Letters in Drug Design & Discovery - Volume 16, Issue 9, 2019

Background: Hydrazide-hydrazones constitute an important class of compounds for new drug development. In this study, a series of 39 new acylhydrazones (3-41), derived from (2S)-3-methyl- 2-[[(4-methylphenyl)sulfonyl]amino]butanoic acid hydrazide were synthesized with further aim to achieve biologically active acylhydrazones carrying an amino acid side chain. Methods: Compounds 3-41 were synthesized by microw Read More

Background: Diabetes is the primary cause of fatality and disability all over the world, in recent past, we have reported various classes of compounds as anti-glycating agents and we have also reported benzimidazole and benzothiazole derivatives as a potential class of anti-glycating agents. This encouraged us to evaluate the pyridinyl benzimidazole/pyridinyl benzothiazole derivatives 1-27 for yeast glucose uptake acti Read More

Background: Cancer is a fatal disease for mankind; continuous research is still going on for the invention of potent anticancer drugs. In this view, 1, 3, 4-Oxadiazoles are privileged molecules which attracted medicinal chemists towards their anticancer properties. Methods: A new series of benzo[d]imidazol-5-yl)-5-(substituted)-1,3,4-oxadiazole derivatives was synthesized in an efficient ‘one-pot’ nitro reductive cyclization usi Read More

Background: The main issue is finding the most efficient method in the treatment of cancer in terms of early and accurate diagnostic. One of the most modern diagnostic techniques is imaging methods. The accuracy and detection speed of MRI and CT SCAN are high. Methods: The most important complication of iodinated contrast agents in medical imaging is severe renal toxicity Nephrogenic Systemic Fibrosis (NSF). In o Read More

Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1H NMR, 13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Their in vitro a Read More

Background: There has been increased interest in the research of proteasome inhibitors for more than two decades. Hotspots in this field are constantly changing. Objective: This study aimed to investigate trends in proteasome inhibitors research from 1992 to 2018 and compare the contributions of such research from different countries and authors. Methods: We used Excel 2013 and VoSviewer to analyze bibliometri Read More

Objective: According to the principles of drug design, the structures of picotamide and betrixaban were combined to design novel series of 2-methoxy-5-aminobenzamides. A total of twenty new compounds 1a-1t have been synthesized and evaluated for their antiplatelet aggregation activities in vitro. Methods: In the structural design of target compounds 1a-1t, the betrixaban was retained group characteristics and th Read More

Background: The Gastric H+/K+-ATPase is also known as proton pump is the enzyme responsible for the acidification of gastric juice. H+/K+ GastroEsophageal Reflux Disease (GERD) and other acid related diseases mainly depend on the inhibition of the gastric H+/K+- ATPase which will finally result in acid secretion in stomach. GERD is one of the diseases that have significant effect on the quality of human life and are th Read More

Background: Drugs that interfere with microtubule dynamics are used widely in cancer chemotherapy. Microtubules are composed of αβ-tubulin heterodimers, and the colchicine binding site of tubulin is an important pocket for designing tubulin polymerization inhibitors. We have previously designed and synthesized a series of colchicine binding site inhibitors (CBSIs). However, these compounds showed no anticancer activity Read More

Background: Diabetes is a chronic endocrine associated metabolic ailment. It is chiefly characterized by hyperglycemia, which results due to deficient insulin levels caused by either obliteration of pancreatic beta cells or the incompetent sensitivity of insulin at the target tissue. Methods: In the present study, selected compounds (Abrotandiol, Abrotanone, Lariciresinol, Pinoresinol, Syringaresinol and Taxiresinol) from Perovski Read More