scholarly journals Σχεδιασμός, σύνθεση και μελέτη βιολογικής δράσης θειαζολικών παραγώγων

2014 ◽  
Author(s):  
Κωνσταντίνος Λιάρας
Keyword(s):  
Wide Spectrum ◽  
Paw Edema ◽  
Thiazole Derivatives ◽  
In Vivo Evaluation ◽  
Design Synthesis ◽  
Edema Model ◽  
Bacteria And Fungi ◽  
Cox 1

This thesis presents and discusses the design, synthesis and evaluation ofbiological activity of twenty-two (22) novel thiazole derivatives, twelve (12) of whichare chalcones, two (2) aminopyrimidines and eight (8), N-phenylpyrazolines.Prediction of biological activity spectra for all compounds was performed bythe program PASS.The aim was to design compounds that would combine antimicrobial and antiinflammatoryactivity, taking into account the wide spectrum of biological activitiesof thiazole derivatives, as well as, the interesting pharmacological properties ofchalcones, aminopyrimidines and N-phenylpyrazolines.The final compounds were identified by elemental analysis and spectroscopicmethods.Σheoritical calculations of several physicochemical parameters, includinglipophilicity, were performed for all final compounds.The evaluation of antimicrobial activity of the compounds against selected Gram(+) and Gram (-) bacteria and fungi was carried out in vitro using microdilution method.For a number of selected compounds, DNA gyrase inhibition assay was alsoperformed, in order to explain the possible mechanism of their antibacterial activity.The in vivo evaluation of anti-inflammatory activity of compounds was carriedout by use of carrageenin induced mouse paw edema model, while selected compoundswere also tested in vitro for their ability to inhibit cycloxygenase (COX 1 and 2).

N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro,in silico and in vivo evaluation

2018 ◽  
Vol 93 (3) ◽  
pp. 364-372 ◽  
Author(s):  
Ajmer Singh Grewal ◽  
Rajeev Kharb ◽  
Deo Nandan Prasad ◽  
Jagdeep Singh Dua ◽  
Viney Lather
Keyword(s):  
In Silico ◽  
In Vivo Evaluation ◽  
Design Synthesis

scholarly journals (E)-2-Cyano-3-(1H-Indol-3-yl)-N-Phenylacrylamide, a Hybrid Compound Derived from Indomethacin and Paracetamol: Design, Synthesis and Evaluation of the Anti-Inflammatory Potential

2020 ◽  
Vol 21 (7) ◽  
pp. 2591
Author(s):  
Pablo Silva ◽  
Maria de Almeida ◽  
Jamire Silva ◽  
Sonaly Albino ◽  
Renan Espírito-Santo ◽  
...  
Keyword(s):  
Condensation Reaction ◽  
Significant Inhibition ◽  
In Vitro Assays ◽  
Paw Edema ◽  
Substituted Anilines ◽  
Hybrid Compound ◽  
Design Synthesis ◽  
Anti Inflammatory

The compound (E)-2-cyano-3-(1H-indol-3-yl)-N-phenylacrylamide (ICMD-01) was designed and developed based on the structures of clinically relevant drugs indomethacin and paracetamol through the molecular hybridization strategy. This derivative was obtained by an amidation reaction between substituted anilines and ethyl 2-cyanoacetate followed by a Knoevenagel-type condensation reaction with indole aldehyde that resulted in both a viable synthesis and satisfactory yield. In order to assess the immunomodulatory and anti-inflammatory activity, in vitro assays were performed in J774 macrophages, and significant inhibitions (p < 0.05) of the production of nitrite and the production of cytokines (IL-1β and TNFα) in noncytotoxic concentrations were observed. The anti-inflammatory effect was also studied via CFA-induced paw edema in vivo tests and zymosan-induced peritonitis. In the paw edema assay, ICMD01 (50 mg kg−1) showed satisfactory activity, as did the group treated with dexamethasone, reducing edema in 2–6 h. In addition, there was no significant inhibition of PGE2, IL-1β or TNFα in vivo. Moreover, in the peritonitis assay that assesses leukocyte migration, ICMD-01 exhibited promising results. Therefore, these preliminary studies demonstrate this compound to be a strong candidate for an anti-inflammatory drug together with an improved gastrointestinal safety profile when compared to the conventional anti-inflammatory drugs.

scholarly journals Design, Synthesis, and Preliminary in Vitro and in Vivo Evaluation ofN-(2-diethylaminoethyl)-4-[18F]fluorobenzamide ([18F]-DAFBA): A Novel Potential PET Probe to Image Melanoma Tumors

2009 ◽  
Vol 20 (3) ◽  
pp. 583-590 ◽  
Author(s):  
Sudha Garg ◽  
Kanchan Kothari ◽  
Shankar R. Thopate ◽  
Aniruddha K. Doke ◽  
Pradeep K. Garg
Keyword(s):  
In Vivo Evaluation ◽  
Design Synthesis

scholarly journals Design, Synthesis, and In Vitro and In Vivo Evaluation of an 18F-Labeled Sphingosine 1-Phosphate Receptor 1 (S1P1) PET Tracer

2016 ◽  
Vol 59 (13) ◽  
pp. 6201-6220 ◽  
Author(s):  
Adam J. Rosenberg ◽  
Hui Liu ◽  
Hongjun Jin ◽  
Xuyi Yue ◽  
Sean Riley ◽  
...  
Keyword(s):  
In Vivo Evaluation ◽  
Design Synthesis ◽  
Pet Tracer ◽  
Sphingosine 1 Phosphate

scholarly journals Design, Synthesis, In Vitro, and Initial In Vivo Evaluation of Heterobivalent Peptidic Ligands Targeting Both NPY(Y1)- and GRP-Receptors—An Improvement for Breast Cancer Imaging?

2018 ◽  
Vol 11 (3) ◽  
pp. 65
Author(s):  
Alicia Vall-Sagarra ◽  
Shanna Litau ◽  
Clemens Decristoforo ◽  
Björn Wängler ◽  
Ralf Schirrmacher ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Imaging ◽  
Breast Cancer Imaging ◽  
In Vivo Evaluation ◽  
Design Synthesis ◽  
Grp Receptors

scholarly journals Design, Synthesis, and in Vitro and in Vivo Evaluation of Ouabain Analogues as Potent and Selective Na,K-ATPase α4 Isoform Inhibitors for Male Contraception

2018 ◽  
Vol 61 (5) ◽  
pp. 1800-1820 ◽  
Author(s):  
Shameem Sultana Syeda ◽  
Gladis Sánchez ◽  
Kwon Ho Hong ◽  
Jon E. Hawkinson ◽  
Gunda I. Georg ◽  
...  
Keyword(s):  
Male Contraception ◽  
In Vivo Evaluation ◽  
Design Synthesis

scholarly journals Design, synthesis, in vitro and in vivo evaluation of tacrine–cinnamic acid hybrids as multi-target acetyl- and butyrylcholinesterase inhibitors against Alzheimer's disease

RSC Advances ◽  
2017 ◽  
Vol 7 (54) ◽  
pp. 33851-33867 ◽  
Author(s):  
Yao Chen ◽  
Hongzhi Lin ◽  
Jie Zhu ◽  
Kai Gu ◽  
Qi Li ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cinnamic Acid ◽  
Cholinesterase Inhibitors ◽  
In Vivo Evaluation ◽  
Design Synthesis

A series of tacrine–cinnamic acid hybrids are synthesized as multi-target cholinesterase inhibitors against Alzheimer's disease.

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