PPAR subtypes and HMG-CoA inhibitory properties. View this paper
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Articles (147)

  • Article
  • Open Access
6 Citations
3,866 Views
18 Pages

New Insights into the Structural Requirements of Isatin-Derived Pro-Apoptotic Agents against Acute Myeloid Leukemia

  • Ahmed K. Hamdy,
  • Takashi Sakamoto,
  • Tsugumasa Toma,
  • Masaharu Sakamoto,
  • Mohammed A. S. Abourehab,
  • Masami Otsuka,
  • Mikako Fujita,
  • Hiroshi Tateishi and
  • Mohamed O. Radwan

17 December 2022

Searching for bioactive compounds within the huge chemical space is like trying to find a needle in a haystack. Isatin is a unique natural compound which is endowed with different bio-pertinent activities, especially in cancer therapy. Herein, we env...

  • Article
  • Open Access
2 Citations
2,850 Views
11 Pages

Heart Uptake of [18F]Fluoro-4-Thia-Oleate in a Non-Alcoholic Fatty Liver Disease Mouse Model

  • Junfeng Li,
  • Weidong Hu,
  • Jiangling Peng,
  • Patty Wong,
  • Fouad Kandeel,
  • Tove Olafsen and
  • John E. Shively

17 December 2022

The world-wide high incidence of non-alcoholic fatty liver disease (NAFLD) is of concern for its progression to insulin resistance, steatohepatitis and cardiovascular disease (CVD). The increased uptake of fatty acids in critical organs plays a major...

  • Article
  • Open Access
4 Citations
3,218 Views
14 Pages

Aromatase-Inhibitor-Induced Musculoskeletal Inflammation Is Observed Independent of Oophorectomy in a Novel Mouse Model

  • Nicholas A. Young,
  • Jeffrey Hampton,
  • Juhi Sharma,
  • Kyle Jablonski,
  • Courtney DeVries,
  • Anna Bratasz,
  • Lai-Chu Wu,
  • Maryam Lustberg,
  • Raquel Reinbolt and
  • Wael N. Jarjour

17 December 2022

Aromatase Inhibitors (AIs) block estrogen production and improve survival in patients with hormone-receptor-positive breast cancer. However, half of patients develop aromatase-inhibitor-induced arthralgia (AIIA), which is characterized by inflammatio...

  • Article
  • Open Access
27 Citations
3,742 Views
29 Pages

Antidiabetic Potential of Novel 1,3,5-Trisubstituted-2-Thioxoimidazloidin-4-One Analogues: Insights into α-Glucosidase, α-Amylase, and Antioxidant Activities

  • Salma M. Khirallah,
  • Heba M. M. Ramadan,
  • Hossam Aladl Aladl Aladl,
  • Najla O. Ayaz,
  • Lina A. F. Kurdi,
  • Mariusz Jaremko,
  • Samar Zuhair Alshawwa and
  • Essa M. Saied

17 December 2022

As the ninth leading cause of death globally, diabetes mellitus (DM) is considered to be the worst chronic metabolic disease requiring an enormous need for healthcare with over 578 million expected cases by 2023. Several recent findings have demonstr...

  • Article
  • Open Access
6 Citations
3,042 Views
19 Pages

Marine Sponge Aaptos suberitoides Extract Improves Antiproliferation and Apoptosis of Breast Cancer Cells without Cytotoxicity to Normal Cells In Vitro

  • Jun-Ping Shiau,
  • Min-Yu Lee,
  • Jen-Yang Tang,
  • Hsin Huang,
  • Zheng-Yu Lin,
  • Jui-Hsin Su,
  • Ming-Feng Hou,
  • Yuan-Bin Cheng and
  • Hsueh-Wei Chang

16 December 2022

The anticancer effects and mechanisms of marine sponge Aaptos suberitoides were rarely assessed, especially for methanol extract of A. suberitoides (MEAS) to breast cancer cells. This study evaluated the differential suppression effects of proliferat...

  • Review
  • Open Access
14 Citations
7,477 Views
23 Pages

The Hidden Pandemic of COVID-19-Induced Organizing Pneumonia

  • Evgeny Bazdyrev,
  • Maria Panova,
  • Valeria Zherebtsova,
  • Alexandra Burdenkova,
  • Ivan Grishagin,
  • Fedor Novikov and
  • Vladimir Nebolsin

16 December 2022

Since the beginning of the COVID-19 pandemic, clinical, radiological, and histopathological studies have provided evidence that organizing pneumonia is a possible consequence of the SARS-CoV2 infection. This post-COVID-19 organizing pneumonia (PCOP)...

  • Review
  • Open Access
49 Citations
13,847 Views
18 Pages

16 December 2022

Atherosclerotic cardiovascular diseases (ASCVD) are a very important cause of premature death. The most important risk factor for ASCVD is lipid disorders. The incidence of lipid disorders and ASCVD is constantly increasing, which means that new meth...

  • Article
  • Open Access
15 Citations
2,626 Views
14 Pages

Peptide-Based Hydrogels and Nanogels Containing Gd(III) Complexes as T1 Relaxation Agents

  • Elisabetta Rosa,
  • Fabio Carniato,
  • Lorenzo Tei,
  • Carlo Diaferia,
  • Giancarlo Morelli,
  • Mauro Botta and
  • Antonella Accardo

16 December 2022

New peptide-based hydrogels incorporating Gd(III) chelates with different hydration states, molecular structures and overall negative charges ([Gd(BOPTA)]2−), [Gd(DTPA)]2−, and ([Gd(AAZTA)]−) were prepared and characterized. N-termi...

  • Article
  • Open Access
15 Citations
5,638 Views
19 Pages

Hyaluronic Acid and Radiofrequency in Patients with Urogenital Atrophy and Vaginal Laxity

  • Piotr Kolczewski,
  • Mirosław Parafiniuk,
  • Piotr Zawodny,
  • Rashad Haddad,
  • Agnieszka Nalewczyńska,
  • Agnieszka Kinga Kolasa,
  • Barbara Wiszniewska,
  • Sophie Menkes,
  • Alexander Bader and
  • Giorgio Stabile
  • + 1 author

16 December 2022

Vaginal laxity (VL) and genitourinary syndrome of menopause (GSM), as well as aesthetic changes in the vulvar skin, often occur together and cause physical, psychological, and functional problems for women and their partners. The current study evalua...

  • Article
  • Open Access
7 Citations
4,912 Views
11 Pages

16 December 2022

Kreon® (Creon®) and Lipancrea® are pancreatic enzyme supplements indicated in the treatment of exocrine pancreatic insufficiency. In order to determine their interchangeability, an in vitro comparison of their physical properties and enzy...

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Pharmaceuticals - ISSN 1424-8247