Open Access and Peer-reviewed
Home Journal Issues Guide for Authors Editorial Board Aims & Scope About Journal News & Announcements


Original Research 


Synthesis and Evaluation of The Thrombolytic Activity of Novel Condensed Pyrimidine Sulfonamide Derivatives

Mazin M. Mohsin, Mahmood J. Jawad, Saif M. Hassan, Samir M. Awad, Yassmine Ali Hussain, Najah R Hadi.

Abstract
Pyrimidine-5-sulfonamides are new organic compounds of wide spectrum activity. A new trend is to incorporate a salicylate moiety in an attempt to enhance a thrombolytic activity. We started this strategy using 2-thiouracil 1 as a blocking unit by its ability to be chlorosulfonated at 5th position by refluxing with chlorosulfonic acid giving sulfonyl derivative 2 which was condensed with three common aromatic amines namingmethyl-4-aminosalicylate, methyl-3-aminobenzoate and methyl-4-aminobenzoate respectively yielding sulfonamide derivatives 3a-c. Moreover, 3a-c derivatives were reacted with chloroacetic acid-producing thiazolopyrimidines 4a-c,which in turn were reacted with p-nitrobenzaldehyde giving arylidine derivatives 5a-c. Also compounds 3a-c were cyclocondensed with anthranilic acid yielding pyrimidoquinazoline derivatives 6a-c. They also were condensed with ethanolamine forming imidazopyrmidine derivatives 7a-c. All the newly synthesized compounds were subjected for thrombolytic evaluation and some of them showed promising activity especially those bearing methyl salicylate moiety as compared to ticlopidine and clopidogrel. We performed different modifications in the thienopyridine chemical structure of ticlopidine and clopidogrel to conclude that the presence of second nitrogen atom in the pyridine ring (yielding pyrimidine moiety) and the presence of the other cycle instead of thienyl ring would lead to enhanced the thrombolytic effect which was maximized by incorporation of a methyl salicylate moiety. We concluded that 4a, 6a, 8a, 7a, 3a, compounds have more potent than both clopidogrel and ticlopidine respectively. They certainly deserve further studying in the future.

Key words: Antiplatelet, condensed pyrimidine sulphonamides; synthesis and evaluation


 
ARTICLE TOOLS
Abstract
PDF Fulltext
How to cite this articleHow to cite this article
Citation Tools
Related Records
 Articles by Mazin M. Mohsin
Articles by Mahmood J. Jawad
Articles by Saif M. Hassan
Articles by Samir M. Awad
Articles by Yassmine Ali Hussain
Articles by Najah R Hadi
on Google
on Google Scholar


How to Cite this Article
Pubmed Style

Mohsin MM, Jawad MJ, Hassan SM, Awad SM, Hussain YA, Hadi NR. Synthesis and Evaluation of The Thrombolytic Activity of Novel Condensed Pyrimidine Sulfonamide Derivatives. doi:http://doi.org/10.31838/ejmcm.07.02.35


Web Style

Mohsin MM, Jawad MJ, Hassan SM, Awad SM, Hussain YA, Hadi NR. Synthesis and Evaluation of The Thrombolytic Activity of Novel Condensed Pyrimidine Sulfonamide Derivatives. http://www.ejmcm.com/?mno=6524 [Access: October 13, 2020]. doi:http://doi.org/10.31838/ejmcm.07.02.35


AMA (American Medical Association) Style

Mohsin MM, Jawad MJ, Hassan SM, Awad SM, Hussain YA, Hadi NR. Synthesis and Evaluation of The Thrombolytic Activity of Novel Condensed Pyrimidine Sulfonamide Derivatives. doi:http://doi.org/10.31838/ejmcm.07.02.35



Vancouver/ICMJE Style

Mohsin MM, Jawad MJ, Hassan SM, Awad SM, Hussain YA, Hadi NR. Synthesis and Evaluation of The Thrombolytic Activity of Novel Condensed Pyrimidine Sulfonamide Derivatives. doi:http://doi.org/10.31838/ejmcm.07.02.35



Harvard Style

Mohsin, M. M., Jawad, . M. J., Hassan, . S. M., Awad, . S. M., Hussain, . Y. A. & Hadi, . N. R. (2020) Synthesis and Evaluation of The Thrombolytic Activity of Novel Condensed Pyrimidine Sulfonamide Derivatives. doi:http://doi.org/10.31838/ejmcm.07.02.35



Turabian Style

Mohsin, Mazin M., Mahmood J. Jawad, Saif M. Hassan, Samir M. Awad, Yassmine Ali Hussain, and Najah R Hadi. 2020. Synthesis and Evaluation of The Thrombolytic Activity of Novel Condensed Pyrimidine Sulfonamide Derivatives. doi:http://doi.org/10.31838/ejmcm.07.02.35



Chicago Style

Mohsin, Mazin M., Mahmood J. Jawad, Saif M. Hassan, Samir M. Awad, Yassmine Ali Hussain, and Najah R Hadi. "Synthesis and Evaluation of The Thrombolytic Activity of Novel Condensed Pyrimidine Sulfonamide Derivatives." doi:http://doi.org/10.31838/ejmcm.07.02.35



MLA (The Modern Language Association) Style

Mohsin, Mazin M., Mahmood J. Jawad, Saif M. Hassan, Samir M. Awad, Yassmine Ali Hussain, and Najah R Hadi. "Synthesis and Evaluation of The Thrombolytic Activity of Novel Condensed Pyrimidine Sulfonamide Derivatives." doi:http://doi.org/10.31838/ejmcm.07.02.35



APA (American Psychological Association) Style

Mohsin, M. M., Jawad, . M. J., Hassan, . S. M., Awad, . S. M., Hussain, . Y. A. & Hadi, . N. R. (2020) Synthesis and Evaluation of The Thrombolytic Activity of Novel Condensed Pyrimidine Sulfonamide Derivatives. doi:http://doi.org/10.31838/ejmcm.07.02.35








AUTHOR LOGIN

REVIEWER LOGIN

Indexed
&
Abstracted


Journal is indexed by the following services:

Scopus
CrossRef
JISC KB+
SHERPA RoMEO
Cengage Learning
Directory of Open Access Journals (DOAJ)
Google Scholar

In addition, all journals are available for harvesting via OAI-PMH.


ABOUT JOURNAL
POLICIES
STATEMENTS

This is an open access journal which means that all content is freely available without charge to the user or his/her institution. Users are allowed to read, download, copy, distribute, print, search, or link to the full texts of the articles in this journal without asking prior permission from the publisher or the author. This is in accordance with the Budapest Open Access Initiative (BOAI) definition of open access.

The articles in European Journal of Molecular & Clinical Medicine are open access articles licensed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc-sa/3.0/) which permits unrestricted, non-commercial use, distribution and reproduction in any medium, provided the work is properly cited.