F.N. KAMAU, I.0. KIBWAGE,G. MURIUKI, A.N. GUANTAI, H. CHEPKWONY,J, J. HOOGMARTENS, E. ROETS, R. BUSSON. Steroidal Indoxyls: Evaluation of Pk, Values and Anti-inflammatory Activity

Citation:
"F.N. KAMAU, I.0. KIBWAGE,G. MURIUKI, A.N. GUANTAI, H. CHEPKWONY,J, J. HOOGMARTENS, E. ROETS, R. BUSSON. Steroidal Indoxyls: Evaluation of Pk, Values and Anti-inflammatory Activity.". 2006.

Abstract:

Three steroidal indoxyls, 3-oxo-16,17-seco-16-nor-l,4-androstadien-15-(7'methoxy-2-indoxyIiden)17-oic
acid, 1-(2' -indoxyJiden )-2-nor-l ,2-secocholestan-3oic
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-16,17seco-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, l-(rindoxyliden)-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 mgikg, while their pK. values were 6.56 and 7.07, respectively,
suggesting that these compounds are relatively weak acids.

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