Search results for "biological evaluation"

<strong>In Silico Repurposing, Design, Synthesis and Biological Evaluation of Bisacodyl Analogues</strong>

2018

In a recent article was described in silico repositioning, design, synthesis, biological evaluation and structure-activity relationship (SAR) of an original class of anti-inflammatory agents based on a polyaromatic pharmacophore structurally related to bisacodyl (BSL) drug used in therapeutic as laxative.

Isolation, structure elucidation, and biological evaluation of the unusual heterodimer chrysoxanthone from the ascomycete IBWF11-95A

2009

Chrysoxanthone, an unusual heterodimer of blennolide A and 2-hydroxychrysophanol linked through a diaryl ether bridge, was isolated from mycelia of the ascomycete IBWF11-95A grown in submerged culture. Its structure was elucidated by two-dimensional NMR spectroscopy. The metabolite shows antibacterial activity against different species with MIC values between 2.5 and 20 μg/mL while also inhibiting the growth of several fungi.

New Cathepsin Inhibitors to Explore the Fluorophilic Properties of the S 2 Pocket of Cathepsin B: Design, Synthesis, and Biological Evaluation

2011

5 páginas, 1 figura, 2 tablas -- PAGS nros. 5256-5260

Synthesis and biological evaluation of new indazole derivatives

2010

New N-methyl and N-ethyl substitutions in the indazole nucleus are reported by reacting 3-(2-aminobenzamido)indazole and the appropriate trimethyl/triethyl orthobenzoate. Single crystal X-ray analysis confirms the N-ethylation position for the 3-(1-ethyl-1H-indazol-3-yl)-2-phenylquinazolin-4(3H)-one derivative 3f. Compounds 11a-d and 3a-d were tested to evaluate their antimicrobial, their antiproliferative activity and their COX inhibitory activities showing scarce or moderately antiproliferative activity and some inhibitory activity against COX-1 and COX-2.

Novel 4-(3-phenylpropionamido), 4-(2-phenoxyacetamido) and 4-(cinnamamido) substituted benzamides bearing the pyrazole or indazole nucleus: synthesis…

2019

Based on some common structural features of known compounds interfering with p53 pathways and our previously synthesized benzamides, we synthesized new ethyl 5-(4-substituted benzamido)-1-phenyl-1H-pyrazole-4-carboxylates 26a-c, ethyl 5-(4-substituted benzamido)-1-(pyridin-2-yl)-1H-pyrazole-4-carboxylates 27a-c and N-(1H-indazol-6-yl)-4-substituted benzamides 31a,b bearing in the 4 position of the benzamido moiety the 2-phenylpropanamido or 2-phenoxyacetamido or cinnamamido groups. A preliminary test to evaluate the antiproliferative activity against human lung carcinoma H292 cells highlighted how compound 26c showed the best activity. This last was therefore selected for further studies wi…

Current Advances in the Synthesis and Biological Evaluation of Pharmacologically Relevant 1,2,4,5-Tetrasubstituted-1H-Imidazole Derivatives

2019

:In recent years, the synthesis and evaluation of the biological properties of 1,2,4,5-tetrasubstituted-1H-imidazole derivatives have been the subject of a large number of studies by academia and industry. In these studies it has been shown that this large and highly differentiated class of heteroarene derivatives includes high valuable compounds having important biological and pharmacological properties such as antibacterial, antifungal, anthelmintic, anti-inflammatory, anticancer, antiviral, antihypertensive, cholesterol-lowering, antifibrotic, antiuricemic, antidiabetic, antileishmanial and antiulcer activities.:The present review with 411 references, in which we focused on the literatur…

History, Processing and Quality Enhancement of Traditional Egyptian Kariesh Cheese: A Review

2013

Kariesh is a soft acid cheese made from skimmed cow's milk, buffalo milk or buttermilk from sour cream; apparently it is made only on farmsteads. It is considered to be one of the most important traditional Egyptian dairy products, commonly made in the Egyptian countryside, especially in small villages, as low-income people such as farmers use Kariesh cheese in their diet owing to its high protein content, low fat and price. Therefore, nowadays, Kariesh cheese is a promising food in the avoidance of health problems associated with fat, particularly for old people. The aim of this article is to provide a wide range of information on Egyptian Kariesh cheese starting with a brief description o…

Lead optimization of pyrazolo[1,2-a]-benzo-[1,2,3,4]-tetrazin-3-one nucleus to increase the biological properties as anticancer compounds

Heterocyclic and Phenyl Double-Bond-Locked Combretastatin Analogues Possessing Potent Apoptosis-inducing activity in HL60 and in MDR Cell lines

2005

Two new series of combretastatin (CA-4) analogues have been prepared. The alkenyl motif of CA-4 was replaced either by a five-membered heterocyclic (isoxazoline or isoxazole) or by a six-membered ring (pyridine or benzene). The new compounds have been evaluated for their effects on tubulin assembly and for cytotoxic and apoptotic activities. Five compounds (18b, 20a, 21a, 34b, and 35b) demonstrated an attractive profile of cytotoxicity (IC501 microM) and apoptosis-inducing activity but poor antitubulin activity. The isoxazoline derivatives 18b, 20a, and 21a, demonstrated potent apoptotic activity different from that of natural CA-4. Their ability to block most cells in the G2 phase suggests…

Synthesis, biological evaluation and chemometric analysis of indazole derivatives. 1,2-Disubstituted 5-nitroindazolinones, new prototypes of antichag…

2012

Chagas disease chemotherapy, currently based on only two drugs, nifurtimox and benznidazole, is far from satisfactory and therefore the development of new antichagasic compounds remains an important goal. On the basis of antichagasic properties previously described for some 1,2-disubstituted 5-nitroindazolin-3- ones (21, 33) and in order to initiate the optimization of activity of this kind of compounds, we have prepared a series of related analogs (22-32, 34-38, 58 and 59) and tested in vitro these products against epimastigote forms of Trypanosoma cruzi. 2-Benzyl-1-propyl (22), 2-benzyl-1-isopropyl (23) and 2-benzyl-1-butyl (24) derivatives have shown high trypanocidal activity and low un…