Linked Life Data

7452695

Source:http://linkedlifedata.com/resource/pubmed/id/7452695

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
12
pubmed:dateCreated
1981-3-24
pubmed:abstractText
The synthesis of various substituted 5-amino-2-pyridinecarboxylic acids and their derivatives is described by three general methods: (1) reductive alkylation of methyl 5-amino-2-pyridinecarboxylates (2) and subsequent hydrolysis; (2) alkylation of the urethane (9), followed by hydrolysis; and (3) selective NaBH4 reduction of the appropriate amide of (2), followed by hydrolysis. A more specific process was used for the 5-(phenylamino) compound, i.e., nucleophilic displacement of nitrite from methyl 5-nitro-2-pyridinecarboxylate by sodioformanilide and subsequent hydrolysis. Many of these 2-pyridinecarboxylic acid derivatives were potent antihypertensive agents in the spontaneously hypertensive rat (SHR). Optimization of structural parameters for this activity yielded compounds 54, 55, 34, 65, and 22, which were selected for further study in the renal hypertensive dog (RHD). Based on these studies, one compound, 5-[(4-fluorobenzyl)amino]-2-pyridinecarboxylic acid (65), was selected for preclinical toxicity evaluation. Based on the toxicological findings, it was decided not to pursue compound 65 clinically.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
23
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1405-10
pubmed:dateRevised
2008-11-21
pubmed:meshHeading
pubmed:year
1980
pubmed:articleTitle
Synthesis and antihypertensive activity of 5-amino-2-pyridinecarboxylic acid derivatives.
pubmed:publicationType
Journal Article