Screening of SdiA Inhibitors from Melia dubia Seeds Extracts Towards the Hold Back of Uropathogenic E.coli Quorum Sensing-Regulated Factors |
Author(s): Vinothkannan Ravichandiran, Karthi Shanmugam and Adline Princy Solomon.
Abstract: Plants have always been a supreme source of drugs and India is endowed with a wide variety of them with high medicinal values. The Quorum Sensing (QS) quenching efficiency of various solvent extracts of Melia dubia seeds was investigated against uropathogenic Escherichia coli (UPEC) to screen the competitive inhibitor of SdiA, a transcriptional activator of quorum sensing in E. coli. In this study, potentiality of five different extracts of Melia dubia seeds for quorum sensing inhibitory activity was investigated against uropathogenic ..
Curcumin Bioconjugates: Studies on Structure-Activity Relationship and Antibacterial Properties against Clinically Isolated Strains |
Author(s): Diwakar Rai, Garima Kumari, Anuradha Singh and Ramendra K Singh.
Abstract: Curcumin bioconjugates, with folic acid, fatty acids and dipeptide, have shown much lower MIC than curcumin against clinically isolated Gram-positive, S.viridians, and Gram-negative bacterial strains, E. coli, P. mirabilis and K. pneumoniae. Polynomial regression analysis was performed to establish a correlation between lipophilicity (logP) and antibacterial activity (pMIC), which showed the efficacy of these molecules against the bacterial strains..
| A QSAR Study on Some Series of Anticancer Tyrosine Kinase Inhibitors |
Author(s): Zaihra Anwer and Satya P Gupta.
Abstract: A quantitative structure-activity relationship (QSAR) study has been made on two different series of anticancer tyrosine kinase inhibitors, namely a series of 4-alkynyl and 4-alkenyl-quinazolines and a series of N-4,6-pyrimidine-Nalkyl- N’-phenyl ureas. For the first series, QSAR results indicate that the activity is controlled by the hydrophobicity of the molecules and molecular connectivity index of the substituent, whereas for the second series of compounds the activity is found to be controlled by the molecular connectivity index of the substituent and some indicator variables.
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Substituted Naphthalen-1-yl-Acetic Acid Hydrazides: Synthesis, Antimicrobial Evaluation and QSAR Analysis |
Author(s): Rakesh Narang, Balasubramanian Narasimhan, Sunil Sharma, Erik De Clercq, Christophe Pannecouque and Jan Balzarini.
Abstract:A series of naphthalen-1-yl-acetic acid benzylidene/(1-phenyl-ethylidene)-hydrazides (1-36) was synthesized and tested, in vitro, for antiviral, antibacterial and antifungal activities. The antibacterial and antifungal screening results indicated that compounds having o-bromo, methoxy and hydroxy substitutents were the most active ones. The results of antiviral evaluation showed that none of the synthesized derivatives inhibited the viral infection at subtoxic concentrations. QSAR investigations revealed that the multi-target QSAR model was more effective in describing the antimicrobial activity than the one-target QSAR models.
| Synthesis, Molecular Docking and Antiamnesic Activity of Selected 2- Naphthyloxy Derivatives |
Author(s): Poonam Piplani, Paramveer Singh and Anuradha Sharma.
Abstract: The present paper describes the design and synthesis of a series of some 2-naphthyloxy derivatives with their antiamnesic activity using mice as the animal model and piracetam as the reference drug. All the synthesized compounds were characterized by spectroscopic techniques and were screened for their efficacy as cognition enhancers by elevated plus maze test and acetylcholinestrase inhibitory assay.
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