Piperidineacrylate derivatives as potential antiallergy agents. 1993

M Sugiyama, and T Sakamoto, and Y Kamigaki, and H Fukumi, and K Itoh, and Y Satoh, and T Yamaguchi
Medicinal Chemistry Research Laboratory, Sankyo Co., Ltd., Tokyo, Japan.

A new series of piperidineacrylate derivatives was prepared and evaluated for antiallergic activity. Most of the compounds showed potent activities in the rat passive cutaneous anaphylaxis (PCA) assay. In particular, ethyl 1-[2-bis(4-fluorophenyl)methoxyethyl]-4-piperidineacrylate (1a) was more potent than oxatomide and terfenadine in this assay, and was selected for further study. Some pharmacological properties of 1a are presented.

UI MeSH Term Description Entries
D006967 Hypersensitivity Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen. Allergy,Allergic Reaction,Allergic Reactions,Allergies,Hypersensitivities,Reaction, Allergic,Reactions, Allergic
D008297 Male Males
D009682 Magnetic Resonance Spectroscopy Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING). In Vivo NMR Spectroscopy,MR Spectroscopy,Magnetic Resonance,NMR Spectroscopy,NMR Spectroscopy, In Vivo,Nuclear Magnetic Resonance,Spectroscopy, Magnetic Resonance,Spectroscopy, NMR,Spectroscopy, Nuclear Magnetic Resonance,Magnetic Resonance Spectroscopies,Magnetic Resonance, Nuclear,NMR Spectroscopies,Resonance Spectroscopy, Magnetic,Resonance, Magnetic,Resonance, Nuclear Magnetic,Spectroscopies, NMR,Spectroscopy, MR
D010323 Passive Cutaneous Anaphylaxis An evanescent cutaneous reaction occurring when antibody is injected into a local area on the skin and antigen is subsequently injected intravenously along with a dye. The dye makes the rapidly occurring capillary dilatation and increased vascular permeability readily visible by leakage into the reaction site. PCA is a sensitive reaction for detecting very small quantities of antibodies and is also a method for studying the mechanisms of immediate hypersensitivity. Anaphylaxis, Passive Cutaneous,PCA,Cutaneous Anaphylaxis, Passive
D010880 Piperidines A family of hexahydropyridines.
D006168 Guinea Pigs A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research. Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea
D000179 Acrylates Derivatives of acrylic acid (the structural formula CH2
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D017207 Rats, Sprague-Dawley A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company. Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

Related Publications

M Sugiyama, and T Sakamoto, and Y Kamigaki, and H Fukumi, and K Itoh, and Y Satoh, and T Yamaguchi
July 1974, Journal of medicinal chemistry,
M Sugiyama, and T Sakamoto, and Y Kamigaki, and H Fukumi, and K Itoh, and Y Satoh, and T Yamaguchi
June 1989, Journal of medicinal chemistry,
M Sugiyama, and T Sakamoto, and Y Kamigaki, and H Fukumi, and K Itoh, and Y Satoh, and T Yamaguchi
October 1977, Journal of medicinal chemistry,
M Sugiyama, and T Sakamoto, and Y Kamigaki, and H Fukumi, and K Itoh, and Y Satoh, and T Yamaguchi
May 1978, Journal of pharmaceutical sciences,
M Sugiyama, and T Sakamoto, and Y Kamigaki, and H Fukumi, and K Itoh, and Y Satoh, and T Yamaguchi
March 1992, Journal of medicinal chemistry,
M Sugiyama, and T Sakamoto, and Y Kamigaki, and H Fukumi, and K Itoh, and Y Satoh, and T Yamaguchi
July 1991, Journal of medicinal chemistry,
M Sugiyama, and T Sakamoto, and Y Kamigaki, and H Fukumi, and K Itoh, and Y Satoh, and T Yamaguchi
October 2022, Molecules (Basel, Switzerland),
M Sugiyama, and T Sakamoto, and Y Kamigaki, and H Fukumi, and K Itoh, and Y Satoh, and T Yamaguchi
January 2016, Current pharmaceutical design,
M Sugiyama, and T Sakamoto, and Y Kamigaki, and H Fukumi, and K Itoh, and Y Satoh, and T Yamaguchi
July 2022, Pharmaceutics,
M Sugiyama, and T Sakamoto, and Y Kamigaki, and H Fukumi, and K Itoh, and Y Satoh, and T Yamaguchi
February 1994, Farmaco (Societa chimica italiana : 1989),
Copied contents to your clipboard!