Click-Chemistry-Based Free Azide versus Azido Sugar Detection Enables Rapid In Vivo Screening of Glycosynthase Activity

2021 ◽  
Author(s):  
Ayushi Agrawal ◽  
Chandra Kanth Bandi ◽  
Tucker Burgin ◽  
Youngwoo Woo ◽  
Heather B. Mayes ◽  
...  
Keyword(s):  
Click Chemistry ◽  
In Vivo Screening

Click Chemistry Expedited Radiosynthesis: Sulfur [18F]fluoride Exchange of Aryl Fluorosulfates

2019 ◽  
Author(s):  
Qinheng Zheng ◽  
Hongtao Xu ◽  
Hua Wang ◽  
Wen-Ge Han Du ◽  
Nan Wang ◽  
...  
Keyword(s):  
Click Chemistry ◽  
High Performance ◽  
Isotopic Exchange ◽  
Tumor Imaging ◽  
Radiochemical Yield ◽  
Exchange Method ◽  
Molar Activity ◽  
Positron Emission ◽  
Sulfur Fluoride

The lack of simple, efficient [<sup>18</sup>F]fluorination processes and new target-specific organofluorine probes remains the major challenge of fluorine-18-based positron emission tomography (PET). We report here a fast isotopic exchange method for the radiosynthesis of aryl [<sup>18</sup>F]fluorosulfate based PET agents enabled by the emerging sulfur fluoride exchange (SuFEx) click chemistry. The method has been applied to the fully-automated <sup>18</sup>F-radiolabeling of twenty-five structurally diverse aryl fluorosulfates with excellent radiochemical yield (83–100%) and high molar activity (up to 281 GBq µmol<sup>–1</sup>) at room temperature in 30 seconds. The purification of radiotracers requires no time-consuming high-performance liquid chromatography (HPLC), but rather a simple cartridge filtration. The utility of aryl [<sup>18</sup>F]fluorosulfate is demonstrated by the <i>in vivo</i> tumor imaging by targeting poly(ADP-ribose) polymerase 1 (PARP1).

Synthesis of Novel 3(N,N-dialkylamino)alkyl/phenyl Substituted Thieno [2,3-d]pyrimidinones as H1-Anti-Histaminic and Antimicrobial Agents

2019 ◽  
Vol 15 (1) ◽  
pp. 63-70
Author(s):  
Shiv Dev Singh ◽  
Arvind Kumar ◽  
Firoz Babar ◽  
Neetu Sachan ◽  
Arun Kumar Sharma
Keyword(s):  
Antimicrobial Activity ◽  
Potassium Hydroxide ◽  
Antimicrobial Agents ◽  
Pyrimidine Ring ◽  
Antimicrobial Activities ◽  
Screening Methods ◽  
Chlorpheniramine Maleate ◽  
In Vivo Screening

Background: Thienopyrimidines are the bioisoster of quinazoline and unlike quinazoline exist in three isomeric forms corresponding to the three possible types annulation of thiophene to the pyrimidine ring viz thieno[2,3-d] pyrimidine, thieno[3,2-d] pyrimidine and thieno[3,4-d]pyrimidine. Heterocyclic containing the thienopyrimidinone moiety exhibits various pronounced activities such as anti-hypertensive, analgesic and anti-inflammatory, antiviral, platelet aggregation inhibitory, antiprotozoal bronchodilatory, phosphodiesterase inhibitory, antihistaminic, antipsychotic and antimicrobial activity. Objective: Synthesis of novel 3(N,N-dialkylamino)alkyl/phenyl substituted thieno[2,3-d]pyrimidinones as H1-anti-histaminic and antimicrobial agents. Methods: A series of 3-[(N,N-dialkylamino)alkyl/phenyl]-2-(1H)thioxo-5,6,7,8-tetrahydrobenzo(b) thieno(2,3-d)pyrimidine-4(3H)-ones[4a-d], their oxo analogous [5a-d] and 3-[(N,N-dialkylamino)alkyl]- 2-chlorophenyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidine- 4 (3H)-ones[6a-d]derivative were synthesized from 2-amino-4,5,6,7-tetrahydrobenzo(b)thiophene-3-carboxylic acid by nucleophilic substitution of different N,N-dialkyl alkylene/phenylene diamines on activated 3-acylchloride moiety followed by cyclocondensation with carbon disulfide and ethanolic potassium hydroxide to get [4a-d] and in second reaction by condensation with 4-chlorobenzoyl chloride to get [6a-d] by single pot novel innovative route. The oxo analogous [5a-d] were prepared by treating derivatives [4a-d] with potassium permagnate in ethanolic KOH. The synthesized compound were evaluated for H1-antihistaminic and antimicrobial activities. Results: All synthesized compounds exhibited significant H1-antihistaminic activity by in vitro and in vivo screening methods and data were verified analytically and statistically. The compound 4a, 4b, 5a and 5b showed significant H1-antihistaminiic activity than the reference standard chlorpheniramine maleate. The compound 6d, 6c, 5c and 4c exhibited significant antimicrobial activity.

