Synthesis and QSAR studies on hypotensive 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines.
A series of 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines has been synthesized and evaluated for hypotensive activity. The QSAR studies indicate that resonance and hydrophobic parameters of the aryl substituents are important for hypotensive activity. The similar role of resonance parameter in describing the variance of 5-HT(2A) receptor binding affinities of these compounds suggests a possible role of 5-HT(2A) receptors in mediating the hypotensive action of title compounds.
Saxena
Anil K
AK
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India. anilsak@gmail.com
Rao
Jyoti
J
Chakrabarty
Ruchika
R
Saxena
Mridula
M
Srimal
R C
RC
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001794:Blood Pressure / Q000187:drug effects; D002415:Cats; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005260:Female; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D051379:Mice; D041681:NIH 3T3 Cells; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology*; D021281:Quantitative Structure-Activity Relationship; D044402:Receptor, Serotonin, 5-HT2A / Q000187:drug effects; D013055:Spectrophotometry, Infrared
D000959:Antihypertensive Agents; D007202:Indicators and Reagents; D010879:Piperazines; D011758:Pyrroles; D044402:Receptor, Serotonin, 5-HT2A