Oriented Crystallization on Organic Monolayers to Control Concomitant Polymorphism.,Chemistry - A European Journal

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Oriented Crystallization on Organic Monolayers to Control Concomitant Polymorphism.
Chemistry - A European Journal ( IF 3.9 ) Pub Date : 2019-12-27 , DOI: 10.1002/chem.201903938
Pranita Bora ₁ , Basanta Saikia ₁ , Bipul Sarma ₁

Affiliation

Nucleation events and crystal growth can be guided by molecular recognition at interfaces through intermolecular interactions. The short-acting antimicrobial sulfa drug sulfathiazole is known for its concomitant crystallization, which has five known polymorphs, due to conformational flexibility and hydrogen-bond synthon variation. In its development stage of a drug the issue of concomitant crystallization needs to be addressed with respect to patent litigation, including legal actions to protect patents against infringement. A functional self-assembled monolayer (SAM) of organic thiol on a gold surface has been employed as an efficient approach to control concomitant nucleation of such flexible drugs. The crystallization on a SAM surface is mostly kinetically driven and often leads to the nucleation of novel metastable forms. Spectroscopic, thermal analysis and X-ray diffraction studies reveal that a previously unknown, sixth form of the drug nucleates on the designed SAM surface.

中文翻译：

在有机单分子层上定向结晶以控制伴随的多态性。

成核事件和晶体生长可以通过分子间相互作用在界面处进行分子识别来指导。短效抗微生物磺胺药物磺胺噻唑以其伴随的结晶而闻名，由于构象柔韧性和氢键合成子的变化，其具有五种已知的多晶型物。在药物的开发阶段，需要解决与专利诉讼有关的伴随结晶问题，包括保护专利免受侵权的法律诉讼。金表面上有机硫醇的功能性自组装单分子层（SAM）已被用作控制此类柔性药物伴随成核的有效方法。SAM表面的结晶主要是动力学驱动的，通常会导致新的亚稳形式的成核。分光镜

更新日期：2019-12-27

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