Design, synthesis, and in vitro antiplasmodial activity of 4-aminoquinolines containing modified amino acid conjugates

2016 ◽  
Vol 25 (6) ◽  
pp. 1148-1162 ◽  
Author(s):  
Kondaparla Srinivasarao ◽  
Pooja Agarwal ◽  
Kumkum Srivastava ◽  
W. Haq ◽  
Sunil K. Puri ◽  
...  
Keyword(s):  
Amino Acid ◽  
Antiplasmodial Activity ◽  
Design Synthesis ◽  
Amino Acid Conjugates

scholarly journals Design, Synthesis, Phloem Mobility, and Bioactivities of a Series of Phenazine-1-Carboxylic Acid-Amino Acid Conjugates

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2139 ◽  
Author(s):  
Linhua Yu ◽  
Di Huang ◽  
Xiang Zhu ◽  
Min Zhang ◽  
Zongli Yao ◽  
...  
Keyword(s):  
Amino Acid ◽  
Carboxylic Acid ◽  
Design Synthesis ◽  
Phloem Sap ◽  
Amino Acid Conjugates ◽  
Highly Active ◽  
Vascular Pathogens ◽  
Phloem Mobility ◽  
Active Parent

Developing fungicides with phloem mobility that can be applied to leaves to control root or vascular pathogens has long been desirable. To achieve this goal, an efficient and economical strategy involves introducing an amino acid into the existing highly active parent pesticide molecule. Hence, 12 L-phenazine-1-carboxylic acid (PCA)-amino acid conjugates 4a–l were designed and synthesized via a simple synthetic route. In vitro bioassays results showed that all synthesized compounds 4a–l exhibited certain fungicidal activities against six tested fungi. Compound 4c exhibited relatively good fungicidal activity against Rhizoctonia solani, and the EC50 value was 0.084 ± 0.006 mmol/L. The phloem mobility experiments revealed that introducing an amino acid to PCA could effectively endow PCA with phloem mobility in R. communis L. Among them, nine conjugates were found in phloem sap, and L-PCA-Valine 4d exhibited the highest phloem mobility. Analysis results from the prediction of the Kleier model indicated that an active carrier-mediated mechanism may be involved in L-PCA-amino acid conjugates—a result that needs to be confirmed and complemented with further tests. The current research provides useful data for modifying non-phloem-mobile fungicidal molecules to phloem-mobile types.

In vitro solubility, stability and permeability of novel quercetin–amino acid conjugates

2009 ◽  
Vol 17 (3) ◽  
pp. 1164-1171 ◽  
Author(s):  
Mi Kyoung Kim ◽  
Kwang-su Park ◽  
Woon-seok Yeo ◽  
Hyunah Choo ◽  
Youhoon Chong
Keyword(s):  
Amino Acid ◽  
Amino Acid Conjugates

Preparation and in vitro evaluation of celecoxib-amino acid conjugates as a colon specific prodrug

2012 ◽  
Vol 42 (3) ◽  
pp. 115-120 ◽  
Author(s):  
Yonghyun Lee ◽  
Eun Hee Jung ◽  
Hyunjung Kim ◽  
Jeong-Hyun Yoon ◽  
Dae-Duk Kim ◽  
...  
Keyword(s):  
Amino Acid ◽  
In Vitro Evaluation ◽  
Amino Acid Conjugates

Building of neomycin–nucleobase–amino acid conjugates for the inhibition of oncogenic miRNAs biogenesis

2018 ◽  
Vol 16 (34) ◽  
pp. 6262-6274 ◽  
Author(s):  
Duc Duy Vo ◽  
Cécile Becquart ◽  
Thi Phuong Anh Tran ◽  
Audrey Di Giorgio ◽  
Fabien Darfeuille ◽  
...  
Keyword(s):  
Amino Acid ◽  
Gastric Adenocarcinoma ◽  
Amino Acid Conjugates ◽  
Adenocarcinoma Cells ◽  
Oncogenic Mirnas ◽  
Mirnas Biogenesis

Neomycin–nucleobase–amino acid conjugates bind to pre-miR-372 and inhibit Dicer-mediated processing thus leading to decreased levels of oncogenic miR-372 in vitro and in gastric adenocarcinoma cells.

Design, synthesis and stimuli responsive gelation of novel stigmasterol–amino acid conjugates

2011 ◽  
Vol 361 (2) ◽  
pp. 587-593 ◽  
Author(s):  
Hana Svobodová ◽  
Nonappa ◽  
Zdeněk Wimmer ◽  
Erkki Kolehmainen
Keyword(s):  
Amino Acid ◽  
Stimuli Responsive ◽  
Design Synthesis ◽  
Amino Acid Conjugates

scholarly journals Enone– and Chalcone–Chloroquinoline Hybrid Analogues: In Silico Guided Design, Synthesis, Antiplasmodial Activity, in Vitro Metabolism, and Mechanistic Studies

2011 ◽  
Vol 54 (10) ◽  
pp. 3637-3649 ◽  
Author(s):  
Eric M. Guantai ◽  
Kanyile Ncokazi ◽  
Timothy J. Egan ◽  
Jiri Gut ◽  
Philip J. Rosenthal ◽  
...  
Keyword(s):  
In Silico ◽  
In Vitro Metabolism ◽  
Antiplasmodial Activity ◽  
Mechanistic Studies ◽  
Design Synthesis

scholarly journals Amino Acid Conjugates of Aminothiazole and Aminopyridine as Potential Anticancer Agents: Synthesis, Molecular Docking and in vitro Evaluation

2021 ◽  
Vol Volume 15 ◽  
pp. 1459-1476
Author(s):  
Shagufta Naz ◽  
Fawad Ali Shah ◽  
Humaira Nadeem ◽  
Sadia Sarwar ◽  
Zhen Tan ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Amino Acid ◽  
Anticancer Agents ◽  
In Vitro Evaluation ◽  
Amino Acid Conjugates

Design, Synthesis and Antitumor Activity of Dimeric Bile Acid-Amino Acid Conjugates

2007 ◽  
Vol 4 (6) ◽  
pp. 414-418 ◽  
Author(s):  
Yan Li ◽  
Zhen Zhang ◽  
Yong Ju ◽  
Chang-Qi Zhao
Keyword(s):  
Bile Acid ◽  
Amino Acid ◽  
Antitumor Activity ◽  
Design Synthesis ◽  
Amino Acid Conjugates

Design, synthesis and evaluation of novel uracil amino acid conjugates for the inhibition of Trypanosoma cruzi dUTPase

2006 ◽  
Vol 16 (14) ◽  
pp. 3809-3812 ◽  
Author(s):  
Orla K. Mc Carthy ◽  
Alessandro Schipani ◽  
Alex Musso Buendía ◽  
Luis M. Ruiz-Perez ◽  
Marcel Kaiser ◽  
...  
Keyword(s):  
Amino Acid ◽  
Trypanosoma Cruzi ◽  
Design Synthesis ◽  
Amino Acid Conjugates
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