Silver mediated one-step synthesis of oxazoles from alpha-haloketones

An efficient silver mediated one-step synthesis/construction of oxazoles using α-haloketones and primary amides is herein described. The methodology is efficient and simple to perform, giving the desired oxazoles in good to excellent yields. © 2011 King Saud University

Anti-ulcerogenic and anti-ulcerative colitis (UC) activities of seven amines derivatives

The Novel target compounds (CP-1-7) were synthesized and tested at doses up to 1000mg/kg for their entitled activities. They exerted promising results without any behavioral changes and mortality in mice. Therefore, according to the results obtained in our study, it could be categorized as highly safe agents for treating UC since substances possessing LD50 higher than 50mg/kg are considered nontoxic. They also possessed a potent anti-ulcerogenic activity with different potentials. The most effective compound was CP-4, it produced 97.7% ulcer protection of control followed by CP-3, which produced 90.3% protection, while the standard drug ranitidine (100mg/kg) produced 49.2% protection. Compound CP-1 showed lowest activity among the current series, it produced 55.5% protection. The target compounds were significantly more effective than the standard in reducing ulcer index. The anti-ulcerative colitis activity was tested using acetic acid induced colitis model. The curative effect of the tested compounds at a dose of 50mg/kg oral administration on rats showed a potent anti-ulcerative colitis activity with different potentials. They induced a significant decrease in ulcer score, ulcer area, ulcer index and weight/length of the colon specimens.The percent protection of control colitis ranged from 66.8% for CP-7 to 22.3% for CP-5; however the percent protection for dexamesathone (0.1. mg/kg) was 59.3%. The effect of the tested compounds CP-7 and CP-3 at dose 50. mg/kg were significantly more effective than dexamesathone (0.1. mg/kg) in reducing all parameters.Liver functions were not affected as there is no effect on the activity of both AST and ALT in animals that received the compounds, so the compounds didn't reveal hepatotoxic manifestation. Although, the results on kidney functions showed that, CP-1 slightly elevated blood urea concentration and CP-3 & CP-4 slightly elevated serum creatinine; no apparent nephrotoxic manifestations were recorded

Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity

Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-p-tolyl3H-quinazolin-4-one (5) and 2-p-Tolyl-3-[3,4,5-trimethoxy-benzylidene-amino]-3H-quinazolin-4-one (6) in addition to one acetamide derivative named as 2-(2-Hydroxycarbonylphenylamino)-N-(4- aminosulphonylphenyl) 11 were synthesized, and evaluated for their anti-ulcerogenic & AntiUlcerative colitis activities. All of the three compounds showed curative activity against acetic acid induced ulcer model at a dose of 50 mg/kg, they produced 65%, 85% & 57.74% curative ratio for compounds 5, 6 & 11 respectively. The effect of the tested compounds 5, 6 & 11 at dose 50 mg/kg were significantly (P < 0.01) more effective than dexamesathone (0.1 mg/kg) in reducing all parameters. Compounds showed curative activity of for peptic ulcer (induced by absolute alcohol (at a dose of 50 mg/kg, it produced Curative of control ulcer 56.00%, 61.70% & 87.1% for compounds 5, 6 & 11 respectively at dose 50 mg/kg, while the standard drug (Omeprazole 20 mg/kg) produced 33.3%. In both tests, the activity of our target compounds were higher than the standard drugs used for treatment of peptic ulcer and ulcerative colitis. No side effects were reported on liver and kidney functions upon prolonged oral administration of this compounds

Novel essential amino acid-sulfanilamide hybrid as safe anti-ulcerogenic agent with anti-helicobacter pylori activity

A novel and safe essential amino acid (Leucine) incorporating sulfanilamide was synthesized, and evaluated for its anti-ulcerogenic activity and in vitro anti-Helicobacter pylori activity. The new molecule showed a dose dependent activity against absolute ethanol-induced ulcer in rats, it produced percent protection of control ulcer by 66.7 at dose 100 mg/kg. In addition it showed a potent anti-Helicobacter pylori activity in vitro against 7 clinically isolated strains. The minimum inhibitory concentration (MIC) ranged from 12.5 to 50 μg/ml. The preliminary safety studies and toxicity profile are optimistic and encouraging

Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents

© 2015 The Authors. Published by MDPI. This is an open access article available under a Creative Commons licence. The published version can be accessed at the following link on the publisher’s website: https://doi.org/10.3390/molecules200815206© 2015 by the authors. A library of 53 benzimidazole derivatives, with substituents at positions 1, 2 and 5, were synthesized and screened against a series of reference strains of bacteria and fungi of medical relevance. The SAR analyses of the most promising results showed that the antimicrobial activity of the compounds depended on the substituents attached to the bicyclic heterocycle. In particular, some compounds displayed antibacterial activity against two methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentrations (MICs) comparable to the widely-used drug ciprofloxacin. The compounds have some common features; three possess 5-halo substituents; two are derivatives of (S)-2-ethanaminebenzimidazole; and the others are derivatives of one 2-(chloromethyl)-1Hbenzo[ d]imidazole and (1H-benzo[d]imidazol-2-yl)methanethiol. The results from the antifungal screening were also very interesting: 23 compounds exhibited potent fungicidal activity against the selected fungal strains. They displayed equivalent or greater potency in their MIC values than amphotericin B. The 5-halobenzimidazole derivatives could be considered promising broad-spectrum antimicrobial candidates that deserve further study for potential therapeutic applications.Published versio

Review on some antioxidant plants growing in Arab world

Cellular damage or oxidative injury arising from free radicals or reactive oxygen species (ROS) now appears the fundamental mechanism underlying a number of human neurodegenerative disorders, diabetes, inflammation, viral infections, autoimmune pathologies and digestive system disorders. Free radicals are generated through normal metabolism of drugs, environmental chemicals and other xenobiotics as well as endogenous chemicals, especially stress hormones (adrenalin and noradrenalin). Accumulated evidence suggests that ROS can be scavenged through chemoprevention utilizing natural antioxidant compounds present in foods and medicinal plants. Plant extracts and their constituents as a natural source of antioxidants have been extensively reviewed. Plant extracts containing low molecular mass compounds have been successively used in phytotherapy since ancient times, as reactive oxygen species are involved in several diseases in this review, research on the antioxidant potential of medicinal plants. © 2011 King Saud University

An overview on natural product drug formulations from conventional medicines tonanomedicines: past, present and future

For decades, naturally produced plants have been studied and used in herbalism (herbal medicines). Despite being natural, these products were not of any interest of any of the major pharmaceutical companies. There are various reasons behind this ignorance but mainly because of the outdated thought, that many people believe about natural products, in which plants are only utilized for their antibiotic benefits since there were successfully used as antibiotics in the post-World War II era. Mainly small pharmaceutical companies have paid attention to natural products and explored their benefits against various diseases such as microbial infection, cancer, cardiovascular diseases, diabetes and other illnesses while big pharmaceutical industries have focused on screening synthetic compounds. Nowadays, natural products and their derivatives have demonstrated their significant impact as therapeutic agents on people heath. Accordingly, about one-third of the top-selling products in the pharmaceutical market are natural products which are either derived from plants or microorganisms. The use of such products is highly preferred by people due to their unique advantages of good therapeutic efficacy, low side effects and cheaper than synthetic products. However, many of natural products are not clearing the clinical trials due to their toxicity and problems with biocompatibility. This review will briefly highlight the history of herbal medicine and will cover pharmaceutical formulations prepared from therapeutically active extracts of natural products. In addition, this article will summarise a range of natural products in conventional dosage forms to the most recent nano-medicinal forms