Current Issue : January - March Volume : 2012 Issue Number : 1 Articles : 9 Articles
Cloxacillin is a semi-synthetic penicillin and antibiotic drug. The interaction of sodium salt of cloxacillin with Zn2 and Pb2 ions were studied using cyclic voltammetric and FT-IR techniques. Cyclic voltammogram of Zn2 and Pb2 ions showed characteristic peaks attributed to reduction/ oxidation through crossover, due to the process of nucleation on the surface of working electrode In presence of sodium salt of cloxacillin, the crossover and reduction peak shifted to negative direction where as oxidation towards more positive potential. These results confirmed that the oxidation/reduction of metal ions become more difficult because of formation of some sort of complexes with these molecules. FT-IR spectra showed the formation of cloxacillin-metal complex through the amide, �Ÿ-lactam carbonyls and a carboxylate group....
a-Aminophosphonates are bioisosteres of amino acids and have several pharmacological activities. These compounds have been synthesized by various routes from reaction between amine, aldehyde, and phosphite compounds. In order to synthesize a-aminophosphonates, catalytic effect of CuCl2 was compared with FeCl3. Also all designed structures as well as griseofulvin were docked into the active site of microtubule (1JFF), using Autodock program. The results showed that the reactions were carried out in the presence of CuCl2 in lower yields, and also the time of reaction was longer in comparison with FeCl3. The chemical structures of the new compounds were confirmed by spectral analyses. The compounds were investigated for antifungal activity against several fungi in comparison with griseofulvin. An indole-derived bis(a-aminophosphonates) with the best negative ?G in docking study showed maximum antifungal activity against Microsporum canis, and other investigated compounds did not have a good antifungal activity....
A triazolyl thienyl-cyclohexane II A was discovered as a tractable starting point for a lead optimization effort in a cdk5 kinase inhibition program. SAR studies aided by the identification of selective inhibition of cdk5/p25 versus cdk2/cyclin E. The compounds V A, V B showed moderate where as compounds X A, X B showed significant inhibition of cdk5/p25 and thus have potential for treatment of Alzheimer's disease....
A series of dibenzo[b,e]ox(thi)epin-11(6H)-one O-benzoyloximes has been\nsynthesized and structurally elucidated by means of IR, 1H-NMR, 13C-NMR, MS,\nand elemental analysis. The newly developed compounds were screened at\nconcentrations of 200ââ?¬â??25 g/mL for their antibacterial activity against Gram+ve\norganisms such as Methicillin-Resistant Staphylococcus Aureus (MRSA),\nGramââ?¬â??ve organisms such as Escherichia coli (E. coli), and at the same\nconcentration range for their antifungal activity against fungal strain Aspergillus\nniger (A. niger) by the cup plate method. Ofloxacin and ketoconazole\n(10 g/mL) were used as reference standards for antibacterial and antifungal\nactivity, respectively. The dibenzo[b,e]oxepines 6aââ?¬â??c and 6eââ?¬â??h showed low\nantimicrobial activity (MIC 125ââ?¬â??200 g/mL) compared to the reference\nsubstances, whereas a major improvement (MIC 50ââ?¬â??75 g/mL) was achieved\nwith the synthesis of the corresponding bromomethyl derivative 6d. Moreover,\nreplacement of oxygen by its bioisosteric sulfur led to isomeric dibenzo[b,e]thiepine\nderivatives 6g,h which significantly exhibited higher antimicrobial activity\n(MIC 25ââ?¬â??50 g/mL) against all tested culture strains used in the present study,\ndemonstrating that a change of chemical class from dibenzo[b,e]oxepine to\ndibenzo[b,e]thiepine significantly improves the antimicrobial activity. Further\nvariation, such as the oxidation of the thiepine sulfur to the corresponding\nisomeric dibenzo[b,e]thiepine 5,5-dioxide derivative 9, comparatively failed to\nexhibit high activity (MIC 200 g/mL) against S. aureus, E. coli or A. niger....
The re-emergence of XDR & MDR tuberculosis have claimed human life potentially. We here note down details of designing and synthesis of several pyrimido-thiazolyl triazole derivatives and their evaluation against 25 different clinical isolates. “Hit” is identified through this series of compounds which has shown promising activity compared with Isoniazid. The candidate is under further trials for identifying the toxophore and to avoid untoward effects....
Cyclisation of 1-(2-hydroxyphenyl)-3-substituted phenylprop-2-en-1-ones (1a-h) in pyridine with mercuric acetate gave different 2-benzylidene-1-benzofuran-3(2H)-ones (2a-h) which on subsequent reaction with hydroxylamine hydrochloride afforded 2-benzylidene-1-benzofuran-3(2H)-one oximes (3a-h). These oximes on reaction with benzoylchloride /p-toluene sulphonyl chloride gave two series of compounds 4a-h and 5a-h.The synthesized compounds have been characterized by physical and spectral data. All the compounds have been screened for antileukemic and antibacterial activities....
A series of isonicotinyl hydrazones and their 4- thiazolidinones have been synthesized by condensation of isonicotinic acid hydrazide with various aromatic aldehydes to yield Schiff’s bases, followed by the cyclocondensation of Schiff’s bases with 2-mercaptoacetic acid to yield their 4-thiazolidinones with promising anti-mycobacterial and cytotoxicity activity. All these compounds were evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using the microplate Alamar Blue assay. Among the compounds synthesized, N-(4-oxo-2-strylthiazolidin-3-yl)isonicotinamide (5k) with a stryl ring at the C-2 position of the thiazolidinone ring and N-[2-(4-fluorophenyl)-4-oxo-1,3-thiazolidin-3-yl] pyridine-4-carboxamide (5i) were found to be the most potent compounds with minimum inhibitory concentrations of 4.92 µM and 9.84 µM respectively against Mycobacterium tuberculosis H37 Rv. In the cytotoxicity testing, compound 7f yielded good antiproliferative activity when tested against MDA-MB cell line by MTT assay with GI50 at 131.58µg/ml. The cell viability of the tested compounds determined on Mouse Embryo Cell Line NIH /3T3 indicated that there was no lytic activity at the tested concentration interval of 100-300µg /ml, thereby demonstrating that the compounds were not cytotoxic to the host cell at these concentrations....
Benzimidazole derivates play vital role in biological field such as antimicrobial, antiviral, antidiabetic, and anticancer activity. The potency of these clinically useful drugs in treatment of microbial infections and other activities encouraged the development of some more potent and significant compounds. These compounds carrying different substituents in the benzimidazole structure are associated with a wide range of biological activities. Changes in their structure have offered a high degree of diversity that has proven useful for the development of new therapeutic agents having improved potency and lesser toxicity....
Two dimensional quantitative structure activity relationship (QSAR) study on series of substituted 2-azetidinone derivatives was performed by using V-LIFE MDS 3.0 software. Several statistical expression for 2D QSAR were developed using statistical methods like multiple regeression, principle component regression, partial least square regression etc. Out of several models, the best five 2D QSAR models having highest correlation coefficient and cross validated squared correlation coefficient were selected for further study ( r2>0.7, q2>0.7). QSAR study revealed that Atomic valence connectivity index, element count, electro topological, estate contribution and alignment-independent descriptors are primarily responsible for biological activity. This approach showed that physicochemical descriptor Hydrogencounts, SddsN(nitro)E-index and alignment-independent descriptors T_C_Cl_3 were found to show significant correlation with biological activity in 2-azetidinone derivatives. The information rendered by 2D QSAR models may lead to a better understanding of structural requirements of antibacterial activity and can help in the design of novel potent molecules....
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