Category: Medicinal Chemistry

Acetamiprid exposure causes molecular and structural changes in the liver and kidney tissues of rats Pesticides are among the most widely used synthetic chemicals worldwide to protect crops, but they pose several environmental and health issues. The present study evaluates toxic effects of acetamiprid (ACMP) in rat liver and kidney tissues. Rats were exposed to…

A novel Fusion-5 Filter based Micro-chip: A highly efficient, On-chip DNA extraction and On-chip PCR amplification for rapid detection A novel, sensitive, portable method for detecting DNA from various human samples is most desirable. This study aims to develop a microdevice for on-chip DNA extraction and detection by PCR from various forensic samples. A microchip…

DNA-protein crosslinks are key to platinum-based chemotherapeutic cytotoxicity Platinum-based chemotherapeutics inflict a spectrum of DNA damage, including DNA adducts, DNA-protein crosslinks (DPCs), and interstrand crosslinks (ICLs) to variable extents. These diverse lesions may contribute to the overall toxicity of these therapeutic agents. Nonetheless, a gap exists in comparative studies elucidating the specific DNA damage responsible…

Synthesis and biological evaluation of 1,2,4-Triazolo[4,3-a][1,8] naphthyridines under Microwave condition Synthesis of 9-(4-bromophenyl)-6 aryl-[1,2,4]triazolo[4,3-a][1,8]naphthyridine-2-carbonitrile (4a-j) from 7-(2-(4bromobenzylidene)hydrazinyl)-6-aryl-1,8-naphthyridine-2-carbonitrile (3) oxidized with chloramines-T in methanol under microwave irradiation is a straight forward and very efficient process. Very high yields and excellent purities of the products were achieved. Elemental analysis, IR, 1H NMR, 13C NMR and Mass spectroscopy…

Combating Antimicrobial Resistance: A paradigm shift from general to precision medicine Antimicrobial resistance (AMR) poses a significant threat to global health. It makes treating bacterial infections increasingly difficult. AMR arises from various mechanisms of antibiotic resistance including enzymatic inactivation, target alteration, efflux pumps, and decreased permeability. The limited and often ineffective treatments relying on antibiotics…

Synthesis and biological evaluation of Trifluoromethoxyphenyl Indole Carboxamide analogs, ADME and toxicity prediction We report synthesis, ADME profile, and biological evaluation of new analogues as effective Anticancer Agents. Trifluoromethoxyphenyl indole-5-carboxamide analogues (4a-4m) were developed as a class of strong inhibitors of BCR-ABL1 kinase. The compounds (4c, 4e, and 4m) showed good anticancer activity in cancer…

Exploring Small-Molecule Inhibitors Targeting MAPK Pathway Components: Focus on ERK, MEK1, and MEK2 Kinases in Cancer Treatment Mitogen-activated protein kinases (MAPKs), also known as extracellular signal regulated kinases (ERKs), are found in numerous signal transduction pathways and are triggered by protein kinase cascades. This article will review the present state of MAPK pathway inhibitors, with…

Remodeling of membrane lipid homeostasis in azole resistant isolates of Candida albicans Azole resistance mechanisms in Candida albicans infections majorly focus around the alteration of target enzymes, overexpression of efflux pump proteins, and changes in lipid metabolism. Our earlier lipidomic studies have linked changes in cellular lipid compositions to drug susceptibilities and phenotypic defects. This…

Design, synthesis and biological evaluation of novel sulfamoyl benzamides as allosteric activators of human glucokinase Glucokinase (GK) activators, which target the GK enzyme, are an emerging class of therapeutics with promising effects against diabetes. The objective of this work was to create a new group of sulfamoyl benzamide derivatives with the ability to activate GK…