Synthesis of Novel 3-Substituted Pyridothienopyrimidine Derivatives with Biological Evaluation as Antimicrobial Agents

doi:10.1007/s40242-016-6218-z

Chemical Research in Chinese Universities ›› 2016, Vol. 32 ›› Issue (6): 967-972.doi: 10.1007/s40242-016-6218-z

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Synthesis of Novel 3-Substituted Pyridothienopyrimidine Derivatives with Biological Evaluation as Antimicrobial Agents

Farag A. El-Essawy^1,2, Nader M. Boshta², Ayman K. El-Sawaf^3,2, Amal A. Nassar⁴, Mohamed S. Khalafallah²

1. Preparatory Year Deanship, Basic Science Department, Prince Sattam Bin Abdulaziz University, KSA;
2. Chemistry Department, Faculty of Science, Menoufia University, Shebin El-Koam, Egypt;
3. Collage of Science and Humanities, Prince Sattam Bin Abdulaziz University, KSA;
4. Faculty of Education for Girls, Prince Sattam Bin Abdulaziz University, KSA

Received:2016-05-26 Revised:2016-08-19 Online:2016-12-01 Published:2016-08-30
Contact: Farag A. El-Essawy, E-mail:faragelessawy@gmail.com E-mail:faragelessawy@gmail.com
Supported by:
Supported by the Deanship of Scientific Research at Prince Sattam Bin Abdulaziz University(No.2015/01/4713).

Abstract

Abstract:

Novel 3-substituted pyridothienopyrimidine derivatives have been synthesized via the reaction of 2-{7,9-dimethyl-4-oxopyrido[3',2':4,5]thieno[3,2-d]pyrimidin-3(4H)-yl}acetohydrazide(5) with a variety of active reagents and chemicals. Structures of the newly synthesized compounds were established based on spectral data. The resulting pyridothienopyrimidine derivatives were evaluated for their possible antimicrobial activity and some of them represent a new class of potentially antimicrobial compounds, especially compounds 9 and 18 which displayed the highest activity against Gram-positive bacteria, Gram-negative bacteria, and Fungi in MIC range of 0.12-1.95 μg/mL.

Key words: Nitrogen-containing heterocycle, Pyridothienopyrimidine, Thieno[2,3-b]pyridine, Antimicrobial

Farag A. El-Essawy, Nader M. Boshta, Ayman K. El-Sawaf, Amal A. Nassar, Mohamed S. Khalafallah. Synthesis of Novel 3-Substituted Pyridothienopyrimidine Derivatives with Biological Evaluation as Antimicrobial Agents[J]. Chemical Research in Chinese Universities, 2016, 32(6): 967-972.

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Synthesis of Novel 3-Substituted Pyridothienopyrimidine Derivatives with Biological Evaluation as Antimicrobial Agents

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