Letters in Drug Design & Discovery - Volume 15, Issue 6, 2018

Background: Now-a-days, the model of “hybrid drugs” has acquired recognition in medicine due to their significant role in the treatment of different health problems. Methods: We have synthesized new series of isoxazole-chalcone conjugates (14a-m) by the Claisen-Schmidt condensation of suitable substituted acetophenones with isoxazole aldehydes (12a-d). In vitro cytotoxic activity of the synthesized compounds was studie Read More

A novel, rapid and efficient microwave-assisted synthesis of S-substituted quinazoline derivatives was obtained using 1,4-dihydroquinazoline-2-thiol and various boronic acids with copper catalyst in one-pot reactions. The versatility of the synthetic protocol with various boronic acids and the optimization processes of the microwave irradiation conditions including temperature, solvent, and reaction time were demonstrated.

Background: Improving the gastrointestinal safety profile of Non-Steroidal Anti- Inflammatory Drugs (NSAIDs) is an important goal. An important strategy to develop NSAIDs with minimal Gastrointestinal (GI) toxicity is to target the COX-2 isoform with a selective inhibitor. Methods: In this study we selected ketoprofen as a lead NSAID for development into safer agents. 1, 2, 4-Oxadiazole moiety was employed to mask the free ac Read More

Introduction: Metal ions are cofactors found in antioxidant enzymes such as superoxide dismutase (SOD), and are essential in catalytic mechanisms for scavenging the free radicals. Therefore, synthetic compounds containing metal ions coordination are designed for SOD mimic and other biological activities. Objective: This study aimed to synthesize metal (Ni, Cu, Mn) complexes of mixed ligands of 2-thiouracil (2TU) with 8- Read More

Background: Antioxidants are compounds that inhibit oxidation in biological systems and in the natural environment as free radical scavengers, reactive oxygen scavengers, or reducing agents. Phenolic acid compounds, such as Protocatechuic Acid (PCA), are one of the most important antioxidants occurring in the natural environment. Methods: In this study, the relationships between structure and antioxidant activities Read More

Background: Benzimidazolium salts include biologically active benzimidazole ring. Some benzimidazolium salts and their metal complexes, containing different groups, showed remarkable antibacterial, antifungal and antitumor effects. Most of these studies are generally related with the 2-unsubstituted derivatives of benzimidazolium salts which named as N-heterocyclic carbenes (NHCs). To enhance the efficacy of the be Read More

Background: Diabetes being among the most prevalent disease is being studied widely to achieve most potent drug with lesser side-effects. Numerous targets have been explored and several drugs have been developed to combat type-2 diabetes. Worldwide scenario depicts an increase in the number of diabetics at an alarming rate. Due to this critical need in the current scenario, the focus has been shifted to natural pro Read More

Background: Quinoline nucleus is found in a vast range of biologically active compounds. The quinoline group of compounds which are anti-infective in nature are found to act by inhibiting different enzymes. DNA gyrase being one of the more common site of action. Methods: Taking the mechanism into consideration, we have designed and synthesised some novel 6-substituted quinoline-4-caboxylic acid derivatives. The d Read More

Background: Cluster of differentiation 38 (CD38) is major NADase and regulates the intracellular level of NAD. It uses NAD as substrate to produce ADP Ribose (ADPR) and cyclic ADP ribose (cADPR) and converts NADP to NAADP. Its inhibition can be utilized to treat several condition. Methods: In this research, for identifying new potent CD38 inhibitors both structure and ligand based virtual screening approaches were used to sear Read More

Background: Sirtuin 2 is a deacylase enzyme which has a significant role in the treatment of neurodegenerative diseases. A reported series of novel thieno[3,2-d]pyrimidine-6- carboxamide derivatives has been chosen as sirtuin inhibitors. Methods: A pharmacophore and atom-based 3D-QSAR studies were carried out in order to understand the molecular features and structural requirement of these molecules to selectively inhi Read More

Background: Aedes aegypti is an important mosquito vector for the transmission of several infectious diseases. Current insecticides play a vital role in controlling mosquitoes; however, the frequent use of insecticides has led to the development of insecticide resistance. In order to control mosquito populations, new and effective bioactive molecules are urgently needed. Methods: In the current work, N-(benzylidene)-3-cycl Read More

Background: Illicium verum Hook. f. (Star anise) has been traditionally used for the treatment of abdominal colic, vomiting, pain, nervousness, insomnia and rheumatism. Objective: The present study was conducted to investigate the anti-inflammatory properties of Illicium verum extracts. Methods: Different extracts of I. verum (IV-Ext-1, IV-Ext-3 and IV-Ext-4) were screened for their anti-inflammatory potential using carrag Read More

Background: The use of laser methods to irradiate currently used drugs in order to obtain photo-products with antimicrobial and anti-tumour activity constitutes a new approach in fighting antimicrobial resistance acquired by bacteria and tumours. Methods: The interaction of UV laser radiation with phenothiazine derivatives, such as chlorpromazine, thioridazine and promethazine, and a hydantoin derivative, SZ-2, was Read More