The pharmacological evaluations of some N-[pyridyl-(phenyl)carbonylamino]hydroxypropyl-1,2,3,6-tetrahy dropyridi nes as potential antiinflammatory agents.
A few novel tetrahydropyridines like benzoylamino-4-hydroxypropyl-1,2,3,6-tetrahydropyridine (THP), 7a (Fig. 1) which had been previously synthesized in our laboratory were tested for their antiinflammatory and hypo/hyperglycemic activities. The tetrahydropyridines contained a hydroxypropyl group in either the 4 or 5 position of the THP ring. Antiinflammatory activities using the Buxco paw edema assay on the male Sprague-Dawley rat model were carried out to investigate if a change in the position of the substituent would produce a corresponding change in the antiinflammatory activities. The two most active analogs that showed significant antiinflammatory activities were N-2-(pyridylcarbonylamino)-4-hydroxypropyl-1,2,3,6-tetrahydropyrid ine, 7b and N-2-(pyridyl-carbonlyamino)-5-hydroxypropyl-1,2,3,6-tetrahydropyri dine, 7f. The other six analogs 7a, 7c, 7d, 7e, 7g and 7h also exhibited antiinflammatory effects in a dose-dependent manner. Compounds 7f and 7h also showed significant hyperglycemic activities when compared with the control.
College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee 32307, USA.
T
T
Wilson
U
U
Onubogu
R
R
Kode
K
K
Redda
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D001786:Blood Glucose / Q000187:drug effects; D002351:Carrageenan; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005079:Excipients; D008297:Male; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
D000893:Anti-Inflammatory Agents; D001786:Blood Glucose; D005079:Excipients; D011725:Pyridines; D002351:Carrageenan