Letters in Drug Design & Discovery - Volume 15, Issue 7, 2018

Background: Coumarins are secondary plant metabolites typically found in the species of Asteraceae, Rutaceae and Umbeliferae families which demonstrate several pharmacological properties, including antioxidant activity. As antioxidants, coumarins are known to influence the formation and uptake of Reactive Oxygen Species (ROS), to reduce the oxidative damage caused by free radicals and to prevent eicosanoid forma Read More

Background: Schiff bases have a broad spectrum of biological activities including antiviral, antibacterial, antifungal, antimalarial, anti-inflammatory antiproliferative and antipyretic properties. 1,3,4-oxadiazoles have been reported to show spectrum of biological activities including such as antiviral, fungicidal, antineoplastic, antimicrobial anti-HIV, antitubercular, antihypoglycemic, antimalarial, antioxidant, analgesic, anti-infl Read More

Background: Ibandronate is a prominent representative of α-hydroxymethylenebisphosphonic acid (dronic acid) derivatives applied in the treatment of bone diseases. Methods: Ibandronate was synthesized from N-methyl-N-pentyl-β-alanine using phosphorus trichloride and phosphorous acid in different ratios, applying sulfolane as the solvent (1.), or under solvent-free conditions (2.), or in ionic liquids as addi Read More

Background: The Wnt signaling is one of the crucial pathways in embryonic development and numerous types of human cancers. Porcupine, as well as the Wnt protein palmitoyltransferase, is essential to the regulation of the Wnt signaling pathway. The aims of this paper are to we use the three-dimensional quantitative structure-activity relationship (3D-QSAR) models to gain indepth comprehension into the structural requiremen Read More

Background: Indole derivatives and 1,2,4-triazolo[3,4-b][1,3,4]thiadiazines are important heterocyclic compounds in medicinal chemistry. They have displayed broad spectrum of biological activities such as anticancer, antimicrobial, antioxidant and anti-inflammatory activities. Objective: The objectives of this research were to synthesize 4-amino-5-mercapto-3-[(5-substituted- 2-methyl-1H-indol-3-yl)methyl]-1,2,4-triazoles and Read More

Background: Pyrazolines have played a pivotal role in antimicrobial and anticancer drug discovery. Moreover, thiazoles have attracted a great deal of interest due to their crucial roles in the lead identification and optimization. Objectives: The purpose of the current work was to design and synthesize new antimicrobial and anticancer agents. Methods: New thiazolyl-pyrazoline derivatives (2a-d) were synthesized via the ring c Read More

Background: A new series of quinazoline linked chalcone conjugates were synthesized and evaluated for their in vitro cytotoxicity. Methods: The quinazoline-chalcone derivatives (13a-r) have been prepared by the Claisen-Schmidt condensation of various substituted benzaldehydes (12a-r) with substituted l-(4-(3,4- dihydroquinazolin-4-ylamino)phenyl)ethanone (11a-b) in the presence of aqueous NaOH. Three potential comp Read More

Objective: In this paper, the synthesis, plasma and microsomal stability, and in vitro and in vivo pharmacological profile of urea derivatives (6a-d) designed by molecular simplification on prototype LASSBio-998 are described. Methodology: Compounds were synthesiized exploring condensation of amine derivatives with cyclohexylisocyanate. Plasma and microsomal stabilities were analyzed by HPLC. Chemical stability was investi Read More

Objectives: The main goal of this paper was to conduct the synthesis to determine cytotoxic activity and to carry out docking studies on new LASSBio-1586 isosteres. LASSBio-1586 is a new combretastatin A4 (CA4) analogue previously identified as a simple antitumor drug candidate, able to inhibit microtubule polymerization with broad in vitro and in vivo cytotoxic activity. Methods: The new isosteres (7b-7h, 8a and 9a) wer Read More

Background: Nano-drug delivery systems as mesoporous silica nanoparticles (MSNs) with unique properties have the potential to improve drug efficacy. The purpose of the present study was to design of CLM loaded MSNs-NH2 to improve the physicochemical properties and antibacterial activity with enhancement delivery to infected tissues. Methods: A large pore amine functionalized MSN (MSNs-NH2) is described here to Read More

Background: Aldose reductase is the key enzyme in the polyol pathway, it is implicated in the development of complications associated with diabetes. Objective: The aim of this review is to classify the medicinal plants and their phytoconstituents used in the inhibition of aldose reductase. Methods: We reviewed 83 papers published between 1997 and 2015 (PubMed and Sciencedirect). All the molecules structures were prov Read More