Current Issue : April - June Volume : 2012 Issue Number : 2 Articles : 11 Articles
The present review focuses on the pharmacological profile of 2- azetidinones with their potential activities. The effect of the structures on the pharmacological activities has been discussed. 2-Azetidinone, a β-lactam four member heterocyclic compound is important for its antimicrobial and antifungal activity. This molecule is gift for patients with high cholesterol. 2-azetidinones were reposted as a potent mechanism based inhibitor of several enzymes like human tryptase, chymase, thrombin, leukocyte elastase, human cytomegalovirus protease and serine protease enzyme. As it has broad spectrum of activities it covers antitubercular, anti-inflammatory, antitumor, anti-HIV, antiparkinsonian, antidiabetic and vasopressin V1a antagonist activity too. 2-azetidinone and its derivaties have opened interesting area of research....
The aryl pyrazole integrated imidazole compounds 9a-g were synthesized by condensing 2-amino-N-methyl-5-ethyl carboxylate imidazole 7 with ethyl 5-methyl-1,3-diphenyl-1H-pyrazole-4-carboxylate 8a-g in presence of anhydrous potassium carbonate and dry acetone. Compounds 9a-g were screened against twelve human pathogens. Among them compound 9f exhibited maximum activity....
We have synthesized mannich bases 1,3,4 oxadiazoles-2-thione using microwave irradiation method, and studied their pharmacological activity. A series of 2, 5 - disubstituted - l, 3, 4 - oxadiazoles were synthesized by refluxing 2-furoic acid with ethanol and conc. H2SO4. The obtained ester (2) with hydrazine hydrate and ethanol was refluxed to give hydrazides (3), reactions of hydrazides (3) with different aromatic acids lead to the formation of 5- furyl- 2-aryl -1, 3, 4-oxadiazoles [R(1-3)]. The hydrazides (3) were also converted to 5-furyl-3- arylmethyl -1,3,4- oxadiazole -2- thione (4) in presence of carbon disulphide and potassium hydroxide . Subsequent reaction of thione with primary or secondary amines in presence of formaldehyde gave the Mannich bases [D (1-3)] by conventional and microwave techniques. The efficiency of microwave assisted organic synthesis has dramatically reduced reaction time and structures were characterized on the basis of IR, NMR and Mass Spectral analysis. All the compounds were screened for in vitro antioxidant activity by DPPH assay method and they have shown positive anti-oxidant activity....
A quantitative structure-activity relationship (QSAR) model of angiotensin-converting enzyme- (ACE-) inhibitory peptides\r\nwas built with an artificial neural network (ANN) approach based on structural or activity data of 58 dipeptides (including\r\npeptide activity, hydrophilic amino acids content, three-dimensional shape, size, and electrical parameters), the overall correlation\r\ncoefficient of the predicted versus actual data points is R = 0.928, and the model was applied in ACE-inhibitory peptides\r\npreparation from defatted wheat germ protein (DWGP). According to the QSAR model, the C-terminal of the peptide was found\r\nto have principal importance on ACE-inhibitory activity, that is, if the C-terminal is hydrophobic amino acid, the peptide�s ACEinhibitory\r\nactivity will be high, and proteins which contain abundant hydrophobic amino acids are suitable to produce ACEinhibitory\r\npeptides. According to the model, DWGP is a good protein material to produce ACE-inhibitory peptides because it\r\ncontains 42.84% of hydrophobic amino acids, and structural information analysis from the QSAR model showed that proteases of\r\nAlcalase and Neutrase were suitable candidates for ACE-inhibitory peptides preparation from DWGP. Considering higher DH and\r\nsimilar ACE-inhibitory activity of hydrolysate compared with Neutrase, Alcalase was finally selected through experimental study....
The small and simple benzothiazole nucleus is present in compounds involved in research aimed at evaluating new products that possess interesting biological activities, such as antitumor, antimicrobial, anti diabetic, anthelmintic, antileishmanial, anticonvulsant and anti-inflammatory. The present review focuses on the benzothiazoles derivatives with potential anti microbial activity that are now in development. In recent year heterocyclic compounds analogues and derivatives have attracted strong interest due to their useful biological and pharmacological properties. Literature revealed that Benzothiazole derivatives may serve as an important model of potent anti microbial agents. When one biological active molecule is linked to another, resultant molecule generally has increased potency. Based on the literature review, the biological profiles of these new generations of benzothiazoles derivatives represent much progress with regards to older compounds....
