Current Issue : January - March Volume : 2011 Issue Number : 1 Articles : 6 Articles
Quinazolin-4-(3H)-one is a versatile lead molecule for the design of potential bioactive agents. The molecular manipulation of a promising lead compound is still a major line of approach for the discovery of new drugs. There has been considerable interest in the development of novel compounds with antibacterial, antifungal, anti-HIV, CNS depressant, antitubercular, anticancer, antioxidant, analgesic, anti-inflammatory, anticonvulsant and antiviral activities. SAR studies have indicated that substitution at position 2 and 3 can modulate activities of the molecule. Therefore many researchers have synthesized these compounds as target structures and evaluated their biological activities. These observation shave been the guiding for the development for new quinazolinones that possesses varied biological activities....
Several approaches have been done so far for the assessment of biological activity of certain molecules before synthesizing them. Successful methods are used to reduce the time, cost and labor. Physical parameters plays important rule in the absorption, distribution, metabolism and excretion (ADME) of a molecule in a biological system. Pre-assessment of those parameters and comparison study with standard can give better idea about ADME of the molecule. Different software has been developed by which we can theoretically check for bioactivity of a molecule towards different receptors. In our present work we have done the comparison study of physical parameters and bioactivity towards different receptors with standard drug. The synthesis was done by using suitable synthetic route and antimicrobial study was performed. IR, NMR, MASS spectral data give the supporting evidence for successful synthesis of desired compounds. From the antimicrobial study it was found that 2-(4-methoxy-5-phenyl-4,5-dihydro-1,3,4-oxadiazol-2-yl)-6,7-diphenylquinoxaline from first series showed highest antifungal activity having closest druglikeness score, physical parameters to standard; 6,7-diphenyl-2-(5-phenyl-1,3,4-oxadiazol-2-yl) quinoxaline from the second series showed nearest druglikeness score, physical parameters to standard and showed highest antibacterial activity. Increase electron density in oxadiazole ring diminishes its antifungal activity and introduces antibacterial activity; as we found it give highest druglikeness score for nuclear receptor legend. Study of physical parameters can be used as an important tool for pre-assessment of its biological activity....
Diclofenac, a non-steroidal anti-inflammatory drug suffers from the side effects of upper GI damage (stomach and duodenum) including lesions ulcers and life threatening perforations and hemorrhage along with short biological half-life. A polymeric prodrug of diclofenac has been synthesized in the present work to overcome the limitations associated with the drug. The diclofenac was coupled to chloro derivative of hydroxy propyl methacrylate (HPMA) to get polymerisable monomeric drug conjugate which was in turn subjected to radicular polymerization to get the polymeric prodrug. The synthesized prodrug was characterized by IR, NMR and Mass spectroscopy. The prodrug was evaluated for its drug content and subjected for in vitro drug release studies in buffer solutions of pH 1.2 and 7.4 mimicking the pH of upper and lower gastro intestinal tract. The drug release studies of the prodrug revealed its potential to release the drug predominantly at lower GI tract and in a sustained manner resulting in reduced GI disturbances and increased biological half life of the drug....
Quantitative Structure Activity Relationship (QSAR) represents an attempt to correlate 2D and 3D properties (descriptors) of compounds with activity. In order to get the relation between various physicochemical descriptors with biological activity, a QSAR study for the antifungal activity of 26 new 1-tolyl-3-aryl-4-methylimidazole-2-thiones against Aspergillus flavus was established with the VLifeMDS 3.5 (VLife sciences Molecular Design Suit Version 3.5) program. With the VLifeMDS 3.5 program more than 1000 different Molecular descriptors were calculated and Stepwise Multiple Linear Regression analysis was performed. The generated model from 16 molecule training set and 10 molecule validation set revealed that polarity of the molecules is governing factor for antifungal activity against Aspergillus flavus. The best model with 4 descriptor was selected which has r2 = 0.84, q2 = 0.63....
In last few decades, though significant progress has been made in the treatment and control strategies of tubercular infections by introducing new diagnostic and monitoring tools and combination therapy, it still continues to be severe problem. Thus with the aim of developing novel molecule with improved potency for treating Mycobacterium tuberculosis H37Rv strain infections and with decreased probability of developing drug resistance, herein we report the synthesis of isatinyl thiazole derivatives, starting from ethyl acetoacetate , by microwave organic reaction enhancement method (MORE) and results of investigations of their antimycobacterial and antimicrobial activities. Many compounds have shown promising activity while others were inactive....
Taking into consideration the aspects of the antimicrobial spectrum and various other problems such as increasing drug resistance etc. associated with the antibiotics from the class of Fluoroquinolones and to search an answer to overcome these problems the concept of complexation is attempted in the present research work. Synthesis of various metal complexes was carried out via formation of Schiff base (ligand) of the Ciprofloxacin -i.e. the parent moiety was first converted in to its respective Schiff base by reacting them with p-Nitroaniline in equimolar ratio, which was then treated with various metal salts for the synthesis of its metal complexes. The formation of ligands and various metal complexes was confirmed by analyzing them for various physical, physico-chemical and analytical parameters. Finally the antibacterial spectrum of the metal complexes thus synthesized was studied against gram positive as well as gram negative bacterial strains using agar plate method and it was found that these metal complexes had shown significant antibacterial activity in the concentrations equal to and near by the minimum inhibitory concentration of the ciprofloxacin determined experimentally....
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