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The synthesis and antiallergic activity in the rat passive cutaneous anaphylactic reaction of a series of 2-phenyl-8-azapurin-6-ones are described. Early in the investigation, a linear free-energy equation was established in which the activity was related to the size and hydrogen bonding capacity of the ortho substituent in the phenyl ring. This relationship was used to provide guidance and limits for subsequent work leading to 2-o-propoxyphenyl-8-azapurin-6-one which is 40 times more potent than disodium cromoglycate. It is suggested that good antiallergic activity in this series is associated with coplanarity of the phenyl group with the azapurin-6-one which would be favored by a high degree of hydrogen bonding.
B J Broughton, and
P Chaplen, and
P Knowles, and
E Lunt, and
S M Marshall, and
D L Pain, and
K R Wooldridge
December 2001,
Farmaco (Societa chimica italiana : 1989),
B J Broughton, and
P Chaplen, and
P Knowles, and
E Lunt, and
S M Marshall, and
D L Pain, and
K R Wooldridge
July 2013,
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B J Broughton, and
P Chaplen, and
P Knowles, and
E Lunt, and
S M Marshall, and
D L Pain, and
K R Wooldridge
October 1983,
Journal of medicinal chemistry,
B J Broughton, and
P Chaplen, and
P Knowles, and
E Lunt, and
S M Marshall, and
D L Pain, and
K R Wooldridge
March 2009,
Bioorganic & medicinal chemistry,
B J Broughton, and
P Chaplen, and
P Knowles, and
E Lunt, and
S M Marshall, and
D L Pain, and
K R Wooldridge
December 1971,
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B J Broughton, and
P Chaplen, and
P Knowles, and
E Lunt, and
S M Marshall, and
D L Pain, and
K R Wooldridge
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B J Broughton, and
P Chaplen, and
P Knowles, and
E Lunt, and
S M Marshall, and
D L Pain, and
K R Wooldridge
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Nucleosides, nucleotides & nucleic acids,
B J Broughton, and
P Chaplen, and
P Knowles, and
E Lunt, and
S M Marshall, and
D L Pain, and
K R Wooldridge
February 1995,
Farmaco (Societa chimica italiana : 1989),
B J Broughton, and
P Chaplen, and
P Knowles, and
E Lunt, and
S M Marshall, and
D L Pain, and
K R Wooldridge
August 2021,
Molecules (Basel, Switzerland),
B J Broughton, and
P Chaplen, and
P Knowles, and
E Lunt, and
S M Marshall, and
D L Pain, and
K R Wooldridge
February 1991,
Bollettino chimico farmaceutico,
