Potential hypotensive agents: Synthesis and hypotensive activity of oxime ethers derived from 1-naphthoxepines and related compounds
The synthesis and pharmacological evaluation of substituted oximino-ethers 1 and 2 of naphth[1,2-b]- and naphth[2,1-b]-oxepin-5-ones (4 and 8) were carried out. The hypotensive activity of oximino-ethers 1 and 2 was evaluated on anaesthetized cats. The results indicated that 1c caused a fall of 80mm/Hg for >100′ at a dose of 5mg/kg iv in anaesthetized cats.
Tandon, Vishnu K.,Kumar, Manoj,Awasthi, Anoop K.,Saxena, Hari O.,Goswamy, Gajendra K.
p. 3177 - 3180
(2007/10/03)
1- and 2-substituted naphthalenes: A new class of potential hypotensive agents
A series of 2-substituted aminomethyloxy naphthalenes 1 and 4-(1-naphthoxy-2-substituted aminomethyl)-butanoic acids 2 were synthesized by Mannich reaction of 4-(2-naphthoxy)-butanoic acid 3 and 4-(1-naphthoxy)-butanoic acid 4 with appropriate secondary amines and para-formaldehyde. The newly synthesized compounds were tested for their hypotensive activity at 5mg/kgiv dose in cats. The results indicated that the analogue 2-(N4-phenyl- N1-piperazino)-methyloxy naphthalene 1d (>N=N4-phenyl- N1-piperazino) was the most active analogue when its hypotensive activity was compared to the reference compound propranolol.
Tandon, Vishnu K.,Singh, Kunwar A.,Goswamy, Gajendra K.
p. 2797 - 2800
(2007/10/03)
An improved two-step regioselective synthesis of naphth- and naphthoxepin-5-ones
An improved regioselective synthesis of naphthoxepin-5-one 1 and naphthoxepin-5-one 2 has been described. The key step is one-step regioselective synthesis of 4-naphthoxybutanoic acids 3 and 4, formed from the corresponding naphthols, and their cyclisation to naphthoxepinones 1 and 2.
Tandon, V. K.,Chhor, R. B.,Goswamy, G. K.
p. 1027 - 1029
(2007/10/03)
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