Five azo compounds where synthesized by coupling reaction between diazonium salt obtained from aniline and some aromatic compounds. The azo compounds obtained from 1-naphthol and 2-naphthol have excellent yields of 96% and 81% respectively while that obtained from phenol has a moderate yield of 58%. The azo compounds obtained from benzene and toluene on the other hand have shown poor yields of the products (4% and 11% respectively).Structures of the compounds were confirmed by FT-IR, 1H NMR, 13C NMR & UV-Visible. All the azo compounds were screened for bioactivity against Streptococcus faecalis, Pseudomonas aeruginosa and Escherichia coli. The results obtained showed that the azo dye synthesized from coupling aniline and 2-naphthol (coded as C-5) showed the highest activity against the three test organisms. At concentrations of 50µg/ml - 100µg/ ml it has an average inhibition zone of 22mm. Escherichia coli showed the highest resistance against all the tested azo compounds. The azo compounds obtained from coupling aniline with benzeneortoluene are completely inactive against E. coli while others have weak activity against it.
Ibrahim Usman Kutama*, Hadiyyah M. Bello, Idris H. Mahmud, Aminu Ahmed.
Three hydrazone derivatives were synthesized by condensation reaction between 2, 4-dinitrophenylhydrazine (2, 4-DNPH) and some carbonyl compounds. The hydrazones obtained from aldehydes: acetaldehyde and benzaldehyde were found to have higher % yields (65% and 74% respectively) than that obtained from acetone (60%). Structures of the compounds were confirmed by spectral analysis. Measured λmax for all the three hydrazone derivatives fall within the literature values. Antimicrobial screening of all the three compounds showed high activity against Salmonella typhi and Streptococcus faecalis with average zone of inhibition of 25mm. The compounds showed activity against Escherichia coli only at higher concentrations of 100µg/ml and 50µg/ml but become inactive at lower concentrations.
Ibrahim Usman Kutama*, Fatima J. Suleiman, Ibrahim I. Fagge, Aminu Ahmed.
The epidermal growth factor receptor (EGFR) plays an important role in cell survival, growth, differentiation, tumorigenesis. Over expression of EGFR has been observed in different types of cancers such as breast, ovarian, colon. These drugs possess many drawbacks such as Drug resistance, decreased RBC, WBC count. So, it is very important to a medicinal chemist to design such molecules which will overcome those limitations, therefore we designed and synthesized few small molecules targeting the ATP binding pocket of EGFR. In case of most of the EGFR inhibitors, 4-anilino-quinazoline is the responsible pharmacophore for the EGFR inhibitory function. On the other hand, pyrazole is another heterocyclic scaffold which is very much abundant in various types of anti-proliferative agents. By considering the above facts we designed the general molecular frame work based on the Molecular Hybridization approach i.e., a molecular framework containing both of these significant scaffolds: 4-anilinoquinazoline and pyrazole. Here in we have reported the synthesis of two compounds (7a, 7b) with the same general molecular structure, mentioned above. There after we have checked the anti-proliferative activity of these compounds in two different types of cancer cell lines i.e. [HCT 116, PC 3]. Both these compounds have shown potent anticancer activity against these two cell lines, particularly much more effective against [HCT 116] in comparison to [PC 3]. Finally, there is a great possibility for this molecular scaffold to be a new generation EGFR inhibitor.
This paper reports on the designing of the new thiazole derivatives that could useful in development of drug candidate for various medicinal activities. Based on the computer aided drug design the drug likeness predicted through Lipinski rule of five. The cytochrome P450 is an enzyme involved in various metabolic biotransformation’s of endogenous and exogenous substances. The use of computational methods used to develop the CYP450 inhibitors in order to find agent with desired properties. Moreover, the current status of knowledge about the use of the computational approach in studies of ligand-enzyme interactions for CYP450. Research on the inhibitors of CYP450 are designed and calculated its properties like atom properties, bond properties, Torsion properties, angle properties and spectral analysis was also reported.
The pharmaceutical analysis deals with qualification and quantification analysis of active pharmaceutical ingredients in pharmaceutical dosage forms and biological matrices. A good literature survey helps to focus on earlier published research and review papers in order to complete the good review work. Isoproterenol hydrochloride is a non-selective β-adrenoreceptor agonist used as medication in the treatment of bradycardia and asthma. Several reviews and research papers published from various journals have been collected and combined for our review work. In this review, we discuss some analytical techniques such as spectrophotometry, spectrofluorimetry, electrochemical method, high-performance liquid chromatography (HPLC), LC-MS/MS and gas chromatography for quantification of isoproterenol hydrochloride. When compared to other analytical techniques, it was found that the HPLC technique is most preferably used for analysis.
P. Vaikunda Narayana Perumal*, R. Vijayakumar, C. N. Nalini.