Current Issue : October-December Volume : 2013 Issue Number : 4 Articles : 9 Articles
Hetrocyclic compounds are indispensable structural units for both the chemists and the biochemists. There are vast numbers of pharmacologically active heterocyclic compounds in regular clinical use. Oxadiazole are the major compounds of heterocyclic nucleus for the development of new drugs and the drugs of oxadiazole were the first effective chemotherapeutic agent to be employed systemically for prevention and cure of bacterial-infection. This review provides an overview of anticancer activity of oxadiazole ring fused with heterocycles as reported over the past decades. Various cell lines used for anticancer activities are PC3, BGC823 and Bcap-37 cell, A431 human epidermoid cells. Oxadiazole ring have been explored in the past years and is still used for future development of new drugs against many more pathological conditions. Oxadiazole is an important pharmacophore in modern drug discovery....
Benzofuran display a diverse array of pharmacological activities. Literature review of compounds with benzofuran nucleus have wide range of therapeutic uses that include antibacterial, antifungal, analgesic, anti-inflammatory, ulcerogenic, antiproliferative, anticonvulsant, anticholinesterase, cytotoxic, DNA cleavage activities. The purpose of this review is to provide an overview of the pharmacological activities of benzofuran....
Enamours ethno medicinal properties with deficient in scientific evidence of a mangrove species Rhizophora mucronata distributed in Kollidam coast (Southeast coast of India). Therefore, we aimed to identify phyto constituents from alkaloid fraction of R.mucronata using GC-MS and evaluate their cytotoxic effect on HepG2 cells. 25g powdered leave material of R.mucronata used extract alkaloid fraction by acid-base extraction method and subjected to GC-MS analysis. The cytotoxic effect of alkaloid fraction on HepG2 cells at different concentration 20, 40, 60, 80 and l00 ?g/ml was confirmed by MTT assay. As a result 57 phyto-constituents identified from the alkaloids fraction. The major peaks showed eicosane, heptadecane, Diethyl phthalate, N-1-Adanantyl-p-methylbenzalimine and hepta decamine alkaloid derivatives present in significant concentration. The alkaloid fractions also possess cytotoxic effect against HepG2 cells. In conclusion R.mucronata derived alkaloids are potent chemotherapeutic agent at preclinical level....
Dihydro-orotate Dehydrogenase (DHODH) is one type of flavo-enzyme. It catalyse the oxydation of Dihydro-orotate (DHO) to the orotate (ORO) as part of fourth and rate limiting step of ‘de novo’ pyrimidine biosynthetic pathway. It has been proven that the DHODH inhibitors having efficacy for the treatment of Cancer, Malaria and Immunological disorder. This 2-D QSAR studies were performed by using software ChemDraw Ultra-8.0, Openbable-2.2.1, Dragon and Valstat. The value of Q2 for model-1 is 0.718091 and R2 value is 0.77607 and for model-2 Q2 = 0.71141 and R2 = 0.769419. Both models were validated by help of Valstat software....
Pathogenic microbes are responsible for billions of dollars in economic losses worldwide each year. In order to discover new antimicrobial molecules with good antimicrobial activity against P. fumigatus, C. albicans, E. fecalis, P. aeurogenosa, S. aureus, E. coli, S. mutans, K. pneumonia, A. niger. We sought to combine the active substructure of aryl-pyrimidines and aromatic amine derivatives together to design and synthesize novel 2H-4-aryl-aminopyrimidines derivatives.A series of novel 2H-4-aryl-aminopyrimidines derivatives were synthesized. The preliminary biological assays revealed that most of the synthesized compounds exhibit favorable antimicrobial activities against P. fumigates, C. albicans, E. fecalis, P .aeurogenosa, S. aureus, E. coli, S. mutans, K. pneumonia, A. niger .The activity of compounds Ia-Ie, IIa-IIe, IIIa-IIIe, IVa-IVe, Va-Ve, VIa-VIe were characterized and the synthesized compounds showed certain antimicrobial activities against P. fumigatus, .albicans, E. fecalis, P. aeurogenosa, S. aureus, E. coli, S. mutans, K. pneumonia, A. niger....
Pathogenic microbes are responsible for billions of dollars in economic losses worldwide each year. In order to discover new antimicrobial molecules with good activity against P. fumigatus, C. albicans, A. fumigates, E. fecalis, P. aeurogenosa, S. aureus, E. coli, S. mutans, K. pneumonia, A. niger. , we sought to combine the active substructure of aryl-pyrimidines and aromatic amine derivatives together to design and synthesize novel pyrazolo[2,4-d]pyrimidines. A series of novel pyrazolo [2,4-d] pyrimidines were synthesized by MWI (Microwave Irradiation). The synthesized compounds Ii-Ixii, IIi-IIiv, IIIi-IIIii, IVi, Vi were characterized by IR , Mass and NMR . The preliminary biological assays revealed that most of the synthesized compounds exhibit promising antimicrobial activities against A. fumigatus, C. albicans ....
Some new 2,5-disubstituted-1,3,4-oxadiazole derivatives of Naproxen were synthesized by reaction of 2-(6-methoxynaphthalen-2-yl) propanehydrazide and various aromatic acids in the presence of phosphorus oxychloride. The structure were verified on the basis of satisfactory analytical and spectral (IR, (1) H NMR, MS) data. The newly synthesized compounds were evaluated for their in-vivo anti-inflammatory and analgesic activities as per standard protocols. Above study showed that some newly synthesized compounds possess significant analgesic and anti-inflammatory activities....
A series of condensed 4-substituted aryl 2-4-substituted phenloxy methyl 4-oxazol-5-ones (1-12) have been synthesized by condensation of the aryloxy acetyl-amino-acetic acids with suitable aldehydes. The synthesized compounds were evaluated for the antibacterial activity against bacterial strains Escherichia coli (gram negative), staphylococcus aureus (gram positive) and antifungal activity against Aspergillus fumigatus. The aim of this study was to investigate the effect of various substitutions at C-2 and C-4 positions of the oxazolone on antimicrobial activities. Norfloxacine (NOR) and Fluconazole (FL) were used as reference standards. Most of the synthesized compounds showed significant antibacterial activity against gram positive bacteria and antifungal activity; however none of the compounds showed activity against gram negative bacteria....
Synthesis and pharmacological activity of 9-(4-bromophenyl)-7-phenyl-4,6-dihydro-1H-[1,4]diazepino[2,3-g]quinoxaline-2,3-dione is reported. The compounds are synthesized by the cyclization of 6,7-diaminoquinoxaline with different bromochalcones in the presence of alcohol. The structures are confined by IR, 1H NMR, mass and elemental analysis. The synthesized compounds were screened for analgesic, anti-inflammatory and ulcerogenic activities. The compounds had shown mild to good activity. The results had shown that the incorporation of diazepines to quinoxalines has produced good anti-inflammatory activity than analgesic activity....
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