scholarly journals Synthetic Methods, Chemistry, and the Anticonvulsant Activity of Thiadiazoles

2013 ◽  
Vol 2013 ◽  
pp. 1-16 ◽  
Author(s):  
Bhawna Sharma ◽  
Amita Verma ◽  
Sunil Prajapati ◽  
Upendra Kumar Sharma

The chemistry of heterocyclic compounds has been an interesting field of study for a long time. Heterocyclic nucleus 1,3,4-thiadiazole constitutes an important class of compounds for new drug development. The synthesis of novel thiadiazole derivatives and investigation of their chemical and biological behavior have gained more importance in recent decades. The search for antiepileptic compounds with more selective activity and lower toxicity continues to be an active area of intensive investigation in medicinal chemistry. During the recent years, there has been intense investigation of different classes of thiadiazole compounds, many of which possess extensive pharmacological activities, namely, antimicrobial activity, anticonvulsant, antifungal antidiabetic, anti-inflammatory, antioxidant, and antituberculosis activities, and so forth. The resistance towards available drugs is rapidly becoming a major worldwide problem. The need to design new compounds to deal with this resistance has become one of the most important areas of research today. Thiadiazole is a versatile moiety that exhibits a wide variety of biological activities. Thiadiazole moiety acts as “hydrogen binding domain” and “two-electron donor system.” It also acts as a constrained pharmacophore. On the basis of the reported literature, we study here thiadiazole compounds and their synthetic methods chemistry and anticonvulsant activity.

Author(s):  
Mohammad Mukim ◽  
Atul Kabra ◽  
Christophe Hano ◽  
Samantha Drouet ◽  
Duangjai Tungmunnithum ◽  
...  

Rivea hypocrateriformis (Desr.) Choisy is a robust woody climbing shrub of the genus Rivea which is found in India, Nepal, Sri Lanka, Pakistan, Bangladesh, Myanmar and Thailand. R. hypocrateriformis is a promising medicinal herb with enormous helpful and wellbeing advancing impacts. R. hypocrateriformis has been utilized as a customary medication for a long time to treat rheumatic pain, fever, urogenital problem, snake bite, cough, piles, malaria, and skin disease. Apart from the traditional uses its leaves and young shoots are cooked and eaten as a vegetable and for preparation of bread with millet flour. This review comprehensively summarizes the up-to-date information on the botanical characterization, distribution, traditional uses, phytochemistry, pharmacology and toxicity study of R. hypocrateriformis. Phytochemical investigation has been revealed that alkaloids, glycosides, coumarins, flavonoids, xanthones, stilbenes, and other organic compounds are contained in R. hypocrateriformis. Crude extracts and isolated compounds have exhibited numerous pharmacological activities such as anovulatory effect, antifertility activity, antiarthritic, antimicrobial, anticancer, antioxidant, hepatoprotective, antilithiatic, antimitotic. R. hypocrateriformis is a promising restorative spice with monstrous remedial and wellbeing advancing impacts. Along these lines, further investigations on the bioactive mixtures and systems of R. hypocrateriformis are justified. Extra clinical and toxicological examinations are expected to assess its wellbeing.


Catalysts ◽  
2020 ◽  
Vol 10 (10) ◽  
pp. 1178
Author(s):  
Guillermo Otárola ◽  
Juan J. Vaquero ◽  
Estíbaliz Merino ◽  
Manuel A. Fernández-Rodríguez

Four carbon ring systems are frequently present in natural products with remarkable biological activities such as terpenoids, alkaloids, and steroids. The development of new strategies for the assembly of these structures in a rapid and efficient manner has attracted the interest of synthetic chemists for a long time. The current research is focused mainly on the development of synthetic methods that can be performed under mild reaction conditions with a high tolerance to functional groups. In recent years, gold complexes have turned into excellent candidates for this aim, owing to their high reactivity, and are thus capable of promoting a wide range of transformations under mild conditions. Their remarkable efficiency has been thoroughly demonstrated in the synthesis of complex organic molecules from simple starting materials. This review summarizes the main synthetic strategies described for gold-catalyzed four-carbon ring formation, as well as their application in the synthesis of natural products.


2019 ◽  
Vol 19 (10) ◽  
pp. 809-825 ◽  
Author(s):  
Qing-Shan Li ◽  
Yao Li ◽  
Girdhar Singh Deora ◽  
Ban-Feng Ruan

Resveratrol is a non-flavonoid polyphenol containing a terpenoid backbone. It has been intensively studied because of its various promising biological properties, such as anticancer, antioxidant, antibacterial, neuroprotective and anti-inflammatory activities. However, the medicinal application of resveratrol is constrained by its poor bioavailability and stability. In the past decade, more attention has been focused on making resveratrol derivatives to improve its pharmacological activities and pharmacokinetics. This review covers the literature published over the past 15 years on synthetic analogues of resveratrol. The emphasis is on the chemistry of new compounds and relevant biological activities along with structure-activity relationship. This review aims to provide a scientific and reliable basis for the development of resveratrol-based clinical drugs.


