Current Issue : July - September Volume : 2012 Issue Number : 3 Articles : 8 Articles
Druglikeness is a qualitative concept used in drug design for how \"druglike\" a substance is with respect to factors like bioavailability. It is estimated from the molecular structure before the substance is even synthesized and tested. The calculation of drug-like property can give us better assumption of biological activity of certain molecule. The theoretical calculation and maintains of certain properties of a molecule can fulfill the parameters which are essential to show certain biological activity. Druglike properties are characteristics of compounds, which need to be in balance to make compounds suitable to act as drugs. Druglikeness may be defined as a complex balance of various molecular properties and structural features which determine whether particular molecule is similar to the known drugs. These properties, mainly hydrophobicity, electronic distribution, hydrogen bonding characteristics, molecule size and flexibility and presence of various pharmacophoric features influence the behavior of molecule in a living organism, including bioavailability, transport properties, affinity to proteins, reactivity, toxicity, metabolic stability and many others....
The study of electrochemical behavior of ciprofloxacin (CPF) is described on a Tyrosine modified carbon paste electrode (TCPE) by using cyclic voltammetry (CV) and differential pulse voltammetric techniques. CV was used to study the influence of pH on peak current and peak potential. The phosphate buffer solution (PBS) of pH 7.0 was found to be reasonable as a supporting electrolyte for assay of the drug. The solution conditions and instrumental parameters were optimized; CPF gave a sensitive oxidation peak at 0.590 V (Vs Ag/AgCl). The peak current varied linearly with increase in the concentration from 20 µM to 80 µM. After being validated, the proposed procedure was successfully applied for the determination of the drug in tablets and human urine with mean recoveries of 99.579 and 98.559%, respectively with detection limit of 4.5µM....
A series of novel 5-methyl-1,3-diphenyl-N-(5-phenyl-1,3,4-oxadiazol-2-yl)-1H-pyrazole-4-carboxamide (5a-e) were synthesized by condensing 2-amino-5-phenyl oxadiazole (4a-c) with ethyl 5-methyl-1,3-diphenyl-1H-pyrazole-4-carboxylic acid (3a-c) using triethylamine. Compounds were screened for antimicrobial activity. The newly synthesized compounds were analyzed by IR, 1H NMR, and elemental analysis. The title compound represents novel class of potent antimicrobial agents....
Benzimidazole derivatives are known for their wide spread pharmacological activities and benzimidazole derived antihistaminics are more widely used group of therapeutic agents in allergic diseases because of their low toxicities. As a part of ongoing effort finding novel Antihistaminics, several N1, 2-substituted benzimidazole derivatives were synthesized and screened for their antihistaminic potential. O-fluoro nitrobenzene condensed with alkyl amines and these condensation products were hydrogenated to get N1-alkyl-o-phenylene diamines. Condensation of substituted o-phenylene diamines with chloro acetic acid gives cyclised intermediates and these intermediates when condensed with N1-alkyl/aryl piperazines gives variously substituted piperazinyl benzimidazole derivatives. The synthesized N1-Alkyl–2(N4- Alkyl/Aryl piperazinyl methyl) Benzimidazole derivatives were screened for antihistaminic activity using Chlorpheniramine maleate (CPM) as reference standard. Interestingly, few synthesized compounds exhibited slight to moderate antihistaminic activity. Based on results obtained we can conclude that these molecules hold potential for further modification as selective Antihistaminics for H1 receptor....
Synthesis and characterization of diazole derivatives has been a developing field within the realm of heterocyclic chemistry for the past several years because of their ready accessibility through synthesis, wide range of chemical reactivity and broad spectrum of biological activity. A new series of benzimidazole derivatives were synthesized and evaluated for their antibacterial and anti fungal activities. Different 2-substituted benzimidazole was treated with benzoyl chloride to form 2-substituted N-benzoyl benzimidazole intermediate which when refluxed with different aniline derivatives for 1-2 hrs gave the comp 2j-2q. The purity of the compounds monitored by TLC .The structures were confirmed on the basis of IR, Mass spectra, 1H NMR spectra. Among the synthesized compounds few compounds have shown promising their antibacterial and anti fungal activities....
Abstracts: Pyrimidine, which is one of the bases of hydrolyzed product of nucleosides is an interesting subject for a medicinal chemist by virtue of its diverse biological activities. Uric acid and its oxidation product, alloxan are among the oldest pyrimidine derivatives of biological interest. Various pyrimidines have been reported as anti inflammatory, analgesic, anti microbial, antiparasitic, and antihistaminic agents. In present scheme, an attempt has been made to synthesize some novel pyrimidine derivatives. The starting compound pyrimidine was synthesized by condensation of various aromatic aldehydes, ethyl cyano acetate, guanidine hydrochloride and NaOH in presence of ethanol. Then those pyrimidine derivatives were subjected benzoylation by using benzoyl chloride, triethyl amine and ethanol. The benzoylated pyrimidine derivatives were treated with phosphorous pentachloride to form chloramino pyrimidine derivatives. Then these chloramino pyrimidine derivatives were treated with sodium azide and sodium acetate in aqueous acetone to yield benzyl tetrazole pyrimidine derivatives. The synthesized compounds were characterized and confirmed by melting point, TLC, IR, 1H NMR and mass spectroscopy and then screened for analgesic and antimicrobial activity. Many compounds have shown promising activity while others were inactive....
A large variety of 1,3,4 substituted oxadiazoles have been found to possess anti-inflammatory, antimicrobial and antitubercular activities. A number of 1,3,4 substituted oxadiazole derivatives have been synthesized and tested for their antimicrobial activities. The chemical structures of the newly synthesized compounds were characterized via IR, 1HNMR and elemental analysis. The compounds synthesized were evaluated for their antimicrobial activity against Gram-positive bacteria (Bacillus subtilis, Staphylococcus aureus), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and fungi (Penicillium notatum, Aspergillus niger, Candida albicans and Aspergillus fumigatus) by well plate method. Ciprofloxacin and ketoconazole were used as standard for bacteria and fungi respectively. The results of preliminary biological tests showed that of these compounds possess good antimicrobial activities with known standard drugs....
A novel series of 4-thiazolidinone (4a-j) was synthesized and characterized by means of TLC, melting point and spectral data like IR, 1HNMR & Mass spectroscopy. Synthesized compounds were screened for their antibacterial activity against four different strains like Staphylococcus aureus (NCIM 2079), Bacillus subtilius (NCIM 2708), Pseudomonas aeruginosa (NCIM 2242) and Escherichia coli (NCIM 2685) with standard drug ampicillin while antifungal activity was determined against strains like Candida albicans(NCIM 22491) with standard drug griseofulvin. Screening of antioxidative capacity was based on ability to scavenge free radicals by DPPH (free radical scavenging activity test).The results were compared to standard substance ascorbic acid. The synthesized compounds (4a-j) showed significant antimicrobial & antioxidant activity. Compound 4e exhibited extremely significant antimicrobial activity and compound 4f showed extremely significant antioxidative activity....
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