Letters in Drug Design & Discovery - Volume 11, Issue 10, 2014

A series of novel salicylic acid-based 1,3,4-oxadiazoles derivatives coupled with chiral oxazolidinones were synthesized to screen for their in vitro antitumor activity against five human cancer cell lines. Some of these compounds showed good antitumor activities with IC50alues ranging from 31.19-57.21 µM. Among the tested compounds 11, 15, 19, 23, 24, and 34 showed broad-spectrum antitumor activity against all the cell l Read More

Cholinesterase plays a vital role in the decline of cholinergic transmission and thus can contribute to the development of Alzheimer’s disease (AD). Thus, compounds that can inhibit acetylcholinesterase (AChe) and butyrylcholinesterase (BuChe) are the potential drugs for the treatment of AD. A series of novel pyrrolopyrimidine derivatives was synthesized and evaluated for their inhibitory activity against cholinesterase by Ellman Read More

A new series of 3',4'-bis(3,4,5-trimethoxyphenyl)-4'H-spiro[indene-2,5'-isoxazol]-1(3H)-one derivatives was designed and synthesized. The cytotoxic effects of the synthesized compounds were evaluated on several different human cancer cells. Among them, compound 9e displayed the most potent in vitro antiproliferative activity with IC50 values of 0.07±0.01 µM on T47D cells. Another potent derivative 9h displayed an IC50 v Read More

Background/Purposes: The objective of this study was to evaluate the inhibitory effects of acetylshikonin on bacteria in periodontal disease and the activities of trypsin-like protease and glycosidic enzyme of P. gingivalis in vitro. Methods: The inhibition activity of acetylshikonin against bacteria was identified by microbial sensitivity tests of broth dilution method on 96-microwell plate. Trypsin-like protease and glycosidic enzyme a Read More

Some 4-aryl-4H-chromenes 3a-h, 5a-g, 7a-g and 9a-g were obtained by reaction of 3-substituted phenol 1, 4, 6 and 8 with α-cyanocinnamonitrile derivatives 2. We explored the structure activity relationship (SAR) of 4-aryl-4Hchromenes with modification at the 4- and 7-positions. The antitumor activity of the synthesized compounds was investigated in comparison with the standard drugs Vinblastine and Doxorubicin us Read More

Trismus-pseudocamptodactyly (TPS) syndrome is a musculoskeletal disorder, caused by mutation in the perinatal MyH8 gene, leading to the incomplete opening of mouth and camptodactyly of fingers upon dorsiflexion of the wrist. MyH8 gene is relevant for muscle regulation, and it plays a significant role in muscle motor function, the hydrolysis of ATP, that is essential for the production of force for muscle movement. To u Read More

Pd/C-Cu mediated alternative and one-pot method has been developed for the synthesis of (Z)-3- methyleneisoindolin-1-ones as potential inhibitors of PDE4. The methodology involved coupling-cyclization of obromobenzamides with a range of terminal alkynes in a single pot to afford the target compounds in acceptable yields. Some of these compounds showed encouraging inhibition of PDE4 when tested in vitro that was suppor Read More

In the present study, 5,5'-(1,4-phenylene)bis[3-(2-thienyl)-4,5-dihydro-1H-pyrazole-1-(4-arylthiazol-2-yl)] derivatives (3a-h) were obtained via the reaction of 5,5'-(1,4-phenylene)bis[3-(2-thienyl)-4,5-dihydro-1H-pyrazole-1- carbothioamide] (2) with phenacyl bromides. The synthesized compounds were investigated for their antimicrobial activity against various bacteria and Candida species. Among these derivatives, 5,5 Read More

Hydrazones are a group of compounds possessing diversified biological activity, anti-inflammatory and analgesic activities. There are also known xanthine derivatives possessing such activity. The aim of our study was to investigate if introduction of hydrazone moiety to 3,7-dimethylpurine-2,6-dion-1-yl acetic and butanoic acid derivatives would enhance the analgesic activity. The designed series of compounds were synthesized Read More

Newer N-(6-substitutedbenzo[d]thiazol-2-yl)-2-((substitutedcarbamothioyl)hydrazinecarboxamides were synthesized having semicarbazone and thioamide as two hydrogen bonding domains attached between proximal and distal aryl rings with a view to explore prospective anticonvulsant candidates. For preliminary screening of synthesized compounds, two convulsant tests i.e. Maximal electroshock (MES) and subcutaneou Read More