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Paper Information

Journal:   IRANIAN JOURNAL OF PUBLIC HEALTH   AUGUST 2014 , Volume 43 , Number SUPPLEMENT 2; Page(s) 50 To 50.
 
Paper: 

DESIGN AND SYNTHESIS OF NOVEL DIPHENYLUREA DERIVATIVES WITH ANTIMICROBIAL AND ANTIFUNGAL POTENTIAL

 
 
Author(s):  NASSIRI KOPAII NASRIN*
 
* DEPARTMENT OF MEDICINAL CHEMISTRY, SCHOOL OF PHARMACEUTICAL SCIENCES, ISLAMIC AZAD UNIVERSITY, TEHRAN
 
Abstract: 

Background: As regards the halogen, atoms in the pharmacophore structure can be beneficial for antimicrobial activity; therefore, chloro derivatives were chosen to synthesize our target compounds. In view of these observations, we have designed new compounds incorporating with the above pharmacophores together in order to prepare molecules having enhanced antimicrobial and antifungal activity. Therefore, we synthesized new compounds containing urea groups in order to investigate their antibacterial and antifungal activities.
Methods: 4-amino phenyl ethyl ester 1 as a base compound was available. 4-amino phenyl hydrazide 2 was prepared by reaction of hydrazine hydrate with compound 1. 4-amino phenyl hydrazone 6, 7 was prepared by reaction of compound 2 with 3-chlorobenzaldehyde and 4- chlorobenzaldehyde. Target compounds were synthesized by the reaction of compound 6, 7 with corresponding isocyanat.
Results: Thin layer chromatography was used to determine the purity of the compounds synthesized. Definition of the melting points was determined in open capillary tubes for the presented Impurities. Then target compounds were reviewed and approved by the FT-IR and H-NMR spectroscopy based on the number of protons. The activity of target compounds about the protein binding sites was evaluated by using the outodock configuration software.
Conclusion: Because of the existence of both hydrazone and urea pharmacophores in the target compounds their antimicrobial and antifungal activity can be considerable. According to the results of spectroscopic and analytical data and a potent active part of urea; it is anticipated that the final composition for the purpose intended, has been accepted in the invitro tests for antibacterial and antifungal effect.

 
Keyword(s): DIPHENYLUREA, HYDRAZONE, ANTIMICROBIAL, ANTIFUNGAL
 
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