Antimicrobial activity of newly synthesized methylsulfanyl‐triazoloquinazoline derivatives. (25th March 2013)

• Record Type: Journal Article
• Authors: Al‐Salahi, Rashad; Marzouk, Mohamed; Awad, Ghada; Al‐Omar, Mohamed; Ezzeldin, Essam
• Is Part Of: Journal of pharmacy and pharmacology. Volume 65:Number 6(2013:Jun.)
• Page Start: 790
• Page End: 797
• Publication Date: 2013-03-25
• Subjects: Pharmacy -- Periodicals; Pharmacology -- Periodicals; 615.1
• DOI: 10.1111/jphp.12039
• Languages: English
• ISSNs: 0022-3573

Abstract

<abstract abstract-type="main"> <title>Abstract</title> <sec id="jphp12039-sec-0001" sec-type="section"> <title>Objective</title> <p>The aim of this research was to study and evaluate the antimicrobial activity of a novel 2‐methylsulfanyl‐[1, 2, 4]triazolo[1, 5‐<italic>a</italic>]quinazoline and its derivatives. Antibacterial activity of the target compounds was tested against a variety of species of Gram‐positive bacteria such as <italic>Staphylococcus aureus</italic> ATCC 29213, <italic>Bacillus subtilis</italic> ATCC6633, and Gram‐negative bacteria such as <italic>Pseudomonas aeruginosa</italic> ATCC27953 and <italic>Escherichia coli</italic> ATCC 25922. In addition some yeast and fungi, <italic>Candida albicans</italic> NRRL Y‐477 and <italic>Aspergillus niger</italic>, respectively, were screened.</p> </sec> <sec id="jphp12039-sec-0002" sec-type="section"> <title>Methods</title> <p>Antimicrobial tests were carried out by the agar well diffusion method, using 100 μl of suspension containing 1 × 10<sup>8</sup> CFU/ml of pathological tested bacteria, 1 × 10<sup>6</sup> CFU/ml of yeast, and 1 × 10<sup>4</sup> spore/ml of fungi spread on nutrient agar (NA), Sabourand dextrose agar (SDA), and potato dextrose agar (PDA), respectively.</p> </sec> <sec id="jphp12039-sec-0003" sec-type="section"> <title>Key findings</title> <p>The minimum inhibitory concentration (MIC) of the tested compounds was determined using the broth double dilution method (serially diluted technique) in proper nutrient. For comparison, ciprofloxacin and ketoconazole were used as antibacterial and antifungal reference drugs, respectively. Compounds <bold>6, 9</bold>, <bold>13</bold>, <bold>14</bold>, and <bold>11</bold> were found to have the highest broad‐spectrum antibacterial activity against <italic>S. aureus</italic> ATCC 29213, <italic>B. subtilis</italic> ATCC6633 and Gram‐negative bacteria such as <italic>P. aeruginosa</italic> ATCC27953 and <italic>E. coli</italic> ATCC 25922 with MIC values of 6.25 and 12.50 μg/ml.</p> </sec> <sec id="jphp12039-sec-0004" sec-type="section"> <title>Conclusions</title> <p>It was clear that many of the synthesized compounds exhibited good antimicrobial activity. This study has revealed that compounds <bold>6, 9</bold>, <bold>13</bold>, <bold>14</bold>, and <bold>11</bold> have been disclosed as moderate antimicrobial agents. These compounds could be useful as templates for further development through modification or derivatization to design more potent antimicrobial agents<bold>.</bold></p> </sec> </abstract>