Synthesis and biological activity of Schiff and Mannich bases bearing 2,4-dichloro-5-fluorophenyl moiety.

The triazole nucleus is one of the most important and well known heterocycles which is a common and integral feature of a variety of natural products and medicinal agents. Triazole nucleus is present as a core structural component in an array of drug categories such as antimicrobial, anti-inflammatory, analgesic, antiepileptic, antiviral, antineoplastic, antihypertensive, antimalarial, local anaesthetic, antianxiety, antidepressant, antihistaminic, antioxidant, antitubercular, anti-Parkinson's, antidiabetic, antiobesity and immunomodulatory agents, etc. The broad and potent activity of triazole and their derivatives has established them as pharmacologically significant scaffolds. The basic heterocyclic rings present in the various medicinal agents are 1,2,3-triazole and 1,2,4-triazole. A large volume of research has been carried out on triazole and their derivatives, which has proved the pharmacological importance of this heterocyclic nucleus. The present paper is an attempt to review the pharmacological activities reported for triazole derivatives in the current literature with an update of recent research findings on this nuclei.

https://www.tandfonline.com/doi/pdf/10.3109/14756360903524304

Pharmacological significance of triazole scaffold.

The systematic review was commissioned by the Australian National Health and Medical Research Council (NHMRC) to evaluate the scientific literature relating to the health effects of fluoride and fluoridation. The systematic review's research questions relate to the caries-reducing benefits and associated potential health risks of providing fluoride systemically (via addition to water, milk and salt) and the use of topical fluoride agents, such as toothpaste, gel, varnish and mouthrinse. Although the review summarises the recent evidence, it does not constitute health policy or clinical practice recommendations. A literature search was undertaken using the Medline and Embase databases (via www.embase.com
 ). In addition, the Cochrane Systematic Review and Clinical Trial databases were searched to help identify additional systematic reviews and original studies. Because of the availability of recent systematic reviews, searches were limited to publications from 1996 onwards . The search was conducted in December 2006 and limited to English-language publications. Based on types of intervention (individual or population) and the outcomes assessed (efficacy or safety), the hierarchy of study types considered most relevant for answering each of the clinical questions defined in this review was chosen (Table 1). The levels of evidence used by NHMRC for intervention and aetiological studies are summarised in Table 2.
 Screening of eligible studies was conducted by three reviewers. Data were extracted for all of the included systematic reviews and individual studies using standardised data-extraction forms. This included information about the study design, NHMRC level of evidence, population, intervention, comparator, outcome definitions and results. Information relating to potential biases and study quality were also extracted. Where appropriate, study results were pooled using standard meta-analysis techniques. In total, 5418 nonduplicate citations were identified. After applying the inclusion and exclusion criteria, 408 citations were considered potentially eligible for inclusion in the review. After the review of the full papers of potentially eligible articles, 77 citations were included in the review. The summary of findings was presented in the context of the research questions (Table 3).
 Fluoridation of drinking water remains the most effective and socially equitable means of achieving community-wide exposure to the caries prevention effects of fluoride. It is recommended (see also www.nhmrc.gov.au/news/media/rel07/_files/fluoride_flyer.pdf
 ) that water be fluoridated in the target range of 0.6–1.1 mg/l, depending on the climate, to balance reduction of dental caries and occurrence of dental fluorosis.n particular with reference to care in hospital for those following stroke.

/pdf/a-systematic-review-of-the-efficacy-and-safety-of-l84tk2wkvy.pdf

A systematic review of the efficacy and safety of fluoridation

Recent synthetic and medicinal perspectives of dihydropyrimidinones: A review.

1,2,4-triazole is an important nucleus present in a large number of compounds. More than thirty-five compounds containing this nucleus are introduced into the market. 1,2,4-triazole nucleus is stable to metabolism and acts as an important pharmacophore by interacting at the active site of a receptor as hydrogen bond acceptor and as a donor. Due to its polar nature, the triazole nucleus can increase the solubility of the ligand and it can significantly improve the pharmacological profile of the drug. A large number of 1,2,4-triazole derivatives are reported to possess a wide range of bioactivities including anti-cancer activity. This review article describes the role of 1,2,4-triazole nucleus in different types of anti-cancer agents such as nucleoside based anti-cancer agents, kinase inhibitors, tubulin modulators, aromatase and steroid sulfatase inhibitors, methionine aminopeptidase inhibitors, tankyrase inhibitors and metal complex based anti-cancer agents. It is expected that the current review article will provide insight into various ligand-receptor interactions and help in the rational design and development of novel 1,2,4-triazole based anti-cancer drugs with improved selectivity for cancer cells.

Recent Developments on 1,2,4-Triazole Nucleus in Anticancer Compounds: A Review

Synthesis and studies on some new fluorine containing triazolothiadiazines as possible antibacterial, antifungal and anticancer agents.

One pot synthesis of thiazolodihydropyrimidinones and evaluation of their anticancer activity.

Synthesis of a series of 7-arylidene-6-(2,4-dichlorophenyl)-3-aryloxymethyl/anilinomethyl-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines (3) by the condensation of 3-aryl-1-(2,4-dichloro-5-fluorophenyl)-2-bromo-propen-1-one (1) and 4-amino-5-mercapto-3-aryloxymethyl/anilinomethyl-1,2,4-triazoles (2) is described. The newly synthesized compounds were characterized by elemental analysis IR, 1H NMR and mass spectral data. These compounds were tested for their antimicrobial activities against Escherichia coli, Staphylococcus aureus (Smith), Psuedomonas aeruginosa (Gessard), Bacillus subtilis and Candida albicans. Some of the newly synthesized compounds were also screened for their anticancer activity. Among them compounds 3m, 3o, 3q showed in vitro anticancer activity.

Synthesis and Studies on Some New Fluorine Containing Triazolothiadiazines as Possible Antibacterial, Antifungal and Anticancer Agents.

The condensation of a series of aromatic ketones with aromatic aldehydes under aldol conditions affords 1-aryl-3-(substituted-phenyl/phenyl furanyl/thienyl)-2-propen-1-ones 1. The resulting propenones undergo facile and clean cyclization with hydrazine and substituted hydrazine derivatives to yield 3-aryl-5-(substitutedphenyl/phenylfuranyl/thienyl)-2-pyrazolines 2. This reaction is carried out in the presence of Amberlyst-15 catalyst to afford the above pyrazolines 2 in considerably good yield. All the synthesized compounds have been characterized by spectral studies.

http://nopr.niscair.res.in/bitstream/123456789/6224/1/IJCB%2045B%282%29%20568-571.pdf

P. M. Akberali

Papers

Synthesis and studies on some new fluorine containing triazolothiadiazines as possible antibacterial, antifungal and anticancer agents.

One pot synthesis of thiazolodihydropyrimidinones and evaluation of their anticancer activity.

Synthesis and Studies on Some New Fluorine Containing Triazolothiadiazines as Possible Antibacterial, Antifungal and Anticancer Agents.

Synthesis of pyrazolines promoted by Amberlyst-15 catalyst

Synthesis of Pyrazolines Promoted by Amberlyst-15 Catalyst.