Results 51 to 60 of about 8,500 (189)

Preparation of Theophylline-Benzoic Acid Cocrystal and On-Line Monitoring of Cocrystallization Process in Solution by Raman Spectroscopy

open access: yesCrystals, 2019
Pure theophylline-benzoic acid cocrystal was prepared via slurry and cooling crystallization in solution to overcome the disadvantages of existing preparation methods.
Yaohui Huang   +8 more
doaj   +1 more source

Discovery of a Potent Fluorescence Polarization Probe for Identifying USP1 Allosteric Inhibitors

open access: yesAdvanced Science, EarlyView.
This study presents the first ubiquitin‐specific protease 1 (USP1) allosteric fluoroprobe and fluorescence polarization assay, enabling the differentiation of allosteric and catalytic site inhibitors. Further, a novel class of tetrahydroisoquinoline‐based USP1 inhibitors is designed, with compound 14a (USP1 IC50 = 29.9 nM) showing strong selectivity ...
Jiawei Cheng   +12 more
wiley   +1 more source

Optimized solubility and bioavailability of genistein based on cocrystal engineering

open access: yesNatural Products and Bioprospecting, 2023
With various potential health-promoting bioactivities, genistein has great prospects in treatment of a series of complex diseases and metabolic syndromes such as cancer, diabetes, cardiovascular diseases, menopausal symptoms and so on.
Zhipeng Wang   +10 more
doaj   +1 more source

Synthesis and Characterization of a New Norfloxacin/Resorcinol Cocrystal with Enhanced Solubility and Dissolution Profile

open access: yesPharmaceutics, 2021
A new cocrystal of Norfloxacin, a poorly soluble fluoroquinolone antibiotic, has been synthetized by a solvent-mediated transformation experiment in toluene, using resorcinol as a coformer. The new cocrystal exists in both anhydrous and monohydrate forms
Hanan Fael   +4 more
doaj   +1 more source

Accelerating Discovery of Organic Molecular Crystals via Materials Informatics and Autonomous Experiments

open access: yesAdvanced Intelligent Discovery, EarlyView.
Materials informatics and autonomous experimentation are transforming the discovery of organic molecular crystals. This review presents an integrated molecule–crystal–function–optimization workflow combining machine learning, crystal structure prediction, and Bayesian optimization with robotic platforms.
Takuya Taniguchi   +2 more
wiley   +1 more source

Complete Cocrystal Formation during Resonant Acoustic Wet Granulation: Effect of Granulation Liquids

open access: yesPharmaceutics, 2021
The manufacturing of solid pharmaceutical dosage forms composed of cocrystals requires numerous processes during which there is risk of dissociation into parent molecules.
Ryoma Tanaka   +5 more
doaj   +1 more source

Air-Stable Cyclohexasulfur as Cocrystal [PDF]

open access: yesCrystal Growth & Design, 2012
A new stable cyclohexasulfur (cyclo-S6) was discovered in the crystal of 3,5-diphenyl-1,2,4-dithiazol-1-ium (dpdti); dpdti was synthesized via an oxidation reaction of thiobenzamide with iodine in ...
Kunihisa Sugimoto   +3 more
openaire   +1 more source

A Chiral Saddle‐Shaped Nanographene With Two Heptagon‐Embedded [4]Helicenes

open access: yesAngewandte Chemie International Edition, EarlyView.
We present a novel synthetic strategy toward a chiral saddle‐shaped nanographene (cSNG) via a two‐step oxidation of a prochiral anthracene precursor. The Scholl‐type oxidation first yields a key intermediate with sp3‐defect heptagons, and subsequent oxidative dehydrogenation affords fully conjugated cSNG.
Felix Trautner   +11 more
wiley   +1 more source

Formation Thermodynamics of Carbamazepine with Benzamide, Para-Hydroxybenzamide and Isonicotinamide Cocrystals: Experimental and Theoretical Study

open access: yesPharmaceutics, 2022
Formation thermodynamic parameters for three cocrystals of carbamazepine (CBZ) with structurally related coformers (benzamide (BZA), para-hydroxybenzamide (4-OH-BZA) and isonicotinamide (INAM)) were determined by experimental (cocrystal solubility and ...
Alex N. Manin   +5 more
doaj   +1 more source

Stafib‐2‐CR: an Improved Nanomolar and Selective Inhibitor of the Transcription Factor STAT5b Developed by Conformational Restriction of Stafib‐2

open access: yesChemistry – A European Journal, EarlyView.
Conformational restriction strategies to increase the activity and selectivity of the STAT5b inhibitor Stafib‐2 are presented. The best conformationally restricted inhibitor Stafib‐2‐CR has threefold higher activity against STAT5b than Stafib‐2. A cell‐permeable prodrug of Stafib‐2‐CR inhibits phosphorylation of STAT5b in cultured human leukemia cells ...
Theresa Münzel   +5 more
wiley   +1 more source

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