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Crystal Modificatio...
Crystal Modifications of a Cyclic Guanosine Phosphorothioate Analogue, a Drug Candidate for Retinal Neurodegenerations
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- Perez, Oswaldo (författare)
- RISE,Kemiska processer och läkemedel,Chemical Processes and Pharmaceutical Development, Research Institutes of Sweden, Forskargatan 20 J, 151 36, Södertälje, Sweden, Forskargatan 20 J; Faculty of Pharmaceutical Sciences, University of Iceland, Sæmundargata 2, 102, Reykjavík, Iceland, Sæmundargata 2
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- Schipper, Nicolaas (författare)
- RISE,Kemiska processer och läkemedel,Chemical Processes and Pharmaceutical Development, Research Institutes of Sweden, Forskargatan 20 J, 151 36, Södertälje, Sweden, Forskargatan 20 J
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- Leandri, Valentina (författare)
- RISE,Kemiska processer och läkemedel,Chemical Processes and Pharmaceutical Development, Research Institutes of Sweden, Forskargatan 20 J, 151 36, Södertälje, Sweden, Forskargatan 20 J
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- Svensson, Per H. (författare)
- RISE,KTH,Tillämpad fysikalisk kemi,Chemical Processes and Pharmaceutical Development, Research Institutes of Sweden, Forskargatan 20 J, 151 36, Södertälje, Sweden,Kemiska processer och läkemedel,KTH Royal Institute of Technology, Sweden
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- Bohlin, Martin (författare)
- RISE,Kemiska processer och läkemedel,Chemical Processes and Pharmaceutical Development, Research Institutes of Sweden, Forskargatan 20 J, 151 36, Södertälje, Sweden, Forskargatan 20 J
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- Loftsson, Thorsteinn (författare)
- Faculty of Pharmaceutical Sciences, University of Iceland, Sæmundargata 2, 102, Reykjavík, Iceland, Sæmundargata 2
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- Bollmark, Martin (författare)
- RISE,Kemiska processer och läkemedel,Chemical Processes and Pharmaceutical Development, Research Institutes of Sweden, Forskargatan 20 J, 151 36, Södertälje, Sweden, Forskargatan 20 J
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(creator_code:org_t)
- Wiley, 2023
- 2023
- Engelska.
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Ingår i: ChemistryOpen. - : Wiley. - 2191-1363. ; 12:12
- Relaterad länk:
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https://doi.org/10.1...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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https://urn.kb.se/re...
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Abstract
Ämnesord
Stäng
- In contribution to the pharmaceutical development of cyclic guanosine monophosphorothioate analogue cGMPSA as a potential active pharmaceutical ingredient (API) for the treatment of inherited retinal degenerations (IRDs), its neutral form (cGMPSA-H) and salts of sodium (-Na), calcium (-Ca), ammonium (-NH4), triethylammonium (-TEA), tris(hydroxymethyl)aminomethane (-Tris), benethamine (-Bnet), and benzathine (-BZ) were prepared. Their solid-state properties were studied with differential scanning calorimetry, thermogravimetric analysis, hot-stage microscopy, and dynamic vapor sorption, and their solubilities were measured in deionized H2O as well as aqueous HCl and NaOH buffers. A total of 21 crystal modifications of cGMPSA were found and characterized by X-ray powder diffraction. Despite their crystalline character, no API forms featured any observable melting points during thermal analyses and instead underwent exothermic decomposition at ≥163 °C. Both the vapor sorption behavior and solubility were found to differ significantly across the API forms. cGMPSA-BZ featured the lowest aqueous solubility and hygroscopicity, with 50 μg/mL and 5 % mass gain at maximum relative humidity. The synthesis and crystallization of some crystal modifications were upscaled to >10 g. Single crystal X-ray diffraction was performed which resulted in the first crystal structure determination and absolute configuration of a cyclic guanosine monophosphorothioate, confirming the RP- conformation at the phosphorus atom.
Ämnesord
- NATURVETENSKAP -- Kemi -- Fysikalisk kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences -- Physical Chemistry (hsv//eng)
- TEKNIK OCH TEKNOLOGIER -- Medicinteknik (hsv//swe)
- ENGINEERING AND TECHNOLOGY -- Medical Engineering (hsv//eng)
Nyckelord
- Configuration determination
- Drug design
- Neurological agents
- Nucleotides
- Solid-state structures
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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