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Raza, Rabia,Saeed, Aamer,Arif, Mubeen,Mahmood, Shamsul,Muddassar, Muhammad,Raza, Ahsan,Iqbal, Jamshed Blackwell Publishing Ltd 2012 Chemical biology & drug design Vol.80 No.4
<P>On the basis of the observed biological activity of the coumarins, a new set of 3‐thiazolocoumarinyl Schiff‐base derivatives with chlorine, hydroxy and methoxy functional group substitutions were designed and synthesized. These compounds were tested against acetylcholinesterase from <I>Electrophorus electricus</I> and butyrylcholinesterase from horse serum and their structure–activity relationship was established. Studies revealed them as the potential inhibitors of cholinesterase (acetylcholinesterase and butyrylcholinesterase). The <B>3f</B> was found to be most potent against acetylcholinesterase with <I>K</I><SUB>i</SUB> value of 1.05 ± 0.3 μ<SMALL>m</SMALL> and <B>3l</B> showed excellent inhibitory action against butyrylcholinesterase with <I>K</I><SUB>i</SUB> value of 0.041 ± 0.002 μ<SMALL>m</SMALL>. The synthesized compounds were also docked into the active sites of the homology models of acetylcholinesterase and butyrylcholinesterase to predict the binding modes of these compounds. It was predicted that most of the compounds have similar binding modes with reasonable binding affinities. Our docking studies have also shown that these synthesized compounds have better interaction patterns with butyrylcholinesterase over acetylcholinesterase. The main objective of the study was to develop new potent and selective compounds, which might be further optimized to prevent the progression of the Alzheimer’s disease and could provide symptomatic treatment.</P>
Lipoxygenase Inhibitory Constituents from Indigofera oblongifolia
Ahsan Sharif,Ejaz Ahmed,Abdul Malik,Naheed Riaz,Nighat Afza,Sarfraz Ahmad Nawaz,Muhammad Arshad,Muhammad Raza Shah,Muhammad Iqbal Choudhary 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.7
Indigin, alkylated xanthene (1) and indigoferic acid (2) have been isolated from the chloroform soluble fraction of Indigofera oblongifolia, along with β-sitosterol (3) and 3-hydroxybenzoic acid (4), which are reported for the first time from this species. Their structures were determined through spectroscopic techniques. Both the new compounds 1 and 2 showed significant activity against enzyme lipoxygenase, while 2 further showed moderate inhibition against BChE.
Lipoxygenase Inhibitory Constituents from Indigofera oblongifolia
Sharif, Ahsan,Ahmed, Ejaz,Malik, Abdul,Riaz, Naheed,Afza, Nighat,Nawaz, Sarfraz Ahmad,Arshad, Muhammad,Shah, Muhammad Raza,Chaudhary, Muhammad Iqbal The Pharmaceutical Society of Korea 2005 Archives of Pharmacal Research Vol.28 No.7
Indigin, alkylated xanthene (1) and indigoferic acid (2) have been isolated from the chloroform soluble fraction of Indigofera oblongifolia, along with $\beta$-sitosterol (3) and 3-hydroxybenzoic acid (4), which are reported for the first time from this species. Their structures were determined through spectroscopic techniques. Both the new compounds 1 and 2 showed significant activity against enzyme lipoxygenase, while 2 further showed moderate inhibition against BChE.