Author(s):  
Mohammad Asif ◽  
Mohammad Imran

: Green synthesis of oxazine and thiazine derivatives have concerned a great impact of concern of medicinal researchers and provided a lead molecule for the design and development of various potential bioactive molecules. This review associated additional green synthetic information and it would extend a great deal of help to researchers in synthesizing the most productive, economical, and clinically important thiazine and oxazine derivatives which will be expected to show potent pharmacological activities. This has led to the discovery of various compounds that have diverse types of interesting biological activities. Propose of this article is to study the various synthetic methods of oxazine and thiazine derivatives by green chemistry methods and their biological activities. We expect that this article will be interesting for researchers concerned with oxazine and thiazine compounds.


Molecules ◽  
2020 ◽  
Vol 25 (2) ◽  
pp. 301 ◽  
Author(s):  
Noha Khalil ◽  
Mokhtar Bishr ◽  
Samar Desouky ◽  
Osama Salama

Ammi visnaga L. (Visnaga daucoides Gaertn., Family Apiaceae), also known as Khella Baldi or toothpick weed, is an annual or biennial herb indigenous to the Mediterranean region of North Africa, Asia, and Europe. The plant is known to have been used in traditional medicine a long time ago. Nowadays, it is used in modern medicine to treat many aliments such as renal colic and coronary insufficiency, and is used as an antioxidant, antifungal, and antibacterial, with a larvicidal effect on mosquito larvae. Peer-reviewed studies show that these pharmacological activities are due its valuable chemical constituents that include mainly essential oil, polyphenolic compounds including flavonoids, as well as γ-pyrones, represented mainly by khellin and visnagin. Its essential oil is reported to have antiviral, antibacterial, and larvicidal effects, while its flavonoid content is responsible for its antioxidant activity. Its γ-pyrone content has a powerful effect on facilitating the passage of kidney stones and relieving renal colic, in addition to having a relaxant effect on smooth muscle including that of the coronary arteries. The current review represents the progress in research on A. visnaga in terms of either its chemistry or biological activities. This review represents scientific support material for the use of the plant by the pharmaceutical industry.


2021 ◽  
Vol 8 (5) ◽  
pp. 365-378
Author(s):  
V. S. Anjana ◽  
P. Manoj Kumar

Benzotriazole (BTA) is a nitrogen containing heterocyclic derivative containing three nitrogen atoms at 1st, 2nd and 3rd positions with chemical formula C6H5N3. Benzotriazole and its derivatives have great significance in medicinal chemistry and these derivatives were used by several chemists for therapeutic conditions because it possessing a wide spectrum of pharmacological activities including anti bacterial, anti fungal, anti viral, anti inflammatory, anti hyperglycemic, anti hypertensive, anti cancer and analgesic activity. In this review, different synthetic methods for the preparation of benzotriazole, importance of benzotriazole derivatives in biomedical research, highlighting its biological behavior, versatile activities and Structure Activity Relationship (SAR) studies are described. This review will help the researchers to understand the structure activity relationships and improvise the concepts in their research field. Keywords: Benzotriazole, Anti microbial, Anthelmintic, Analgesic, Anti mycobacterial, Anti viral, Anti oxidative, Anti tumor, Anti inflammatory, Anti hyperglycemia, Anti fungal, Anticonvulsant activity.


2020 ◽  
Vol 24 (12) ◽  
pp. 1315-1330
Author(s):  
Hui Lei ◽  
Peng Jiang ◽  
Dan Zhang

Gorgonian corals are considered as a rich source of secondary metabolites with unique structural features and biological activities. A large number of novel metabolites with potent pharmacological properties have been isolated from gorgonian corals. Some of these compounds have exhibited to possess new mechanisms of action, which hold great promises as potential lead compounds in future marine drug development. This review aims to provide an overview of chemical constituents and biological activities of gorgonian corals from 2015 to December, 2019. Some 145 metabolites, including 16 sesquiterpenoids, 62 diterpenoids, 62 steroids and 5 alkaloids were reported during this period and their pharmacological activities were investigated. Moreover, the peculiar structure and potential medicinal value of these new compounds are discussed in this review.


