Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives
Nov 09, 2011
DOI: https://doi.org/10.3390/molecules16119386
Published in: Molecules 2011, 16, 9386-9396
Publisher: MDPI
Abstract: A new series of 1,3-thiazole and benzo[d]thiazole derivatives 10–15 has been developed, characterized, and evaluated for in vitro antimicrobial activity at concentrations of 25–200 μg/mL against Gram+ve organisms such as methicillin-resistant Staphylococcus aureus (MRSA), Gram–ve organisms such as Escherichia coli (E. coli), and the fungal strain Aspergillus niger (A. niger) by the cup plate method. Ofloxacin and ketoconazole (10 μg/mL) were used as reference standards for antibacterial and antifungal activity, respectively. Compounds 11 and 12 showed notable antibacterial and antifungal activities at higher concentrations (125–200 μg/mL), whereas benzo[d]thiazole derivatives 13 and 14 were found to display significant antibacterial or antifungal activity (50–75 μg/mL) against the Gram+ve, Gram–ve bacteria, or fungal cells used in the present study. In addition, a correlation between calculated and determined partition coefficient (log P) was established which allows future development of compounds within this series to be carried out based on calculated log P values. Moreover, compounds 13 and 14 show that the optimum logarithm of partition coefficient (log P) should be around 4.
Other Researches
Quality Attributes and In Vitro Bioequivalence of Different Brands of Amoxicillin Trihydrate Tablets
Abstract: Bacterial resistance and antibiotic drug effectiveness can be related to administering generic products with a subtherapeutic dose or poor in vivo drug release. The aim of this study was to investigate whether locally marketed amoxicilli...
Abstract: Objective: To investigate whether particular courses in modern pharmacy curriculum equips enrolled students with knowledge/skills to differentiate between different claims of weight loss products. Methods: Claims from weight loss products...
Evaluation of Certain Pharmaceutical Quality Attributes of Lisinopril Split Tablets
Abstract: Tablet splitting is an accepted practice for the administration of drugs for a variety of reasons, including dose adjustment, ease of swallowing and cost savings. The purpose of this study was to evaluate the physical properties of lisin...
Performances of New Generation of Delayed Release Capsules
Abstract: Objective: The purpose of this study was to verify the claimed acid-resistant properties and other performance indicators for AR Caps (Capsule 5 from CapsCanada) and DRcaps (Capsule 6 from Capsugel) and compare them with the immediate re...
The purpose of this study was to assess the in vitro performances of “vegetable” capsules in comparison to hard gelatin capsules in terms of shell weight variation, reaction to different humidity conditions, resistance to stress in the absence of mo...
A number of 2-((4-ethylphenoxy)methyl)-N-(substituted-phenylcarbamothioyl) benzamides (1a–h) were synthesized via reaction of 2-((4-ethylphenoxy)methyl)benzoyl isothiocyanate (2) as a key intermediate with several substituted primary aromatic amines...
ABSTRACT The purpose of this study was to find out if the pharmacists working in community pharmacy and outpatient pharmacy have undergone any formal education regarding drug information, and to describe the drug information resources available,...
Abstract: Problem statement: Several studies on the synthesis of new nifedipine analogs have been carried out, but the literature reveled that no study on the synthesis and calcium channel blocking activity of the substituted ester with an amide (5-...
Synthesis, Characterization, and Antimicrobial Evaluation of Oxadiazole Congeners
A series of 1,3-oxazole, 1,3-thiazole, isomeric 1,2,4-oxadiazole, 1,3,4-oxadiazole, and 1,2,3,4-tetrazole heterocycles was synthesized. All the compounds shared as a common feature the presence of a 4-hydroxyphenyl substituent. The structures of the...
