EventsThe 20th International Electronic Conference on Synthetic Organic Chemistry
Published
This submission belongs to the session b. Bioorganic, Medicinal and Natural Products Chemistry of the event The 20th International Electronic Conference on Synthetic Organic Chemistry
Published date
01 Nov, 2016
Citation
M. Matilde Marques, Mohamed Y Mahgoub, Awatef M. Elmaghraby, Abd-Elfttah A. Harb, Filipa Galego, M. Conceição Oliveira, João Luís Ferreira da Silva, Synthesis and characterization of 2-arylidene derivatives of thiazolopyrimidines with potential biological activity, in Proceedings of The 20th International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 2016, MDPI: Basel, Switzerland, doi: 10.3390/ecsoc-20-b008
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Synthesis and characterization of 2-arylidene derivatives of thiazolopyrimidines with potential biological activity

Awatef M. Elmaghraby 2
Abd-Elfttah A. Harb 2
Filipa Galego 1
M. Conceição Oliveira 1
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1. Centro de Química Estrutural, Instituto Superior Técnico, Universidade de Lisboa, 1049-001 Lisboa, Portugal
2. Chemistry Department, Faculty of Science, South Valley University, Qena 83523, Egypt
Abstract

Aryl-3,4-dihydropyrimidinones (DHPM), thiazolopyrimidines and related heteroaromatic compounds are important classes of N-containing fused heterocycles widely used as key building blocks for pharmaceutical agents due to a wide range of biological activities that include  antimicrobial and antitumor properties[1-6]. As part of a program aimed at preparing new bioactive heterocycles, we designed and synthesized a series of thiazolopyrimidines and their 2-arylidene derivatives. The compounds were fully characterized by 1D- and 2D-NMR, high resolution ESI-MS/MS and single crystal X-ray diffraction analysis, which indicated a consistent Z configuration at the arylidene double bond. In addition, the ESI-MS fragmentation mechanisms for representatives of the DHPM, thiazolopyrimidine, and 2-arylidene-thiazolopyrimidine classes were elucidated. Studies are underway to assess the biological activities of the new compounds.

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Keywords
Aryl-3,4-dihydropyrimidinones
thiazolopyrimidines
biological activity
Manuscript
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