Letters in Drug Design & Discovery - Volume 15, Issue 4, 2018

Background: MRSA is a gram positive pathogen resistant to methicillin and other betalactam antibiotics, including penicillin, oxacillin, and declooxacillin. Statistical data suggest that as many as 19,000 people per year die from MRSA in the USA. Methods: Prudent use of existing drugs, coupled with the development of new antibacterial agents has been suggested as a way to combat the public health burden, posed by M Read More

Background: Plant diseases caused by plant pathogens are important constraints to agricultural production throughout the world and at least 10% of global food production is lost to plant diseases. In order to discover new fungicides and control the plant diseases, a series of novel 1,2,4- triazole thioether derivatives carrying a pyrimidine moiety were designed and synthesized. Methods: Thirteen novel 1,2,4-triazole thioether deriv Read More

Background: Infectious pathogenic bacteria are the key virulence in our daily life. Especially diseases produced by multidrug resistant Staphylococcus aureus (MRSA) still contributing in morbidity and mortality in humans. Discovery of new and safer antibiotics is an upmost task in current medicinal research. Methods: By keeping in mind the considerable antimicrobial activities of coumarin scaffold, 3-substituted co Read More

Background: Influenza is a common respiratory tract infection caused by RNA-virus of the family Orthomyxoviridae; influenza virus, causing variety of symptoms including fever, nasal secretions, cough, muscle pain and pneumonia. It is classified into three distinct types A, B & C. Many 1,3,4-thiadiazoles, 1,3,4-oxadiazoles and 1,2,4-triazoles have showed broad spectrum of biological activities. These heterocycles are consider Read More

Background: Combrestastatin A-4 (CA-4) is a potent anticneoplastic and antiangiogenesis natural substance isolated from Combretum caffrum. Over the past two decades, numerous derivatives of CA-4 have been discovered. However, none of these derivatives has reached the clinical stage. Thus, continuing effort is needed in developing CA-4 analogues with improved pharmacological properties. Methods: In this study, two se Read More

Background: Carcer is one of the most common diseases that endanger human health and even lives in the world today. As it reported, lung, breast and colon cancers are most common in the developing and under developed countries. Fortunately, several therapeutic regimes have been successfully approached for fighting cancer nowadays. Osimertinib (AZD9291), approved in 2015 by the FDA, as the third-generation inh Read More

Background: Epilepsy affects approximately 50 million people globally. It is generally characterized by periodic seizures of unpredictable nature, though a variety of anticonvulsant drugs are available but the major drawback is undesirable side effects. Here an effort is being made to utilise the beneficial effect of benzothiazoles and oxadiazoles as potent anticonvulsants and there is an anticipation of synergistic effect from the h Read More

Background: Eplilepsy is defined as one of the most common neurological diseases, which affects approximately 50 million people all over the word. Despite the development of several new antiseizure drugs, the treatment of epilepsy remains still inadequate, because generally, anticonvulsant drugs can cause serious side effects such as neurotoxicity, depression, and impaired memory function. It is therefore im Read More

Background: Alzheimer's Disease (AD) is a complicated neurodegenerative disorder with a multifaceted pathogenesis.AD, characterized by gradual memory loss, falling in language ability and other cognitive deterioration, and has been a prominent risk to ageing population. This means that there is an urgent need to find new lead compounds for controlling and fighting against (AD). In this way, a new thiophene-2-pyrazoline Read More

Background: In this work, a wide spectrum of 5-aminomethylene barbituric/ thiobarbituric acid derivatives was synthesized and evaluated for their Jack bean urease inhibitory activity. Methods: Among the synthesized compounds, 5-cyclohexylaminomethylene barbituric acid (3a) showed the most potent activity (IC50 = 25.8 μM), 4 times more potent than hydroxyurea (IC50 = 100.0 μM) and a similar activity to thiourea (IC50 Read More

Background: NSAIDs have been extensively used for the treatment of pain and inflammation. There are about 30 different NSAIDs available in market and about 80 percent of prescriptions throughout the world contains one or the other painkiller. Chronic use of these drugs has many side effects such as gastric ulceration and the COX-2 inhibitors suffer from major drawback of cardiac toxicity. The need for a potential and s Read More