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Impact of Conformations and Size on the Antileishmanial Activity of New Quinazoline Derivatives
ChemRxiv Pub Date : 2020-08-03 , DOI: 10.26434/chemrxiv.12746915.v1
Cesar Mendoza-Martinez , Alejandro Rodriguez-Lezama , Norma Galindo-Sevilla , Fernando Cortés-Guzmán , Jessica Hernandez-Pineda , Abril Nieto-Lara , Francisco Hernandez-Luis

There is an urgency of finding molecules available to treat Leishmaniasis, which is one of the significant issues of health in undeveloped countries. For that reason is needed to explore molecular diversity to find novel scaffolds. Fluorinated and adamantane derivatives exhibit a formidable starting point. They are proved to improve the antileishmanial activity when attached to molecules already active as we have shown in this paper. Particularly fluorinated methoxy and ethoxy derivatives can increase its volume depending on the number of fluorine, a unique behaviour that can be exploited for molecular drug design purposes.

中文翻译:

构型和大小对新型喹唑啉衍生物抗leishmanial活性的影响

迫切需要找到可用于治疗利什曼病的分子,这是不发达国家健康的重要问题之一。因此,需要探索分子多样性以发现新颖的支架。氟化和金刚烷衍生物显示出令人生畏的起点。如我们在本文中所显示的,当它们附着到已经具有活性的分子上时,它们被证明可以改善抗菌活性。特别是氟化的甲氧基和乙氧基衍生物可以根据氟的数量增加其体积,这是一种可以用于分子药物设计目的的独特行为。
更新日期:2020-08-03
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