Letters in Drug Design & Discovery - Volume 14, Issue 6, 2017

Background: Halogen-substituted thiourea derivatives exert well-documented antimicrobial, antiviral and anticancer properties. Objective: This work evaluates antimicrobial and cytotoxic activities of newly synthesized fluorinated thiourea compounds. Method: Two series of thioureas were obtained by the condensation reaction of 4-amino-1- benzylpiperidine (1a-14a) or furfurylamine (1b-14b) and fluorinated isothiocyanate Read More

Background: A set of novel sulfanyl aminonaphthoquinone derivatives (5a-j) were synthesized starting from 2,3-dichloro-1,4-naphthoquinone (1). The amine substituents were introduced via a nucleophilic substitution at reflux temperature. Subsequent reactions of 2-chloro- 3-arylamino-1,4-naphthoquinones (3a-d) with different thiols (4a-c) led to the formation of the desired amino- and thio- substituted products (5a-j). Meth Read More

Background: On the basis that various substituted salicylamides have shown interesting biological properties, we designed and synthesized new salicylamide derivatives with dipeptide moieties. Methods: The synthesis was based on the gradual building of target molecules and provided optically pure compounds. Conclusion: The obtained compounds were tested for their antiproliferative effect against three leukaemia ce Read More

Background: In recent years, thiazole derivatives incorporated with hydrazone moiety have attracted a great deal of interest due to their pivotal role in the field of current cancer research. Methods: In the present study, new thiazolyl hydrazone derivatives were synthesized via the reaction of 1-(4-phenylcyclohexylidene)thiosemicarbazide with 2-bromoacetophenone derivatives. MTT assay was performed to assess the cytotoxi Read More

Background: In continuation of our research on sonochemistry and due to the importance and application of hydrazones and N-acylhydrazones in drug discovery, in this work we report a new general and efficient synthesis of these classes with different aromatic and heteroaromatic nucleus assisted by ultrasound and their respective anti-tuberculosis and anti-cancer activities. Method: Derivatives 7-chloroquinoline 10 and 12 Read More

Background: Tetrandrine has good pharmacological effects, especially in the treatment of pulmonary hypertension. It has the potential to be valuable for clinical applications, however the poor solubility and the high variability of oral bioavailability greatly limited its development. Our research group prepared a new type of tetrandrine microspheres by using chitosan. However, it was lack of pharmacodynamic evaluati Read More

Background: A series of new class of twenty four 1, 4-benzodizepines were designed and by using molecular docking study with GABAA receptor, high scoring fourteen molecules were synthesized from this library. Binding affinity of ligands towards GABAA was evaluated on the basis of dock score and bonding interactions like hydrogen bonds, hydrophobic bonds and pi-stacking. Methods: All compounds were found to possess Read More

Background: A new series of pyrazole containing 1,4-dihydropyridine derivatives 5a-i and 6a-i were synthesized from substituted acetylated aryls and substituted phenylhydrazine by the multistep reaction. Method: The target compounds 1,4-dihydropyridine derivatives were obtained from green synthesis of 1,3-disubstituted phenyl-1H-pyrazole-4-carbaldehydes 4a-i with ethyl acetoacetate and methyl acetoacetate at highe Read More

Background: This work reports synthesis and in vitro cholinesterase inhibitory activity of novel indole-isoxazole hybrids. Method: The synthetic procedure was started from different ethyl 5-arylisoxazole-3-carboxylate derivatives. Hydrolysis and reaction of the later compound with tryptamine afforded the desired products in good yields. Conclusion: Among the synthesized compounds, N-(2-(1H-indol-3-yl)ethyl)-5-(2- Read More

Background: Matrix metalloproteinase-9 (MMP-9) expression is elevated in neurological diseases, and its up-regulation may exert to the pathogenesis of many neurological disorders. Therefore, inhibition of MMP-9 can be of neuroprotective approach. Objective: The present in silico study carried out to explore the possible neuroprotective potential of Withania somnifera phytochemicals through inhibition of MMP-9. M Read More

Background: Nicotinamide adenine dinucleotide (NAD) is an essential coenzyme that plays crucial roles in energy metabolism, DNA repair and cell death. Due to the high proliferation rate and the high energy necessity in cancer cells, NAD biosynthesis and salvage is required. Owing to the NAD importance in cancer cells, NAD salvage/recycling enzymes are targets for drug discovery. Methods: Herein we focused on NMNAT is a h Read More

Background: Depression is highly prevalent in uremic patients undergoing hemodialysis (HD). We previously found that low free-carnitine levels are associated with depression severity in male patients undergoing HD. However, whether L-carnitine supplementation improves the depression state in male patients undergoing HD remains unclear. Methods: Sixteen male patients undergoing HD were orally administered 900 mg L-car Read More

Background: Alzheimer’s disease is progressive neurodegenerative disease incidence of which has been steadily growing for past decades. Etiology of Alzheimer’s disease consists of multiple micro and macroscopic changes and to this day is not satisfactorily understood. Conventional therapy is based on inhibition of acetylcholinesterase of Alzheimer’s disease is connected with considerable worldwide expenses. Objective: Six clin Read More