Letters in Drug Design & Discovery - Volume 17, Issue 12, 2020

Background: In the 1960s, the human coronavirus was designated, which is responsible for the upper respiratory tract disease in children. Back in 2003, mainly 5 new coronaviruses were recognized. This study directly pursues to govern knowledge, attitude and practice of viral and droplet infection isolation safeguard among the researchers during the outbreak of the COVID-19. Introduction: Coronavirus is a proteinaceous Read More

Background: Oxidative stress is a defense mechanism against malarial intracellular parasite infection. On the other hand, the Human glutathione reductase enzyme reduces oxidative stress in the cells, making the inhibitors of this enzyme a promising candidate for malaria treatment. Objective: Rational drug design was used in this work to plan new human glutathione reductase inhibitors. Methods: Virtual screening wa Read More

Background: Type-2-diabetes mellitus is associated with many side effects affecting vital body organs, especially heart. Thiazolidinediones are potent antidiabetics. Studies have proven that amino-acids and peptides promote glucose transport, have antioxidant properties, and fewer side effects, thus we designed hybrids by combining amino-acid esters and peptide esters with 2, 4 thiazolidinedione acetic acid moiety whic Read More

Background: Designing and development of molecules for cancer treatment useful and with no side effects are a big challenge for the researchers in the field of drug discovery. The use of phytochemicals for chemoprevention is gaining more advantages, and intake of flavonoids has proved to reduce the occurrence of various cancers. Objectives: The present study was focused on selecting eight flavonoids and study them by in Read More

Background: Cancer is the name given to various diseases that are mainly uncontrolled, related to cell growth and can affect various organs. Among them, lung cancer is the one, which, in its earliest stages, is difficult to diagnose, and it is asymptomatic until the disease progresses. Triazole ring is an important heterocyclic ring known with various pharmacological activities. Objective: It is aimed to synthesize and cha Read More

Background: The intentional dissemination of the “anthrax letter” led the researchers to increase their efforts towards the development of medical countermeasures against anthrax bioterrorism. A virulent strain of Bacillus anthracis secretes deadly three protein exotoxin (protective antigen, lethal factor and edema factor) that is the causative agent of anthrax and considered as serious biological weapons. Objective: Due to li Read More

Background: Currently, infectious diseases caused by pathogenic and resistant bacteria are more challenging for anti-bacterial drug discovery. The discovery of new anti-bacterial agents developed in many mechanisms includes disruption of the bacterial cell wall formations. The MurA is a key enzyme contributing to the first step of bacterial peptidoglycan biosynthesis and is, therefore, proposed as an effective bactericidal targ Read More

Background: Pyrimidine ring is one of the most important heterocyclic scaffolds due to its biological benefits as antimicrobial agents via acting as competitive suppressors of dihydropteroate synthase (DHPS) enzyme, inhibiting dihydrofolate reductase or glucosamine N-phosphate synthase. Objective: The objective of this work is preparing twenty four derivatives of pyrimidine heterocycle 1a-f, 2a-f, 3a-f and 4a-f via a facile o Read More

Background: Cancer is a leading cause of deaths worldwide, accounting for 9.6 million deaths in 2018. According to the WHO, the most common causes of cancer deaths are lung, colorectal, stomach liver and breast cancer. Introduction: PARP-1 has a crucial role in cell proliferation, survival and death due to its role in the regulation of multiple biological processes. Quinazolinone and its derivatives represent a large class of bi Read More

Background: NSAIDs are used as first-line drugs for the treatment of various inflammatory disorders. Chronic use of NSAIDs is known to be associated with gastrointestinal and renal toxicity. Local generation of reactive oxygen species finally resulting in cellular apoptosis is one of the accepted mechanisms for NSAID-induced toxicity. Objective: The objective of the present study was to design and synthesize a series of Read More

Background: The use of antibiotics has compromised due to the appearance of multidrug- resistant strains and decreased susceptibility of strains to antibiotics. Antibiotic resistance has become a worldwide threat as well as Helicobacter pylori induced gastric cancer is a major problem nowadays. Therefore, it is the need of time to synthesize potent anti-urease motifs. Introduction: Schiff bases represent a large class of biologically Read More