Synthesis and Pharmacological Evaluation of Piperidine Derivatives with Various Heterocyclic Rings at the 4-Position

• Published in: Chemical & pharmaceutical bulletin Vol. 33; no. 3; pp. 1104 - 1115
• Main Authors: TAKAI, HARUKI, SHUTO, KATSUICHI, HASHIMOTO, TAMOTSU, TERANISHI, MASAYUKI, KUBO, KAZUHIRO, OBASE, HIROYUKI, NAKAMIZO, NOBUHIRO
• Format: Journal Article
• Language: English
• Published: Tokyo The Pharmaceutical Society of Japan 01.01.1985; 公益社団法人日本薬学会; Maruzen; Japan Science and Technology Agency
• Subjects: 1, 2, 3-benzotriazine; 1, 3-benzoxazine; 2, 1, 3-benzothiadiazine; Animals; Anti-Inflammatory Agents; antihypertensive activity; antiinflammatory activity; antiulcer activity; Chemistry; Exact sciences and technology; Female; Heterocyclic compounds; Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms; Male; Organic chemistry; Peptic Ulcer Hemorrhage - prevention & control; piperidine; Piperidines - chemical synthesis; Piperidines - therapeutic use; Preparations and properties; quinazoline; Rats; Rats, Inbred Strains; Stomach Ulcer - prevention & control; Structure-Activity Relationship; Non steroidal antiinflammatory agent; Sulfur nitrogen heterocycle; Nitrogen heterocycle; Six membered ring; Bicyclic compound; Antihypertensive agent; Benzenic compound; Antiulcer agent; Aromatic compound; Biological activity; Oxygen nitrogen heterocycle
• ISSN: 0009-2363; 1347-5223; 1347-5223
• DOI: 10.1248/cpb.33.1104

A series of piperidine derivatives with various heterocyclic rings at the 4-position was prepared and tested for antihypertensive activity and other biological activities. The antihypertensive effects of the present compounds in the spontaneous hypertensive rat were less potent than those of previously reported compounds. However, among the compounds tested for antiulcer activity and antiinflammatory activity, some exhibited interesting properties.