Letters in Drug Design & Discovery - Volume 14, Issue 4, 2017

Background: The healthy appearance of the skin becomes increasingly important worldwide, and among the problems that affect the skin are oxidation and hyperpigmentation. The first causes loss of tissue elasticity, and the second causes dermatitis, melasma, and lentigo. Quinolines are used as treatment of a variety of diseases, as malaria, tumor, hyperpigmentation, and it has also other properties such as antioxidant. Read More

Background: Oxidative stress caused by reactive oxygen species (ROS) plays a significant role in many human disorder such as cancer, rheumatoid arthritis, atherosclerosis, stroke, neurodegeneration, and diabetes as well as the process of aging. Compounds interfere with the action of ROS might be useful in prevention and treatment of these pathologies. Indole nucleus seems to protect the nervous system against oxidative Read More

Background: Cancer is the leading cause of death worldwide. Induction of apoptosis in cancer cell is the main strategy for the development of anticancer agents targeting apoptosis pathway. Procaspase-3 is one such target for the induction of apoptosis via activation of caspase 3. Novel molecules are needed as procaspase-3 activators which will induce apoptosis in cancer cell. Objective: The main objective of this work is Read More

Background: Prostate cancer represents the second most frequently diagnosed malignancy in men, and is considered as the fifth leading cause of death from cancer in men. The aims of this paper are shown the development of new, rapid, and clean synthetic routes toward focused libraries of such compounds is therefore of great importance to both medicinal and synthetic chemists. Methods: The preparation of benzochrome Read More

Method: This work reports on the Surflex docking and 3D-QSAR studies viz., CoMFA, CoMSIA and Topomer CoMFA on a set of 64 compounds that are inhibitors of enoyl ACP reductase enzyme. Diversity method was used to validate the generated test and training set. Results and Discussion: These sets were then used to generate, steric, electrostatic, hydrophobic, H-bond donor and acceptor contour maps. The results showe Read More

Background: A series of pyrimidothiadiazinones 5a-n were prepared from aminomethylation of pyrimidinethione 1 with different primary amines and formaldehyde through Mannich reaction. The spectral data of the formed products confirmed the suggested structures. Method: Most of the newly synthesized compounds were tested for their antimicrobial and anticancer activities. Depending on the obtained results, the newly Read More

Background: The amine 2 obtained via two steps starting from thiomorpholine was converted into the corresponding 1,3-thiazole (4), arylmethileneamino (5a-d) and hydrazide (7) derivatives using conventional and also microwave techniques. The synthesis of 1,3,4-oxadiazole (8), arylidenenhydrazide (9a-c) and carbothioamides (10a,b) was performed with the treatment of 7 with CS2, suitable amines and suitable i Read More

Background: Considering that inflammation is involved in many degenerative conditions, some derivatives of tolfenamic acid, naproxen and indomethacin were synthesised and evaluated biologically. They were found to possess increased anti-inflammatory activity, being more potent than the parent drugs. Method: Thus, compound 4, the ester of naproxen with di-tert-butyl-4-(hydroxymethyl)phenol, caused about 80% Read More

Background: Melatonin, a hormone synthesised by the pineal gland, has a significant role in the regulation of the circadian biological clock. Objective: The present study aims at investigating how matrix tablets comprised of common hydrogels influence the release profile of melatonin at both physiological pH’s. Moreover, we designed and developed liposomes incorporating this hormone in order to compare its release pr Read More

Background: Obesity alters endocrine and metabolic function of the adipose tissue leading to an increased release of fatty acids, adipokynes and pro-inflammatory molecules which in turn lead to complications related to the onset of metabolic syndrome. Methods: To this regard, natural antioxidants have been found to have anti-inflammatory and protective action in cardiovascular diseases, diabetes mellitus and obesity. Read More

Introduction: Chronic inflammation of organs has been linked with various steps involved in carcinogenesis. Delta-opioid receptors (DOR) and farnesyl transferase (FT) inhibitors have the capability to obstruct various intracellular pathways affecting inflammation and cell proliferation. They become an effective targets for the treatment of inflammation and cancer. Objectives: The work presented here reports the in-silico stu Read More

Background: Sequential therapy is one of the most common regimens for H. pylori eradication. The progressive ageing may lead to several problems in the management of H. pylori. Objective: We aimed to assess the effectiveness/safety of sequential therapy in elderly patients and evaluate possible predictive factors of failure. Methods: We retrospecively enrolled 76 patients >65 years old (elderly group) and 69 con Read More