Nonsteroidal antiinflammatory agents. 2. Synthesis of 4',5-disubstituted 3-biphenylylacetic acids and their derivatives with antiinflammatory and analgesic activities. 1981

Y Tamura, and Y Yoshimoto, and K Kunimoto, and S Tada, and S Matsumura, and M Murayama, and Y Shibata, and H Enomoto

A series of 5',5-disubstituted 3-biphenylylacetic acids (5a-n) and several alpha-methyl derivatives (5o-v) were prepared as analogues of a newly developed nonsteroidal antiinflammatory agent, 5'-chloro-5-methoxy-3-biphenylylacetic acid [1 (DKA-9), R = 4-C1Ph; R' = Me], and evaluated for antiinflammatory and analgesic activities using both carrageenan rat paw edema and AcOH writhing assays. Among them, 5-fluoro-3-biphenylylacetic acid (5m) showed the highest antiinflammatory activity, while 2-(3-biphenylyl)propionic acid (5o) showed the highest analgesic activity. However, they were less potent than 1 (R = 4-C1Ph; R' = Me) in these assays.

UI MeSH Term Description Entries
D007213 Indomethacin A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES. Amuno,Indocid,Indocin,Indomet 140,Indometacin,Indomethacin Hydrochloride,Metindol,Osmosin
D007928 Lethal Dose 50 The dose amount of poisonous or toxic substance or dose of ionizing radiation required to kill 50% of the tested population. LD50,Dose 50, Lethal
D008297 Male Males
D010648 Phenylacetates Derivatives of phenylacetic acid. Included under this heading are a variety of acid forms, salts, esters, and amides that contain the benzeneacetic acid structure. Note that this class of compounds should not be confused with derivatives of phenyl acetate, which contain the PHENOL ester of ACETIC ACID. Benzeneacetates,Benzeneacetic Acids,Phenylacetic Acids,Acids, Benzeneacetic,Acids, Phenylacetic
D002621 Chemistry A basic science concerned with the composition, structure, and properties of matter; and the reactions that occur between substances and the associated energy exchange.
D000700 Analgesics Compounds capable of relieving pain without the loss of CONSCIOUSNESS. Analgesic,Anodynes,Antinociceptive Agents,Analgesic Agents,Analgesic Drugs,Agents, Analgesic,Agents, Antinociceptive,Drugs, Analgesic
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
D000893 Anti-Inflammatory Agents Substances that reduce or suppress INFLAMMATION. Anti-Inflammatory Agent,Antiinflammatory Agent,Agents, Anti-Inflammatory,Agents, Antiinflammatory,Anti-Inflammatories,Antiinflammatories,Antiinflammatory Agents,Agent, Anti-Inflammatory,Agent, Antiinflammatory,Agents, Anti Inflammatory,Anti Inflammatories,Anti Inflammatory Agent,Anti Inflammatory Agents
D001713 Biphenyl Compounds Whitish aromatic crystalline organic compounds made up of two conjoined BENZENE rings. Compounds, Biphenyl
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

Y Tamura, and Y Yoshimoto, and K Kunimoto, and S Tada, and S Matsumura, and M Murayama, and Y Shibata, and H Enomoto
December 1987, Il Farmaco; edizione scientifica,
Y Tamura, and Y Yoshimoto, and K Kunimoto, and S Tada, and S Matsumura, and M Murayama, and Y Shibata, and H Enomoto
January 2015, Anti-inflammatory & anti-allergy agents in medicinal chemistry,
Y Tamura, and Y Yoshimoto, and K Kunimoto, and S Tada, and S Matsumura, and M Murayama, and Y Shibata, and H Enomoto
May 1974, Journal of medicinal chemistry,
Y Tamura, and Y Yoshimoto, and K Kunimoto, and S Tada, and S Matsumura, and M Murayama, and Y Shibata, and H Enomoto
October 1977, Journal of medicinal chemistry,
Y Tamura, and Y Yoshimoto, and K Kunimoto, and S Tada, and S Matsumura, and M Murayama, and Y Shibata, and H Enomoto
October 1974, Journal of medicinal chemistry,
Y Tamura, and Y Yoshimoto, and K Kunimoto, and S Tada, and S Matsumura, and M Murayama, and Y Shibata, and H Enomoto
August 1973, Journal of medicinal chemistry,
Y Tamura, and Y Yoshimoto, and K Kunimoto, and S Tada, and S Matsumura, and M Murayama, and Y Shibata, and H Enomoto
March 2005, Archiv der Pharmazie,
Y Tamura, and Y Yoshimoto, and K Kunimoto, and S Tada, and S Matsumura, and M Murayama, and Y Shibata, and H Enomoto
May 1995, Farmaco (Societa chimica italiana : 1989),
Y Tamura, and Y Yoshimoto, and K Kunimoto, and S Tada, and S Matsumura, and M Murayama, and Y Shibata, and H Enomoto
February 2006, European journal of medicinal chemistry,
Y Tamura, and Y Yoshimoto, and K Kunimoto, and S Tada, and S Matsumura, and M Murayama, and Y Shibata, and H Enomoto
April 2001, Farmaco (Societa chimica italiana : 1989),
Copied contents to your clipboard!