Convenient Synthesis of Some New Thiophene, Pyrazole, and Thiazole Derivatives Bearing Biologically Active Sulfonyl Guanidine Moiety

2021 ◽  
pp. 1-19
Author(s):  
Sawsan A. Fouad ◽  
Marwa S. El-Gendey ◽  
Entsar M. Ahmed ◽  
Sadia A. Hessein ◽  
Yousry A. Ammar ◽  
...  
Keyword(s):  
Biologically Active ◽  
Thiazole Derivatives ◽  
Convenient Synthesis ◽  
Guanidine Moiety

A convenient synthesis of unsymmetrically substituted terphenyls of biologically active stilbenes via a double Suzuki cross-coupling protocol

2003 ◽  
Vol 44 (14) ◽  
pp. 3005-3008 ◽  
Author(s):  
Daniele Simoni ◽  
Giuseppe Giannini ◽  
Pier Giovanni Baraldi ◽  
Romeo Romagnoli ◽  
Marinella Roberti ◽  
...  
Keyword(s):  
Cross Coupling ◽  
Biologically Active ◽  
Convenient Synthesis

Novel convenient synthesis of biologically active esters of hydroxylamine

Amino Acids ◽  
2009 ◽  
Vol 38 (2) ◽  
pp. 509-517 ◽  
Author(s):  
Maxim A. Khomutov ◽  
Swati Mandal ◽  
Janne Weisell ◽  
Neiha Saxena ◽  
Alina R. Simonian ◽  
...  
Keyword(s):  
Biologically Active ◽  
Active Esters ◽  
Convenient Synthesis

scholarly journals Synthesis, Characterization, and Biological Evaluation of Some Novel Pyrazolo[5,1-b]thiazole Derivatives as Potential Antimicrobial and Anticancer Agents

Molecules ◽  
2021 ◽  
Vol 26 (17) ◽  
pp. 5383
Author(s):  
Abdulrhman Alsayari ◽  
Abdullatif Bin Muhsinah ◽  
Yahya I. Asiri ◽  
Faiz A. Al-aizari ◽  
Nabila A. Kheder ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
13C Nmr Spectroscopy ◽  
Biological Evaluation ◽  
Anticancer Activities ◽  
Thiazole Derivatives ◽  
1H And 13C Nmr ◽  
Future Design ◽  
Drug Molecules ◽  
Convenient Synthesis ◽  
Leading Compounds

The pharmacological activities of thiazole and pyrazole moieties as antimicrobial and anticancer agents have been thoroughly described in many literature reviews. In this study, a convenient synthesis of novel pyrazolo[5,1-b]thiazole-based heterocycles was carried out. The synthesized compounds were characterized by IR, 1H and 13C NMR spectroscopy and mass spectrometry. Some selected examples were screened and evaluated for their antimicrobial and anticancer activities and showed promising results. These products could serve as leading compounds in the future design of new drug molecules.

scholarly journals Biradical Formation by Deprotonation in Thiazole-Derivatives: The Hidden Nature of Dasatinib

2019 ◽  
Author(s):  
Carlos Heras ◽  
Daniel Reta ◽  
Rosendo Valero ◽  
Guillermo Albareda ◽  
Nicholas Chilton ◽  
...  
Keyword(s):  
Continuous Wave ◽  
Valence Bond ◽  
Biologically Active ◽  
Structural Motif ◽  
Structure Property ◽  
Thiazole Derivatives ◽  
Structure Property Relationship ◽  
Pulse Epr ◽  
Elementary Chemical ◽  
Electronic Ground

The formation of stable organic biradicals by a deprotonation process is reported for a series of conjugated heterocycles that share a Ph-N(H)-2-thiazole structural motif. We characterise the paramagnetic electronic ground state by means of continuous-wave and pulse EPR. We propose a simple valence bond mechanism for a deprotonation-induced formation of paramagnetic organic molecules, based on the interplay between the electronegativity of heteroatomic groups and the recovery of aromaticity to stabilise the biradical species. The Ph-N(H)-2-thiazole motif is found in a variety of biologically active molecules, exemplified here with the anticancer drug Dasatinib, and our results suggest a radical-based mechanism for the protein kinase inhibition activity of the drug. The existence of this structure-property relationship for an elementary chemical motif suggests that biradical species may be more prevalent than previously thought and have an important role in bioorganic chemistry.

Silyl Modification of Biologically Active Compounds. Part 8. Trimethylsilyl Ethers of Hydroxyl-Containing Thiazole Derivatives.

ChemInform ◽  
2003 ◽  
Vol 34 (14) ◽  
Author(s):  
A. Zablotskaya ◽  
I. Segal ◽  
S. Germane ◽  
I. Shestakova ◽  
I. Domracheva ◽  
...  
Keyword(s):  
Biologically Active Compounds ◽  
Biologically Active ◽  
Thiazole Derivatives ◽  
Active Compounds ◽  
Trimethylsilyl Ethers

scholarly journals A Search for Cardiotropic Biologically Active Substances among New Derivatives of R- phenylimin-1,3-thiazole

2018 ◽  
Author(s):  
Lina O. Perekhoda ◽  
Irina V. Drapak ◽  
Marharyta M. Suleiman ◽  
Marina V. Rakhimova ◽  
Svetlana G. Таran ◽  
...  
Keyword(s):  
1H Nmr Spectroscopy ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Hantzsch Reaction ◽  
Thiazole Derivatives ◽  
Laboratory Rats ◽  
Pharmacological Screening ◽  
Derivatives Of ◽  
Active Substances ◽  
Cardiotropic Activity

The purpose of our work was the search for safe and effective biologically active substances of cardiotropic action among 1,3- thiazole derivatives. New derivatives of 1-[(2Z)-2-[R-imin]-4-methyl-3-R1-2,3-dihydro-1,3-thiazole-5-yl]ethan-1-one and ethyl-(2Z)-2-[R-imin]-4-methyl-3-R1-2,3-dihydro-1,3-thiazole-5-carboxylate were synthesized by the Hantzsch reaction. The structure of the compounds obtained was confirmed by 1H NMR spectroscopy and by the elemental analysis. The pharmacological screening showed that the obtained substances possess cardiotropic activity. The cardiotropic properties of the new 1,3-thiazole derivatives were studied on the isolated rings of the thoracic aorta of laboratory rats. A prospective substance 1-[(2Z)-2-[(4-methoxyphenyl)imin]-4-methyl-3-(4-methylpiperazin-1-yl) -2,3-dihydro-1,3-thiazol-5-yl]ethan-1-one hydrochloride, which exhibits cardiotropic activity exceeding the activity of L-carnitine and meldonia has been revealed during pharmacological researches of the substances obtained.

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