Letters in Drug Design & Discovery - Volume 20, Issue 3, 2023

The utilization of biomaterials in the human body was first practiced several years ago to restore normal functional activities by replacing the impaired organs with bio-inspired materials without devastating the cells and tissues. Today, many advanced technologies are reported to be worthwhile to effectively prepare different categories of biomaterials with amplified properties and characteristics for therapeutic applic Read More

Background: Even with the massive increase in financial investments in pharmaceutical research over the last decade, the number of new drugs approved has plummeted. As a result, finding new uses for approved pharmaceuticals has become a prominent alternative approach for the pharmaceutical industry. Objective: Drug repurposing or repositioning is a game-changing development in the field of drug research tha Read More

Objective: Thymus transcaspicus (Lamiaceae) is an Iranian species of Thymus, and Ungernia trisphaera Bunge belongs to the family Amaryllidaceae. Cytotoxic properties of total ethanolic extract of T. transcaspicus and U. trisphaera were investigated against different cell lines including B16F10, PC3, U87, and MCF-7. Methods: The proliferation, cell cycle, and migration of the cells were determined by thiazolyl bl Read More

Background: Kelch-like protein 22 (KLHL22) was a newly discovered proto-oncogene and it is highly expressed in multiple breast cancer cell lines. Inhibition of KLHL22 can induce autophagy in tumor cells by regulating the mTORC1 pathway. Methods: In this study, the structure of the KLHL22 protein was predicted by homology modelling. The model was evaluated by Ramachandran Plot and Profile-3D. Virtual screening of a dr Read More

Aim: Frequent use of antibiotics is responsible for the development of antibiotic resistance; thus, there is an urgent need for the development of new antibacterial agents that act by novel mechanism pathways. Objective: The aim of the study was to develop hybrid novel 4-aminoquinoline 1,3 5-triazine derivatives and determine their antibacterial activity. Methods: Novel hybrid 4-aminoquinoline 1,3,5-triazine derivatives were s Read More

Background: Plasmodium falciparum dihydroorotate dehydrogenase (PfDODH) is one of the enzymes currently explored in the treatment of malaria. Although there is currently no clinically approved drug targeting PfDODH, many of the compounds in clinical trials have [1, 2, 4,] triazolo [1, 5-a] pyrimidin- 7-amine backbone structure. Objective: This study sought to design new compounds from the fragments of known ex Read More

Background: Bacterial infections caused by multidrug-resistant bacteria have emerged as major threats to human communities worldwide. There is a great need to develop new mechanisms by which anti-bacterial agents can combat bacterial antibiotic resistance. Objective: This study aims to synthesize and characterize a series of novel tetrahydrobenzothiophene derivatives and evaluate their anti-bacterial activities. Methods: Read More

Background: Trihexyphenidyl chloride (THP) is an antidyskinetic medication used in single and combination therapy to symptomatically treat Parkinson's disease. Due to its fast metabolism and short elimination of half-life, it causes changes in plasma concentrations and requires frequent dosage. Objective: The aim of this study was to prepare a sustained release formulation of Trihexyphenidyl chloride (THP). Materials and Read More

Background: Mimosa pudica Linn has been used in traditional medicine to support the treatment of type 2 diabetes. In the present study, we aimed to isolate and evaluate α-glucosidase and Protein Tyrosine Phosphatase 1B (PTP1B) inhibitory activities of bioactive compounds from Mimosa pudica’s leaf extract. Methods: Mimosa pudica leaves were extracted with 80% of ethanol. Bioactive compounds were isolated using a c Read More

Background: α-Aminophosphonates are potentially biologically active species. Objective: We wished to compare the synthetic methods and evaluate the effect of the α- aminophosphonates on sarcoma cell lines. Methods: We investigated microwave-assisted Kabachnik–Fields and Pudovik reactions, as well as substitutions, and applied in vitro cytotoxicity screening. Results: The Kabachnik–Fields condensation and th Read More