![](/images/graphics-bg.png)
Design, Antileishmanial Activity, and QSAR Studies of a Series of Piplartine Analogues
المؤلفون المشاركون
Lima, Tamires Cardoso
Bezerra, Daniel Pereira
Perez-Castillo, Yunierkis
Nóbrega, Flávio R.
Silva, Larisse V.
Bezerra Filho, Carlos da Silva M.
Lima, Tatjana K. Souza
de Sousa, Damião Pergentino
المصدر
العدد
المجلد 2019، العدد 2019 (31 ديسمبر/كانون الأول 2019)، ص ص. 1-12، 12ص.
الناشر
Hindawi Publishing Corporation
تاريخ النشر
2019-01-08
دولة النشر
مصر
عدد الصفحات
12
التخصصات الرئيسية
الملخص EN
Piplartine is an alkamide found in different Piper species and possesses several biological activities, including antiparasitic properties.
Thus, the aim of the present study was to evaluate a series of 32 synthetic piplartine analogues against the Leishmania amazonensis promastigote forms and establish the structure-activity relationship and 3D-QSAR of these compounds.
The antileishmanial effect of the compounds was determined using the MTT method.
Most compounds were found to be active against L.
amazonensis.
Among 32 assayed derivatives, compound (E)-(−)-bornyl 3-(3,4,5-trimethoxyphenyl)-acrylate exhibited the most potent antileishmanial activity (IC50 = 0.007 ± 0.008 μM, SI > 10), followed by benzyl 3,4,5-trimethoxybenzoate (IC50 = 0.025 ± 0.009 μM, SI > 3.205) and (E)-furfuryl 3-(3,4,5-trimethoxyphenyl)-acrylate (IC50 = 0.029 ± 0.007 μM, SI > 2.688).
It was found that the rigid substituents contribute to increasing antiparasitic activity against L.
amazonensis promastigotes.
The presence of the unsaturated heterocyclic substituent in the phenylpropanoid chemical structure (furfuryl group) resulted in a bioactive derivative.
Molecular simplification of benzyl 3,4,5-trimethoxybenzoate by omitting the spacer group contributed to the bioactivity of this compound.
Furthermore, bornyl radical appears to be important for antileishmanial activity, since (E)-(−)-bornyl 3-(3,4,5-trimethoxyphenyl)-acrylate exhibited the most potent antileishmanial activity.
These results show that some derivatives studied would be useful as prototype molecules for the planning of new derivatives with profile of antileishmanial drugs.
نمط استشهاد جمعية علماء النفس الأمريكية (APA)
Nóbrega, Flávio R.& Silva, Larisse V.& Bezerra Filho, Carlos da Silva M.& Lima, Tamires Cardoso& Perez-Castillo, Yunierkis& Bezerra, Daniel Pereira…[et al.]. 2019. Design, Antileishmanial Activity, and QSAR Studies of a Series of Piplartine Analogues. Journal of Chemistry،Vol. 2019, no. 2019, pp.1-12.
https://search.emarefa.net/detail/BIM-1171107
نمط استشهاد الجمعية الأمريكية للغات الحديثة (MLA)
Nóbrega, Flávio R.…[et al.]. Design, Antileishmanial Activity, and QSAR Studies of a Series of Piplartine Analogues. Journal of Chemistry No. 2019 (2019), pp.1-12.
https://search.emarefa.net/detail/BIM-1171107
نمط استشهاد الجمعية الطبية الأمريكية (AMA)
Nóbrega, Flávio R.& Silva, Larisse V.& Bezerra Filho, Carlos da Silva M.& Lima, Tamires Cardoso& Perez-Castillo, Yunierkis& Bezerra, Daniel Pereira…[et al.]. Design, Antileishmanial Activity, and QSAR Studies of a Series of Piplartine Analogues. Journal of Chemistry. 2019. Vol. 2019, no. 2019, pp.1-12.
https://search.emarefa.net/detail/BIM-1171107
نوع البيانات
مقالات
لغة النص
الإنجليزية
الملاحظات
Includes bibliographical references
رقم السجل
BIM-1171107
قاعدة معامل التأثير والاستشهادات المرجعية العربي "ارسيف Arcif"
أضخم قاعدة بيانات عربية للاستشهادات المرجعية للمجلات العلمية المحكمة الصادرة في العالم العربي
![](/images/ebook-kashef.png)
تقوم هذه الخدمة بالتحقق من التشابه أو الانتحال في الأبحاث والمقالات العلمية والأطروحات الجامعية والكتب والأبحاث باللغة العربية، وتحديد درجة التشابه أو أصالة الأعمال البحثية وحماية ملكيتها الفكرية. تعرف اكثر
![](/images/kashef-image.png)