SYNTHESIS AND QSAR STUDIES ON HYPOTENSIVE N-[3-ARYL(THIO SULFONO)PROPYL]-PIPERAZINES PIPERIDINES

Authors
SAXENA AK RAO J SRIMAL RC AUDRY E CARPY A
Citation
Ak. Saxena et al., SYNTHESIS AND QSAR STUDIES ON HYPOTENSIVE N-[3-ARYL(THIO SULFONO)PROPYL]-PIPERAZINES PIPERIDINES, Indian journal of chemistry. Sect. B: organic chemistry, including medical chemistry, 32(12), 1993, pp. 1249-1257
Citations number
33
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Indian journal of chemistry. Sect. B: organic chemistry, including medical chemistry → ACNP
ISSN journal
03764699
Volume
32
Issue
12
Year of publication
1993
Pages
1249 - 1257
Database
ISI
SICI code
0376-4699(1993)32:12<1249:SAQSOH>2.0.ZU;2-C
Abstract
A series Of 3-aryl(thio/sulfono)propyl]piperazines/piperidines has bee n synthesized and evaluated for hypotensive activity in anaesthetized cats. The QSAR studies indicate that resonance or electronic parameter s for the substituents in the thioaryloxy part are important for hypot ensive activity. The optimum distances between common lipophilic and h ydrophilic zones derived from molecular lipophilicity potential (MLP) calculations are almost attained in the l)piperazin-1-yl]-3-(4-acetami dophenylthio)propane (4), the most active compound.