Medicinal Chemistry - Volume 5, Issue 5, 2009

The HIV-1 reverse transcriptase (RT) associated ribonuclease H (RNase H) activity hydrolyzes the RNA component of the viral heteroduplex RNA:DNA replication intermediate. Even though this function is essential for viral replication, until now only very few compounds have been reported to inhibit it. Anthraquinones are common secondary metabolites which have diverse biological activities. In particular, some of Read More

The synthesis and docking studies of novel benzo[b][1,8]naphthyridines are described. The docking studies show that the derivatives prefer to bind the AT-rich region of double stranded DNA (ds-DNA). The maximum binding energy -7.16 (kcal/mol) was observed for benzo[b][1,8]naphthyridine-5-thiol 5a and it is a better candidate as an enantioselective binder to ds-DNA than the other derivatives of benzo[b][1,8]naphthyridines. W Read More

We report in this work the antibacterial evaluation of 12 lipophilic fluoroquinolone derivatives containing diaminoalkyl side chains at C-7 position. The compounds were investigated against 15 bacterial strains including Gramnegative and Gram-positive species of clinical and microbiological importance. Three compounds (5, 10 and 11) were as active as or more efficient than gatifloxacin against Gram-positive bacteria M. len Read More

Novel 2-[3-(4-bromo-2-fluorobenzyl)-4-oxo-3,4-dihydro-1-phthalazinyl]acetic acid hydrazones were synthesized from phthalic anhydride by a six step synthesis and evaluated for in vitro, in vivo activities against eight mycobacterial species and Mycobacterium tuberculosis (MTB) isocitrate lyase (ICL) enzyme inhibition studies. Among twenty six compounds N'1-[(4-nitrophenyl)methylene]-2-[3-(4-bromo-2-fluorobenzyl)-4-oxo- Read More

Staphyloccoccus aureus, Escherichia coli, Pseudomona aeruginosa Klebsiella pneumoniae, Acinetobacter baumannii, Enetrobacter cloacae and more bacterias have shown resistance to antibiotics in Colombia, therefore, resistance to antibiotics is a problem that is on increase in Colombia. The resistance mechanism to penicillin antibiotics in these bacterias is the expression of β-Lactamase enzyme. In order to use the penici Read More

Cyclooxygenase inhibitory and selectivity profile of a combined series of thirty one aryl sulphonamide compounds possessing 4-benzylideneamino or 4-phenyliminomethyl scaffolds were subjected to QSAR study using Hansch approach. The compounds in the selected series were characterized using classical aromatic substituent constants like hydrophobicity (p), molar refractivity (MR), Hammett electronic (s), electronic field eff Read More

QSAR study was carried out for a series of piperazinyl phenylalanine derivatives exhibiting VLA-4/VCAM-1 inhibitory activity to find out the structural features responsible for the biological activity. The QSAR study was carried out on V-life Molecular Design Suite software and the derived best QSAR model by partial least square (forward) regression method showed 85.67% variation in biological activity. The statistically significant mo Read More

QSAR study on N- (Aryl)-4-(azolylethyl) thiazole-5-carboxamides analogues, which are novel potent inhibitor of VEGF receptor II and I, were performed using topological, electronic and physicochemical descriptors. The results obtained demonstrate in detail, which specify that topological descriptors of the compounds play a significant role in developing QSAR models. The significance of presence and absence of substituen Read More

Objectives: To study the mechanisms underlying cerebrogenic multiple organ dysfunction syndrome (CMODS) through investigation of endotoxin levels and the expression of endotoxin receptor CD14 and interleukin IL-1β mRNAs in a rat CMODS model. Methods: Acute cerebral hemorrhage was induced in Wistar rats by focal intracerebral injection of collagenase into the caudate nucleus. Serum endotoxin levels were quantit Read More

6-Fluoro-3-oxo-indan-1-acetic acid (5) and 6-fluoroindan-1-acetic acid (6) were conveniently synthesised from 3-fluorobenzaldehyde in four and five steps, respectively. The structures of these new compounds and two other intermediates, 3-fluorobenzylidine-bis-acetoacetate (2) and 3-fluoro-β-phenyl glutaric acid (3) were elucidated by spectroscopic means, notably, HRMS, 1D and 2D NMR. The analgesic activity of compounds 5 Read More

Non-transferrin bound iron (NTBI) is detectable in plasma of β-thalassemia patients and participates in freeradical formation and oxidative tissue damage. Desferrioxamine (DFO), deferiprone (DFP) and deferasirox (DFX) are iron chelators used for treatment of iron overload; however they may cause adverse effects. Curcuminoids (CUR) exhibits many pharmacological activities and presents β-diketone group to bind metal i Read More

This study assessed the effect of the antidepressants, Fluoxetine and Venlafaxine, on the size (GS), mass (M), cellular volume (CV), of rat parotid salivary glands and salivary flow rate (SFR), as well as the secretagogue action of pilocarpine on this flow. Ninety animals were divided into 9 treatment groups with the antidepressants, antidepressants associated with the application of pilocarpine, antidepressants and physiolo Read More