ABSTRACT
A series of I-substituted sulfonyl indole -3-pyrazolines [4a-j and 5-a-j] and isoxazolines [6a-j] were prepared and tested for their antimicrobial and anti-inflammatory activities. The preparation of compounds 4-6a-j was achieved by treatment of the corresponding chalcones 3a-j with hydrazine hydrate in absolute ethanol, hydrazine hydrate in the presence of glacial acetic acid, and with hydroxylamine hydrochloride in absolute ethanol. The purified products were screened for their antimicrobial activity towards Gram positive, Gram negative bacteria and fungi and also for their anti-inflammatory activity using the carrageenan-induced rat paw oedema. Evaluation of the compounds revealed remarkable antibacterial activity reflected by their ability to inhibit Gram positive and Gram negative bacteria, and also revealed remarkable anti-inflammatory activity reflected by their ability to reduce the carrageenan-induced inflammation in rats
Subject(s)
Indoles , Pyrazoles/chemistry , Isoxazoles/chemistry , /pharmacology , Anti-Infective Agents/pharmacologyABSTRACT
Tumor cells intensely utilize glutamine as the major source of respiratory fuel. Glutamine-analogue acivicin inhibits tumor growth and tumor-induced angiogenesis in Ehrlich ascites carcinoma. In the present study, antitumor properties of acivicin in combination with glutaminase enzyme is reported. Acivicin along with E. coli glutaminase synergistically reduced in vitro proliferation and matrigel invasion of human MCF-7 and OAW-42 cells. Effects of single and combined treatments with acivicin and glutaminase on angiogenic factors were also analyzed in these cell lines. Co-administration of the treatment agents inhibits the release of VEGF and MMP-9 by cells in culture supernatant significantly than single agent treatments. The result suggests that combination of acivicin with glutaminase may provide a better therapeutic option than either of them given separately for treating human breast and ovarian cancer. However, further studies are required to be conducted in vivo for its confirmation.
Subject(s)
Antimetabolites, Antineoplastic/chemistry , Breast Neoplasms/metabolism , Cell Line, Tumor , Cell Proliferation , Collagen/chemistry , Drug Combinations , Female , Glutaminase/metabolism , Glutamine/chemistry , Humans , Isoxazoles/chemistry , Laminin/chemistry , Matrix Metalloproteinase 9/metabolism , Neoplasm Invasiveness , Ovarian Neoplasms/metabolism , Proteoglycans/chemistry , Tetrazolium Salts/pharmacology , Thiazoles/pharmacology , Vascular Endothelial Growth Factor A/metabolismABSTRACT
Significant increase in polyamines levels in inflamed tissue was observed in the experimental animal models of inflammation. Treatment with dexamethasone positively modulated the levels of polyamines whereas non-steroidal drugs, diclofenac and valdecoxib negatively modulated their levels.
Subject(s)
Animals , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Carrageenan/pharmacology , Cell Proliferation , Cyclooxygenase Inhibitors/pharmacology , Dexamethasone/pharmacology , Diclofenac/pharmacology , Drug Interactions , Inflammation , Isoxazoles/chemistry , Polyamines/chemistry , Rats , Rats, Wistar , Steroids/chemistry , Sulfonamides/chemistryABSTRACT
Some new 2,7-dimethyl-4-[p-[5-aryl-2-pyrazolin-3-yl] anilino] 1, 8-naphthyridines [4a-d] and other related products of the isoxazolines [5a-d] and the pyrimidines [6a-d] were synthesized for the purpose of antimicrobial evaluation. Some representative examples of 4b,c, 5a and 6a showed moderate activity against the growth of Bacillus subtilis, Staphylococcus aureus and Aspergillus niger
Subject(s)
Naphthyridines , Antibiosis , Pyrazoles/chemistry , Isoxazoles/chemistry , Anti-Infective Agents/chemical synthesisABSTRACT
Synthesis of 2-[p-[5-aryl-1-[H or phenyl]-delta2 pyrazolin-3-yl] anilino] benzimidazoles [4a, b], 2-[p-aryl-2-isoxazolin-3-yl] anilino] benzimidazole [5], 2-[p-[6-aryl-2-[oxo or thioxo]-1,2,5,6- tetrahydropyrimidin-4-yl] anilino] benzimidazoles [6a,b] and 2-[p- sulfamoylanilino] benzimidazoles [7a-g] were synthesized. The new compounds showed inhibitory effect against the growth of Gram +ve, Gram -ve bacteria, yeast and fungi