Letters in Drug Design & Discovery - Volume 16, Issue 12, 2019

Background: Monobactam antibiotics have been testified to demonstrate significant antibacterial activity especially the treatment of infections by superbug microbes. Recently, research has been focused on the structural modifications, and new generation of this privileged natural scaffold. Objective: Efforts have been made to discover the structure-antibacterial relationship of monbactams in order to avoid the aimless work Read More

Background: Striatal-enriched Tyrosine Phosphatase (STEP) plays a key role in the mechanisms of neuronal signaling and is a potential molecular target for new generation of psychotropic drugs. STEP inhibitor, 8-(trifluoromethyl-1,2,3,4,5-benzopentathiepin-6-amine hydrochloride (TC-2153), shows anxiolytic effect on mice. Zebrafish (Danio rerio) is a suitable model for the study of anxiety pharmacology. Objective: The objecti Read More

Background: Albendazole is a drug, belongs to the family of benzimidazole, and used as an anthelmintic agent in both human and veterinary medicine. It is marketed as Albenza which is used for the treatment of a variety of parasitic worm infestations such as roundworms, tapeworms, and flukes. In recent past, we have reported various classes of compounds as anti-glycating agents, in continuation of Biology-oriented Read More

Background: Multidrug Resistance (MDR) is a serious hindrance to cancer chemotherapy and profoundly influences the clinical findings. Many Traditional Chinese Medicines (TCM) have been tested with the aim of developing effective resistance modulators or anticancer drugs to overcome the MDR of human cancers. Methods: The anticancer effect of baicalin on multidrug-resistant MC3/5FU (5-fluorouracil) cells was investig Read More

Background: Disaccharide core 1 (Galβ1-3GalNAc) is a common O-glycan structure in nature. Biochemical studies have confirmed that the formation of the core 1 structure is an important initial step in O-glycan biosynthesis and it is of great importance for human body. Objective: Our study will provide meaningful and useful sights for O-glycan synthesis and their bioassay. And all the synthetic glycosides would be used Read More

Background: Breast cancer is the common cause of deaths among women globally with 15% mortality globally. Introduction: Today, about 80% of the rural population depends on natural products as primary health care. Pulicaria crispa (L., family Compositae) is utilized in traditional medicine for curing colds, coughs, colic, and excessive sweating and as a carminative. Methods: The extracts of Pulicaria crispa; grown in Saudi A Read More

Background: Adamantane derivatives possess multiple pharmacological activities such as antiviral, anticancer, antimycobacterial, antidiabetic, antiparkinsonian and others. The interest of medicinal chemists in adamantane compounds is due to their unique spatial structure, high lipophilicity, and carbon cage rigidity. As a result, these molecules can easily penetrate biological lipid membranes and often have unique target-spe Read More

Introduction: The alteration of histone acetylation is a known mechanism to regulate gene expression, and thereby affecting various cellular processes. Histone deacetylases (HDACs) are known to regulate histone acetylation by removal of the acetyl group from lysines. HDAC inhibitor such as Sodium Phenylbutyrate (PB) and Valproic Acid (VPA) have been reported to affect multiple virus infection while whether they aff Read More

Background: The single-agent therapy was unable to provide an effective control of the malignant process, a well-established strategy to improve the efficacy of antitumor therapy is the rational design of drug combinations aimed at achieving synergistic effects. Objective: The objective of this study is generating the new potential anticancer agents with synergistic activity. Owing to the unique mechanism of action of Camptothe Read More

Background: This article describes the challenges in the discovery and optimization of mGlu2/4 heterodimer Positive Allosteric Modulators (PAMs). Methods: Initial forays based on VU0155041, a PAM of both the mGlu4 homodimer and the mGlu2/4 heterodimer, led to flat, intractable SAR that precluded advancement. Screening of a collection of 1,152 FDA approved drugs led to the discovery that febuxostat, an approved xanth Read More