Results 101 to 110 of about 14,340 (184)

Targeting Human Immunodeficiency Virus Integrase Beyond the Active Site: The Discovery and Development of Allosteric Integrase Inhibitors

ChemMedChem, Volume 21, Issue 16, 27 August 2026.
Human immunodeficiency virus (HIV) allosteric integrase inhibitors (ALLINIs) offer a vital alternative to standard therapies by targeting noncatalytic sites. By inducing aberrant integrase multimerization, they disrupt viral maturation. This review explores their medicinal chemistry evolution, detailing structural insights, structure–activity ...
Francesco Saccoliti, Elisa Patacchini, Emanuele Cara, Laura Zarbo, Antonella Messore, Aurora Albano, Giuseppe Ruggieri, Valentina Noemi Madia, Luigi Scipione, Roberta Costi, Roberto Di Santo   +10 more
wiley   +1 more source

Cocrystallization and Particle Size Reduction of Active Pharmaceutical Ingredients (APIs) Using Supercritical Carbon Dioxide Crystallization or Spray Drying

Modern active pharmaceutical ingredients (APIs) often exhibit poor aqueous solubility, leading to poor bioavailability. Methods to improve dissolution include altering solid form (salts, polymorphs, cocrystals), creating amorphous dispersions, and ...
MacEachern, Lauren
core  

Enhanced dissolution and stability of adefovir dipivoxil by cocrystal formation

, 2011
Objectives The objectives of this study were to prepare and characterize the novel adefovir dipivoxil–saccharin cocrystal and to demonstrate the enhanced dissolution and stability of adefovir dipivoxil by cocrystal formation.
Hui Zu, Jianjun Zhang, Yuan Gao
core   +1 more source

Structural and Biophysical Characterization of C‐Glycosylic 1,2‐Thiodisaccharides Reveals Determinants of Selective Binding to Galectin‐7 and Galectin‐8N

ChemMedChem, Volume 21, Issue 16, 27 August 2026.
The molecular basis of galectin recognition by C‐glycosylic 1,2‐thiodisaccharides is revealed. While Gly‐1 provides a conserved affinity driving interaction, Gly‐2 governs isoform selectivity through contacts with variable CRD regions. Unique galectin‐8N residues are identified as attractive handles for the development of next‐generation selective ...
Anastasia S. Tsagkarakou, Anastassia L. Kantsadi, Vasiliki I. Theodoridou, Nikolaos Veliotis, László Lázár, János József, László Juhász, George Kontopidis, Hakon Leffler, Ulf J. Nilsson, László Somsák, Demetres D. Leonidas   +11 more
wiley   +1 more source

Investigating the Binding Mode of a Naphthol‐Based Inhibitor Targeting SARS‐CoV‐2 Main Protease

ChemMedChem, Volume 21, Issue 16, 27 August 2026.
A highly integrated workflow combining various computational, biophysical, and biochemical methods guides the discovery and characterization of an original naphthol‐based scaffold with inhibitory activity against the main protease of SARS‐CoV‐2 and demonstrates the efficiency of a sophisticated, open‐access consensus ranking protocol for virtual ...
Ifigeneia Akrani, Haifa El Kilani, Franck Touret, Sophia Kouvali, Veronika Gourni, Aggeliki Tsoka, Joulia K. Tsetis, Constantinos Vorgias, Rolf Hilgenfeld, Ioannis K. Kostakis, Vassilios Myrianthopoulos, Emmanuel Mikros   +11 more
wiley   +1 more source

Effect of Micellar Solubilization on Cocrystal Solubility and Stability

, 2016
Micellar solubilization of cocrystals is explained by the distribution of cocrystal components in micellar and aqueous pseudophases. The dependence of cocrystal solubilization on surfactant concentration is characterized by nonlinear behavior and an ...
Neal Huang (2301430), Naír Rodríguez-Hornedo (2049193)   +1 more
core   +1 more source

Sulfonylurea Bioisosteres of Sulfonic Acid in JFD 00458‐Based ST6GAL1 Inhibitors Enhance Membrane Permeability

ChemMedChem, Volume 21, Issue 16, 27 August 2026.
ST6GAL1 sialylates glycoconjugates in the Golgi, modulating immune recognition and enabling tumor immune evasion. To effectively reach ST6GAL1, inhibitors should demonstrate good membrane permeability. Based on nonpermeable hit JFD 00458, we developed sulfonylurea analogs achieving increased membrane permeability and potency.
Natan Koraj, Sushmaa Dangudubiyyam, Adelyn M. Betances‐Mora, Ema Faganeli, Anne Harduin‐Lepers, Jesús Angulo, Tan Khanh Nguyen, María Bort‐Griñó, Ramon Hurtado‐Guerrero, Marko Anderluh   +9 more
wiley   +1 more source

Crystal structure, Hirshfeld surface and intermolecular interaction energy analysis of the halogen-bonded 1:1 cocrystal 1-bromo-3,5-dinitrobenzene–N,N-dimethylpyridin-4-amine

Acta Crystallographica Section E: Crystallographic Communications
The structure of the 1:1 cocrystal formed between 1-bromo-3,5-dinitrobenzene and N,N-dimethylpyridin-4-amine that features a C—Br...N halogen bond is reported. The cocrystal, C6H3BrN2O4·C7H10N2, crystalizes in the monoclinic space group P21/c with Z = 4.
Eric Bosch
doaj   +1 more source

Kinetic entrapment of a hidden curcumin cocrystal with phloroglucinol

, 2014
© 2014 American Chemical Society. The existence of a cocrystal between curcumin (CUR) and phloroglucinol (PHL) was suspected but could not be demonstrated in a recent systematic effort to synthesize novel curcumin cocrystals.
Wai Wing Ng, Karthik Nagapudi, Leung, Kari Hoi Yan, Shing Fung Chow, Shi, Limin, Nagapudi, Karthik, Sun, Changquan Calvin, Kari Hoi Yan Leung, Albert H. L. Chow, Changquan Calvin Sun, Chow, Shing Fung, Ng, Wai Wing, Chow, Albert H.L., Limin Shi   +13 more
core   +1 more source

Silybin Cocrystals with Improved Solubility and Bioavailability

Pharmaceuticals
Backgroud/Objectives: Silymarin, an extract from milk thistle, is widely recognized for its therapeutic potential in treating liver disorders. However, its clinical utility is limited by the poor solubility and low bioavailability of its key active ...
Bingqing Zhu, Zhenfeng Ding, Xiaoyi Rong, Shengqiang Li, Xuefeng Mei   +4 more
doaj   +1 more source