13 research outputs found
Synthesis and evaluation of analgesic, anti-asthmatic activity of (E)-1-(8-hydroxyquinolin-7-yl)-3-phenylprop-2-en-1 ones
Abstract Seventeen (E)-1-(8-hydroxyquinolin-7-yl)-3-phenylprop-2-en-1 one derivatives were synthesized via aldol condensation of substituted benzaldehydes with quinoline chalcones starting from 8-hydroxy quinoline. Molecular docking studies were performed on COX-2 protein for analgesic activity and PDE 4 enzyme for anti-asthmatic activity. Docking studies for analgesic activity reveal that the compounds 2 , 4 , 12 , 14 , and 15 showed significant interaction in terms of hydrogen bonding, hydrophobic attachment and van der Waal interaction with COX-2. The docking studies and pharmacological screening indicate that substitution of hydroxyl and conjugated ketone groups on the aldehyde ring and the quinoline ring accelerates analgesia with better binding to active site. Eddy's hot plate method was used to evaluate analgesic activity of the synthesized compounds. Compounds showed a substantial increase in reaction time when compared with standard pentazocin. Compounds 2 , 4 , 7 , 9 and 13 showed significant binding interactions with PDE 4 enzyme and hence were selected for evaluation of anti-asthmatic activity using the goat tracheal chain method. Studies reveal that substitution of the methoxy group at 4th & 5th positions for compounds 2 , 4 & 7 leads to significant percentage inhibition of histamine induced contraction. The synthesized compounds are thus found to be potent as analgesic and anti-asthmatic agents
Mild, efficient and economical oxidative deprotection of allyl aryl ethers
328-333An efficient, economical
procedure for the cleavage of allyl aryl ethers using a catalytic amount of
iodine in dimethyl sulphoxide gives corresponding alcohols or phenols in high
yields under mild condition. The reaction can be performed in air without loss
of variety of oxidisable fuctional groups. Allyl ether of phenols is
selectively deprotected in preference to alcohols. The reaction is highly
regioselective and chemoselective
<span style="font-size:12.0pt;font-family: "Times New Roman";mso-fareast-font-family:"Times New Roman";mso-ansi-language: EN-GB;mso-fareast-language:EN-US;mso-bidi-language:AR-SA" lang="EN-GB">Oxidation of aryl and heteroaryl methyl ketone to aryl and heteroarylglyoxals by using CuCl<sub>2</sub>-DMSO</span>
300-305The oxidation of aryl
methyl ketone and heteroaryl methyl ketone to arylglyoxals and heteroaryl
glyoxal respectively has been carried out by using the cheap and easily
available, non toxic, Lewis acid CuCl2 in DMSO solvent at 70-80°C
within 1-2 hr. The reaction can be performed in air without loss of variety of
oxidisable fuctional group like phenolic OH, hetroaryl ring, aryl substituted
methyl, halo, nitro group, etc
Iodine-mediated direct synthesis of 3-iodoflavones
<p>Molecular iodine has been used for the regioselective, one pot, direct synthesis of 3-iodoflavones from 2′-allyloxy chalcones, 2′-hydroxy chalcones and flavones. Allyl deprotection, cyclization dehydrogenation and α-iodination of 2′-allyloxychalcones has been achieved in a single step to offer 3-iodoflavones.</p
A One-Pot Direct Iodination of the Fischer–Borsche Ring Using Molecular Iodine and Its Utility in the Synthesis of 6‑Oxygenated Carbazole Alkaloids
An
efficient regioselective iodination of the Fischer–Borsche
ring has been achieved using molecular iodine, in a one-pot synthesis.
The acid-, metal-, and oxidant-free conditions of the present method
are highly convenient and practical. Furthermore, the one-pot direct
iodination process is extended to the concise synthesis of glycozoline,
3-formyl-6-methoxy-carbazole, and 6-methoxy-carbazole-3-methylcarboxylate
natural alkaloids. This method has been proven to be tolerant to a
broad range of functional groups, with good to excellent yields
Copper (II) chloride: A regioselective catalyst for oxidative aromatization of pyrazoline, isoxazoline and 3-methyl flavanones
1091-1097A new protocol has
been reported in which a series of pyrazoline, isoxazoline and 3-methyl
flavanone has been conveniently aromatized by using CuCl2.2H2O
in DMSO within a short reaction time in excellent yields. The attraction of
this new protocol is regioselective aromatization of substrate 3i-j and <b style="mso-bidi-font-weight:
normal">5a-e which has been carried out to afford the aromatized product
with O-allyl group intact in excellent yield