Letters in Drug Design & Discovery - Volume 16, Issue 10, 2019

The article discusses the basic properties of fluorine atom that have made it so useful in drug development. It presents several examples of therapeutically useful drugs acting against many life-threatening diseases along with the mechanism as to how fluorine influences the drug activity. It has been pointed out that fluorine, due to its ability to increase the lipophilicity of the molecule, greatly affects the hydrophobic interac Read More

Background: Human tumor cells lines and tumor samples overexpress the neurokinin-1 receptor (NK-1R). Substance P (SP), after binding to NK-1Rs, induces tumor cell proliferation, an antiapoptotic effect and promotes angiogenesis and the migration of cancer cells for invasion and metastasis. Methods: In contrast, NK-1R antagonists block the previous pathophysiological actions mediated by SP. These antagonists promote the d Read More

High cholesterol and triglyceride levels are mainly related to further generation of lifethreating metabolism disorders including cardiovascular system diseases. Therefore, hypercholesterolemia (i.e., also referred to as hyperlipoproteinemia) is a serious disease state, which must be controlled. Currently, the treatment of hypercholesterolemia is mainly achieved through the employment of statins in the clinic, althoug Read More

Dietary fatty acids have exerted numerous pathophysiological effects in humans. Indeed, monounsaturated fatty acids and ω-3 polyunsaturated fatty acids are generally thought to have favorable cardiometabolic actions via their anti-inflammatory and anti-thrombotic properties, while saturated fatty acids and trans fatty acids are supposed to contribute to the development and progression of atherosclerotic cardiovasc Read More

Coffee, one of the world’s most consumed products, is extracted from the roasted seeds of Coffea sp., a plant native to Africa. The effects of coffee on the human body have been recognized for centuries and have now become the subject of systematic research. Caffeine’s impact on a person’s cognitive ability was reviewed through a large set of literature related to the subject. Learning and memory tasks are not typically influe Read More

Background: A new series of O-benzyloximes derived from eugenol was synthesized and was evaluated for its antinociceptive and anti-inflammatory properties. Methods: The target compounds were obtained in good global 25-28% yields over 6 steps, which led us to identify compounds (Z)-5,6-dimethoxy-2,2-dimethyl-2,3-dihydro-1H-inden-1-one-O-(4- (methylthio)benzyloxime (8b), (Z)-5,6-dimethoxy-2,2-dime Read More

Background: One of the best known to date GPCR class A (Rhodopsin) includes more than 100 orphan receptors for which the endogenous ligand is not known or is unclear. One of them is N-arachidonyl glycine receptor, named GPR18, a receptor that has been reported to be activated by Δ9-THC, endogenous cannabinoid receptors agonist anandamide and other cannabinoid receptor ligands suggesting it could be considered Read More

Background: As the first phenylpyrazole pesticide, fipronil has been widely used in crop protection and public hygiene. In the low energy conformation of fipronil, a pseudo-six-membered ring is observed through an intramolecular hydrogen bond. Methods: A scaffold hopping strategy was applied to mimic the pseudo-six-membered ring of fipronil by non-aromatic ring. All compounds were synthesized with a proper syn Read More