New 2-substituted-[1,3,4]-oxadiazino-[5,6-b]-indoles have been prepared and tested for their antibacterial, antifungal, H1-antihistaminic and antimuscarinic activities. Among them, compounds 5b, 5d, 5k exhibited higher H1-antihistaminic activity than pheniramine maleate. Compounds 5c, 5d showed higher antibacterial activity than ampicillin against Staphylococcus aureus and E. coli, respectively.
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Pharmazie
December 2002
Department of Pharmaceutical and Medicinal Chemistry, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, India.
New 2-substituted-[1,3,4]-oxadiazino-[5,6-b]-indoles have been prepared and tested for their antibacterial, antifungal, H1-antihistaminic and antimuscarinic activities. Among them, compounds 5b, 5d, 5k exhibited higher H1-antihistaminic activity than pheniramine maleate. Compounds 5c, 5d showed higher antibacterial activity than ampicillin against Staphylococcus aureus and E.
View Article and Find Full Text PDFJ Med Chem
June 1992
Institute of Pharmacy, Freie Universität Berlin, Germany.
The synthesis and biological evaluation of a new class of histamine H2 antagonists with N-cyano-N'-[omega-[3-(1-piperidinylmethyl)phenoxy] alkyl]guanidine partial structure are described as part of an extensive research program to find model compounds for the development of new radioligands with high H2 affinity and specific activity. High receptor affinity is achieved by an additional (substituted) aromatic ring, which is connected with the third guanidine N by a carbon chain spacer and an amine, carboxamide, ester, or sulfonamide link ("polar group"). In functional studies for H2 antagonistic activity and other pharmacological actions [e.
View Article and Find Full Text PDFEur Respir J
October 1989
Institute of Pharmacological Sciences, University of Milan, Italy.
LG 30435 is a new quarternary phenothiazine derivative with H1-antihistaminic and antimuscarinic properties. The ability of LG 30435 to prevent changes in respiratory mechanics, induced by different mediators and the immunological reaction, was monitored together with biological and radioimmunological determination of circulating thromboxane-A2 (TxA2) in anaesthetized guinea-pigs. LG 30435 dose-dependently reduces the bronchoconstriction and TxA2 generation caused by different stimuli such as histamine, acetylcholine, leukotriene C4 (LTC4) and PAF-acether.
View Article and Find Full Text PDFPretreatment of strips of rabbit aorta with 10(-3) M sodium cyanide reduced contractions to 10(-8) through 10(-4) M norepinephrine (NE) added cumulatively. This antagonism by cyanide was not altered by 4 X 10(-6) M ouabain or verapamil, suggesting a lack of involvement of Na+, K+ ATPase or of calcium influx in the antagonism. Cyanide potentiated contractions caused by 3 X 10(-2) M potassium, but reduced contractions induced by higher potassium concentrations.
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