scholarly journals Design, Synthesis, and Characterization of Novel Series of Pharmacologically-important Sperm-shaped Amphiphilic Heterocyclic Compounds derived from Natural Palmitic Acid

2022 ◽  
Author(s):  
Amgad Rabie
Keyword(s):  
Palmitic Acid ◽  
Research Work ◽  
Synthesis And Characterization ◽  
Aliphatic Chain ◽  
Carboxyl Group ◽  
Efficient Design ◽  
Design Synthesis ◽  
Biochemical Processes ◽  
Heterocyclic Derivatives ◽  
Derivatives Of

Natural palmitic acid is a pivotal saturated fatty acid used in many biochemical processes occurring in humans and diverse living creatures, as it is the most common natural long-chain carboxylic acid whose unrivaled amphiphilic sperm-like skeleton with the inert single 15-C aliphatic chain (tail or carrier) and the very active one carboxyl group (head) represent a rich reactive entity and carrier for several organic/medicinal chemistry and pharmaceutics applications with respect to drug design and formulation. Derivatives of 1,3,4-oxadiazoles along with their 1,3,4-thiadiazoles and 1,2,4-triazoles analogs exhibit a broad spectrum of substantial pharmacological activities. Agreeing with the well-known hybridization principles and incorporation norms in hybrid chemistry, if a substituted nitrogenous heterocyclic aromatic nucleus of the three aforementioned kinds is straightway attached to the simple straight palmitic acid backbone at the position of the carboxyl group, the produced molecules are supposed to be very bioactive. This research work reports for the first once the efficient design/synthesis and characterization/elucidation of four one-tailed nitrogen-containing heterocyclic derivatives of palmitic acid constructure, which introduce a novel biologically-important pharmacophore having biocompatible amphiphilic sperm-shaped heteroaromatic structure.

Design, Synthesis, and Characterization of Fatty Acid Derivatives of a Dimeric Peptide-Based Postsynaptic Density-95 (PSD-95) Inhibitor

2015 ◽  
Vol 58 (3) ◽  
pp. 1575-1580 ◽  
Author(s):  
Klaus B. Nissen ◽  
Julie J. Andersen ◽  
Linda M. Haugaard-Kedström ◽  
Anders Bach ◽  
Kristian Strømgaard
Keyword(s):  
Fatty Acid ◽  
Postsynaptic Density ◽  
Synthesis And Characterization ◽  
Design Synthesis ◽  
Fatty Acid Derivatives ◽  
Derivatives Of

scholarly journals Design, Synthesis and Characterization of Pyrimidine based Thiazolidinedione Derivatives

2020 ◽  
Vol 32 (5) ◽  
pp. 1101-1108
Author(s):  
Vijay Kumar Sharma ◽  
Anup Barde ◽  
Sunita Rattan
Keyword(s):  
Knoevenagel Condensation ◽  
Condensation Reaction ◽  
Synthesis And Characterization ◽  
Metal Reduction ◽  
Aliphatic Chain ◽  
Pyrimidine Derivatives ◽  
Design Synthesis ◽  
Synthetic Strategy ◽  
Knoevenagel Condensation Reaction

Novel thiazolidine-2,4-dione (TZD) based pyrimidine derivatives have been synthesized by Knoevenagel condensation reaction between thiazolidine-2,4-dione and amino pyrimidinyl aliphatic aldehydes followed by heterogeneous metal reduction. Synthetic strategy involved nucleophillic substitution of hydroxyl protected six membered aliphatic chain on 4,6-dichloropyrimidine followed by Suzuki coupling. This approach is regioselective, efficient and versatile for synthesis of such analogs

scholarly journals A New Derivatives of Benzodiazepine, Imidazole, Isatin, Maleimide, Pyrimidine and 1,2,4-Triazole: Synthesis and Characterization

2008 ◽  
Vol 5 (2) ◽  
pp. 305-312
Author(s):  
Baghdad Science Journal
Keyword(s):  
1H Nmr ◽  
13C Nmr ◽  
Nmr Spectra ◽  
Synthesis And Characterization ◽  
13C Nmr Spectra ◽  
Organic Reagents ◽  
Cyclocondensation Reaction ◽  
Heterocyclic Derivatives ◽  
Ft Ir ◽  
Derivatives Of

