Synthesis of some heterocyclic phosphonates and their antibacterial and antifungal activities

Abstract

197-200Fifteen heterocyclic phosphonate derivatives and their starting compounds have been evaluated in vitro for antibacterial and antifungal activities against standard strains: Enterococcus faecalis (ATCC 29212), Staphylococcus aureus (ATCC 2921)), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and yeast-like fungi ; Candida albicans and <span style="font-size:16.0pt; mso-bidi-font-size:10.0pt;font-family:" times="" new="" roman";mso-fareast-font-family:="" "times="" roman";mso-ansi-language:en-us;mso-fareast-language:en-us;="" mso-bidi-language:ar-sa"="">Candida tropicalis. <span style="font-size: 15.0pt;mso-bidi-font-size:9.0pt;font-family:" times="" new="" roman";mso-fareast-font-family:="" "times="" roman";mso-ansi-language:en-us;mso-fareast-language:en-us;="" mso-bidi-language:ar-sa"="">The compounds newly synthesised have been identified by 1H-NMR,FT-IR and micro analysis. Among the tested compounds 12, 13, 16, 17, 18, 22 and 23 are found effective to inhibit the growth of <span style="font-size:16.0pt;mso-bidi-font-size:10.0pt; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" mso-ansi-language:en-us;mso-fareast-language:en-us;mso-bidi-language:ar-sa"="">Candida albicans <span style="font-size:15.0pt;mso-bidi-font-size:9.0pt; font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" mso-ansi-language:en-us;mso-fareast-language:en-us;mso-bidi-language:ar-sa"="">and <span style="font-size:16.0pt;mso-bidi-font-size:10.0pt;font-family: " times="" new="" roman";mso-fareast-font-family:"times="" roman";mso-ansi-language:="" en-us;mso-fareast-language:en-us;mso-bidi-language:ar-sa"="">Candida tropicalis at the MICs between <span style="font-size:14.5pt;mso-bidi-font-size:8.5pt;font-family:Arial;mso-fareast-font-family: " times="" new="" roman";mso-ansi-language:en-us;mso-fareast-language:en-us;="" mso-bidi-language:ar-sa;mso-bidi-font-style:italic"="">100-800 μg/mL. The compounds tested here generally do not exhibit considerable antibacterial activity at the concentration studied (100-800 <span style="font-size:14.5pt;mso-bidi-font-size:8.5pt; font-family:Arial;mso-fareast-font-family:" times="" new="" roman";mso-ansi-language:="" en-us;mso-fareast-language:en-us;mso-bidi-language:ar-sa;mso-bidi-font-style:="" italic"="">μg/mL), <span style="font-size:15.0pt;mso-bidi-font-size: 9.0pt;font-family:" times="" new="" roman";mso-fareast-font-family:"times="" roman";="" mso-ansi-language:en-us;mso-fareast-language:en-us;mso-bidi-language:ar-sa"="">except compound 18 which exhibits antibacterial activity against gram-positive bacteria at the MIC of 400 <span style="font-size:14.5pt;mso-bidi-font-size:8.5pt;font-family:Arial;mso-fareast-font-family: " times="" new="" roman";mso-ansi-language:en-us;mso-fareast-language:en-us;="" mso-bidi-language:ar-sa;mso-bidi-font-style:italic"="">μg/mL.</span