Eight halogenated N,N�´-diphenethylethylenediamines were synthesized, characterized and evaluated for s1 receptor binding affinity in vitro. Measurements of lipophilicity also were obtained. The substitution pattern on one of the aromatic rings remained constant as 3,4-dichloro, while the substituents on the other aromatic ring were varied to include fluorine, bromine or iodine in either the 2-, 3- or 4- positions. Two main structure activity relationships were observed. First, halogen substitution on the 3- or 4-positions of the aromatic ring conferred higher binding affinities (Ki values 6.35 - 15.82 nM) than the corresponding substitutions at the 2-position (Ki values 12.08 - 43.15 nM). Second, derivatives containing either a bromo or fluoro substituent at a given position showed higher s1 receptor binding affinities than derivatives with a corresponding iodo substituent. The data indicate that s1 receptor affinity for this structural series is sensitive to steric bulk at the 2-position. Log k�´w measurements for the halogenated N,N�´- diphenethylethylenediamines were determined by high performance liquid chromatography, and varied from 2.54 - 3.71. In particular, the 3-fluoro analog exhibited a log k�´w = 2.54 accompanied by a s1 receptor Ki = 7.8 nM. These novel N,N�´-diphenethylethylenediamines warrant further investigation in behavioral assays, and radiolabeled versions may prove suitable for in vivo studies of s1 receptors....
The present study deal with the synthesis of novel Dihydropyrimidinone derivatives from the reaction of N-substituted piperazine and substituted Dihydropyrimidinone in presence of Dimethyl formamide(DMF).All the compounds were characterized using IR,1H-NMR,MS and elementary analysis. They were screened for their antihypertensive activity. Result revealed that compound which contains SO2 between piperazine and DHPM skeletal (7g) was most active compound among the all 9 compounds. Compound 7g which showed nearer to similar activity to standard drug prazosin. Other compound showed good to moderate activity. Structure activity relationship of these compounds showed that piperazine ring should be necessary for the a1A adrenergic receptor blocking activity. Substituted primary aromatic amine attached to Dihydropyrimidinone ring instead of piperazine ring resulted in very less activity....
The rapid emergence of extensively drug resistant tuberculosis (XDR-TB) strains highlights the urgent necessity of finding new classes of drugs to kill Mycobacterium tuberculosis with new mechanisms of action. The scarcity of new TB drugs discovered during the last few decades reflects our limited knowledge of essential metabolic processes in M. tuberculosis outside the repertoire of known targets. In this study, small molecules as siderophore inhibitors represent a potential new class of M. tuberculosis inhibitors. Several of the compounds synthesised were found active with compound 10p emerging as a lead for further development....
The phenyloxy acetamide esters (3-6) were synthesized reacting [3-(trifluoromethyl)phenoxy]acetic acid with ethyl esters of Phenylalanine, Tyrosine, 2-aminopyridine-3-carboxylic acid and 4-aminobenzoic acid. These compounds were hydrolyzed using sodium hydroxide to their respective acids (7-10). The newly synthesized compounds were tested for antimicrobial activity against Escherichia coli, Staphylococcus Aureus, Pseudomonas Aeruginos, Aspergillus Flavus, Chrysosporium Keratinophilum, Candida Albicans and antioxidant activity by DPPH method. Compounds 3, 7, and 8 were most active as antimicrobials and 6 and 10 have shown promising antioxidant activity....
A series of novel flavonoids derivatives containing sulfhydryl groups have been designed, designing for potential FAK inhibitors. Docking simulation was performed to position these compounds into the FAK active site to determine the probable binding model. Simulation results showed that 5-hydroxy-3-(4-hydroxyphenyl)-7-mercapto-4H-chromen- 4-one(4a),7-mercapto-3-(4-methoxyphenyl)-4H-chromen-4-one(4b) and 5-hydroxy-7-mercapto- 2-phenyl- 4H- chromen- 4-one(4c) displayed the most potent biological activity. So the three compounds have been synthesized. Antiproliferative assay results demonstrated that the three compounds own fairly good antiproliferative activity .Therefore compounds 4a, 4b and 4c would be potential anticancer agents....
The Schiff base, 2-[(2,3-dihydro-1H-inden-4-ylimino)methyl]-5-nitrophenol coordinates to Mn(II), Cu(II), Zn(II), and Pd(II)\nions through the phenolic O and imine N atoms. The complexes are characterized by physicochemical and spectroscopic methods.\nThe metal complexes formed as [ML2]xH2O with exception of the Cu(II) complex which is anhydrous. Spectroscopic data\ncorroborate the adoption of a four-coordinate, tetrahedral geometry for theMn(II), and Zn(II) complexes, and a four-coordinate,\nsquare planar geometry for the Cu(II) and Pd(II) complexes. None is an electrolyte in DMSO. The in vitro anticancer activities\nof the metal free ligand, Cu(II), Zn(II), and Pd(II) complexes against MCF-7 (human breast adenocarcinoma) and HT-29 (colon\ncarcinoma) cells reveal that the Pd(II) complex has the best cytotoxic activity against MCF-7 cells with an IC50 of 5.94 Ã?µM, which\nis within the same order of activity as cisplatin. Furthermore, the ligand and the Zn(II) complex exhibit broad-spectrum activity\nagainst two gram-positive bacteria, three gram-negative bacteria, and a fungus with inhibitory zones range of 10.0ââ?¬â??20.0 and 10.0ââ?¬â??\n17.0 mm, respectively....
Loading....