2021 ◽  
Vol 24 (5-esp.) ◽  
pp. 667-671
Author(s):  
Adélia Segin Vale Velosa ◽  
Vagner Pereira da Silva ◽  
Susana Nogueira Diniz Cristina ◽  
Cristina Eunice Okuyama Costa ◽  
Márcio Luiz Dos Santos ◽  
...  

Sulfonamida é uma classe de compostos de interesse para obtenção de novos medicamentos por apresentar propriedades químicas e biológicas como antitumoral, antimicrobiana, antifúngica, anti-inflamatória, antiobesidade, diurético, hipoglicêmico, anti-neuropática, entre outras. Mais de trinta medicamentos contendo esse grupo funcional estão em uso clínico, incluindo antibacterianos, diuréticos, anticonvulsivantes, hipoglicêmicos e inibidores de protease do vírus da imunodeficiência humana (HIV). Aproximadamente, 150 diferentes sulfonamidas são comercializadas como agentes bactericidas, contendo variações estruturais para potencializar a eficiência e solubilidade em sistemas biológicos. É importante estabelecer métodos rápidos e simples para a síntese de novas sulfonamidas com rendimento satisfatório. Nesse trabalho foi relatado um método sintético eficiente e fácil para obter sulfonamidas à partir da cumarina-6-clorossulfonada e as aminas primárias, tercbutilamina (CSNtert), isobutilamina (CSNiso) e isopropilamina (CSNisop) com rendimento de 71%. Essas novas sulfonamidas à base de cumarina foram caracterizadas por análise elementar, espectroscopia ultravioleta, espectroscopia no infravermelho por refletância total atenuada (ATR) e Ressonância Magnética Nuclear de 1H e 13C. Além disso, foram realizados testes de condutividade e ponto de fusão. A caracterização espectroscópica e química confirmou a formação de novos compostos e foi possível propor sua estrutura. Estudos da citotoxicidade da CSNtert, CSNiso e CSNisop em células epiteliais normais mostrou que estes compostos apresentam menor citotoxicidade que a cumarina-6-clorossulfonada.   Palavras-chave: Cumarina. Sulfonamida. Síntese   Abstract Sulfonamide is an important class of compounds that play an important role in the discovery of new medicines due to its  broad chemical and biological activities such as antitumoral, antimicrobial, antifungic, anti-inflammatory, anti-obesity, diuretic, hypoglycemic, anti-neuropathic pain activities, among others. More than 30 drugs containing this functional group are in clinical use, including, antibacterial, diuretics, anticonvulsants, hypoglycemic and human immunodeficient virus (HIV) protease inhibitors. Approximately 150 different sulfonamides have been sold as bactericidal agents, and structural variations seems to increase their efficiency, potency and solubility in biological systems. Fast and simple synthetic methods for the construction of new sulfonamides with satisfactory yielding are important to be stablished. In this work an efficient and easy synthetic method  was reported to obtain sulfonamides from coumarin-6-sulfonyl chloride and primary amines, tert-butyl amine (CSNtert), isobutylamine (CSNiso) and isopropylamine (CSNisop) with excellent yield, (71%). These new coumarin-based sulfonamides were characterized by elementary analysis, spectroscopy UV, Infrared by Attenuated Total Reflectance (ATR) and Nuclear Magnetic Resonance of 1H and 13C. In addition, conductivity tests were performed and melting point determined. The spectroscopic and chemical characterization confirmed the structures of the new compounds and could be possible to propose the structure. Studying their cytotoxicity against normal epithelial cells shows that the new compounds have lower cytotoxicity than coumarin-6-sulfonyl chloride.   Keywords: Coumarin. Sulfonamide. Synthesis


2017 ◽  
Author(s):  
Mohit S. Verma ◽  
Michael J. Fink ◽  
Gabriel L Salmon ◽  
Nadine Fornelos ◽  
Takahiro E. Ohara ◽  
...  

Two biological activities of butyrate in the colon (suppression of proliferation of colonic epithelial stem cells and inflammation) correlate with inhibition of histone deacetylases. Cellular and biochemical studies of molecules similar in structure to butyrate, but different in molecular details (functional groups, chain-length, deuteration, oxidation level, fluorination, or degree of unsaturation) demonstrated that these activities were sensitive to molecular structure, and were compatible with the hypothesis that butyrate acts by binding to the Zn<sup>2+</sup> in the catalytic site of histone deacetylases. Structure-activity relationships drawn from a set of 36 compounds offer a starting point for the design of new compounds targeting the inhibition of histone deacetylases. The observation that butyrate was more potent than other short-chain fatty acids is compatible with the hypothesis that crypts evolved (at least in part), to separate stem cells at the base of crypts from butyrate produced by commensal bacteria.


2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.


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