Synthesis and In Vivo Screening of Isosteviol Derivatives as New Cardioprotective Agents

2021 ◽  
pp. 113396
Author(s):  
Hanyuan Zhang ◽  
Bo Liu ◽  
Geng Xu ◽  
Chao Xu ◽  
E. Ou ◽  
...  
Keyword(s):  
In Vivo Screening

Click-Chemistry Reactions in Radiopharmaceutical Chemistry: Fast & Easy Introduction of Radiolabels into Biomolecules for In Vivo Imaging

2010 ◽  
Vol 17 (11) ◽  
pp. 1092-1116 ◽  
Author(s):  
C. Wangler ◽  
R. Schirrmacher ◽  
P. Bartenstein ◽  
B. Wangler
Keyword(s):  
Click Chemistry ◽  
In Vivo Imaging ◽  
Radiopharmaceutical Chemistry

scholarly journals Biological activity from indigenous medicinal plants of Mauritius

2005 ◽  
Vol 77 (1) ◽  
pp. 41-51 ◽  
Author(s):  
A. Gurib-Fakim ◽  
H. Subratty ◽  
F. Narod ◽  
J. Govinden-Soulange ◽  
F. Mahomoodally
Keyword(s):  
Medicinal Plant ◽  
Plant Extracts ◽  
Biological Properties ◽  
Pharmacological Properties ◽  
Plant Materials ◽  
In Vivo Screening ◽  
Medicinal Plant Extracts ◽  
Minor Ailments

The Mauritian population has a long tradition in the use of ethno-medicine, and the practice is still strong, especially in the treatment of minor ailments. Such interest stems from an existing culture, and many “tisanes” are still prepared from plant materials and sold in several markets around the island.This paper will focus on the various chemical/biological screening techniques currently being used to evaluate the biological properties of medicinal plant extracts. Particular emphasis will be put on extraction and various screening for biological/pharmacological properties. Due consideration will be given to the pharmacological approaches that utilize different animal models for the in vitro and in vivo screening of medicinal plant extracts.

scholarly journals Comparison of In Vitro and In Vivo Screening Models for Androgenic and Estrogenic Activities

2005 ◽  
Vol 89 (1) ◽  
pp. 173-187 ◽  
Author(s):  
Edwin Sonneveld ◽  
Jacoba A. C. Riteco ◽  
Hendrina J. Jansen ◽  
Bart Pieterse ◽  
Abraham Brouwer ◽  
...  
Keyword(s):  
In Vivo Screening

An injectable and self-healing hydrogel with covalent cross-linking in vivo for cranial bone repair

2017 ◽  
Vol 5 (20) ◽  
pp. 3739-3748 ◽  
Author(s):  
Shaoyu Lü ◽  
Xiao Bai ◽  
Haidi Liu ◽  
Piao Ning ◽  
Zengqiang Wang ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Bone Repair ◽  
Cranial Bone ◽  
Cross Linking ◽  
Self Healing

DA click chemistry and dynamic acylhydrazone bond cross-linking are employed to obtain injectable and self-healing hydrogels for cranial bone repair.

scholarly journals In Vivo Screening of Hepatocellular Carcinoma Using AC Susceptibility of Anti-Alpha Fetoprotein-Activated Magnetic Nanoparticles

PLoS ONE ◽  
2012 ◽  
Vol 7 (10) ◽  
pp. e46756 ◽  
Author(s):  
Jen-Jie Chieh ◽  
Kai-Wen Huang ◽  
Yang-De Lee ◽  
Herng-Er Horng ◽  
Hong-Chang Yang ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Magnetic Nanoparticles ◽  
Ac Susceptibility ◽  
Alpha Fetoprotein ◽  
In Vivo Screening
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