Steroidal Indoxyls: Evaluation of Pk, values and anti-inflammatory activity
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Date
2006Author
Kamau, FN
Kibwage, IO
Muriuki, G
Guantai, AN
Chepkwony, H
Hoogmartens, J
Roets, E.
Busson, R
Type
ArticleLanguage
enMetadata
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Three steroidal indoxyls, 3-oxo-16,17-seco-16;.nor-l,4-androstadien-15-(7'-methoxy-2-indoxyliden)17-oic acid, 1-(2'-indoxyliden)-2-nor-l,2-secocholestan-3~ oic acid and 1-(5'- chloro-2-indoxyliden)-2-nor-l,2-secocholestan-3-oic acid were synthesized and screened for anti-inflammatory activity. Their pK. values were also determined using a solubility method. The first compound, 3-oxo-16,17- seco-16-nor-l ,4-androstadien-15-(7' -methoxy-2-indoxyliden) 17 -oic acid, had an EDso value of 15.3 mg/kg and a pK. of 7.09. The cholestane derivative, 1-(2'-indoxyliden)-2-nor-l,2-secocholestan-3-oic acid, and its chloro analogue 1-(5'-chloro-2-indoxyliden)-2-nor-l,2-secocholestan-3-oic acid had EDso values of 16.2 and 22.8 mg/kg, while their pK. values were 6.56 and 7.07, respectively, suggesting that these compounds are relatively weak acids.
Citation
East and Central African Journal ofPhannaceutical Sciences Vol. 9 (2006) 52-57Publisher
Department of Pharmaceutical Chemistry, School of Pharmacy, University of Nairobi 'Department of Pharmacology and Pharmacognosy, School of Pharmacy, University of Nairobi National Quality Control Laboratory, Katholieke Universiteit Leuven, Faculteit Farmaceutische Wetenschappen, Van Evenstraat
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- Faculty of Health Sciences (FHS) [10377]