The synthesis of new benzodiazepine, imidazole, isatin, maleimide, pyrimidine and 1,2,4-triazole derived from 2-amino-4-hydroxy-1,3,5-triazine, via its cyclocondensation reaction with different organic reagents, is described. FT-IR, 1H-NMR and as well as 13C-NMR spectra disclosed the structures of the precursors and heterocyclic derivatives formed.

scholarly journals Design, synthesis, and spasmolytic activity of thiophene-based derivatives via Suzuki cross-coupling reaction of 5-bromothiophene-2-carboxylic acid: their structural and computational studies

2020 ◽  
Vol 44 (5) ◽  
pp. 1410-1422
Author(s):  
Nasir RASOOL ◽  
Hafiz Mansoor IKRAM ◽  
Ammara RASHID ◽  
Nazia AFZAL ◽  
Muhammad Ali HASHMI ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Density Functional ◽  
Research Work ◽  
Coupling Reaction ◽  
Design Synthesis ◽  
Spasmolytic Activity ◽  
Reactivity Descriptors ◽  
Cross Coupling Reaction ◽  
Structural And Electronic Properties ◽  
Derivatives Of

In the current research work, a facile synthesis of a series of novel thiophene-based derivatives of 5-bromothiophene-2- carboxylic acid (1) have been synthesized. All analogs (5a-5e, 10a-10f) were obtained from the coupling reaction of 5-bromothiophene- 2-carboxylic acid (1) and different arylboronic acids with moderate-to-good yields under controlled and optimal conditions. The structures of the newly synthesized compounds were characterized through spectral analysis and their spasmolytic activity, and most of the compounds exhibited potentially good spasmolytic effect. Among the synthesized analogs, compound phenethyl 5-(3,4-dichlorophenyl)thiophene-2-carboxylate (10d) particular showed an excellent spasmolytic effect with an EC50 value of 1.26. All of the compounds were also studied for their structural and electronic properties by density functional theory (DFT) calculations. Through detailed insight into frontier molecular orbitals of the compounds and their different reactivity descriptors, it was found that the compounds 10c and 5c are the most reactive, while 10a is the most stable in the series. Furthermore, compounds 10c and 5c showed a very good NLO response with the highest β values.

Design, Synthesis and Evaluation of Novel Derivatives of Orotic Acid Amide as Potent Glucokinase Activators

2017 ◽  
Vol 14 (3) ◽  
pp. 252-261 ◽  
Author(s):  
Leilei Zhang ◽  
Shengquan Hu ◽  
Lei Lei ◽  
Yuliang Zhang ◽  
Lijing Zhang ◽  
...  
Keyword(s):  
Orotic Acid ◽  
Acid Amide ◽  
Design Synthesis ◽  
Glucokinase Activators ◽  
Derivatives Of

Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Hybridized Quinoline Derivatives as Anticancer Agents: Design, Synthesis, Biological Evaluation and Molecular Docking

2019 ◽  
Vol 19 (4) ◽  
pp. 439-452 ◽  
Author(s):  
Mohamed R. Selim ◽  
Medhat A. Zahran ◽  
Amany Belal ◽  
Moustafa S. Abusaif ◽  
Said A. Shedid ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Caspase 3 ◽  
Biological Evaluation ◽  
Tubulin Polymerization ◽  
Design Synthesis ◽  
Chemical Structures ◽  
M Phase ◽  
Induced Apoptosis ◽  
Derivatives Of

Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.

Three Amino Acid Derivatives of Valproic Acid: Design, Synthesis, Theoretical and Experimental Evaluation as Anticancer Agents

2014 ◽  
Vol 14 (7) ◽  
pp. 984-993 ◽  
Author(s):  
Gabriela Luna-Palencia ◽  
Federico Martinez-Ramos ◽  
Ismael Vasquez-Moctezuma ◽  
Manuel Fragoso-Vazquez ◽  
Jessica Mendieta-Wejebe ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Amino Acid ◽  
Anticancer Agents ◽  
Experimental Evaluation ◽  
Amino Acid Derivatives ◽  
Design Synthesis ◽  
Derivatives Of
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