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Thiadiazoles: the appropriate pharmacological scaffolds with leishmanicidal and antimalarial activities: a review.

ABSTRACT: Leishmaniasis and malaria are serious public health problems in tropical and sub-tropical regions worldwide. Development of drug-resistant strains has disrupted efforts to control the spread of these diseases in the world. The conventional antiparasitic chemotherapy still suffers from side effects and drug resistance. Therefore, the development of novel antimalarial and leishmanicidal drugs remains a critical topic to combat against these diseases. Five-membered heterocyclic systems have possessed antiparasitic activity such as thiadiazole scaffold which is a prevalent and an important heterocyclic ring. For this purpose, the authors introduce a series of synthetic thiadiazole derivatives with antileishamanial activity. Also, the authors searched a number of sources and articles to find thiadiazole derivatives with antileishamnial and antimalarial activity. Then all of the findings were reviewed. 5-nitroheteroaryl-1,3,4-Thiadiazole derivatives with different substituents at position 2 of the thiadiazole ring (8, 10-11) presented the best antileishmanial activity with low toxicity compared with reference drug. Also, 1,3,4-thiadiazole-2-sulfonamide derivative (18) showed excellent inhibitory activity against pfCA as a special enzyme in Plasmodium falciparum. Thiadiazole scaffold has the suitable physicochemical and pharmacokinetic properties and still stays as a therapeutic target for the development of a novel lead in the medicinal chemistry. Therefore, the current review provides a brief summary of medicinal chemistry of thiadiazole ring and introduces novel leads possessing this nucleus with antimalarial and antileishmanial activities.

SUBMITTER: Tahghighi A

PROVIDER: S-EPMC5569449 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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Thiadiazoles: the appropriate pharmacological scaffolds with leishmanicidal and antimalarial activities: a review.

Tahghighi Azar A Babalouei Fateme F

Iranian journal of basic medical sciences 20170601 6

Leishmaniasis and malaria are serious public health problems in tropical and sub-tropical regions worldwide. Development of drug-resistant strains has disrupted efforts to control the spread of these diseases in the world. The conventional antiparasitic chemotherapy still suffers from side effects and drug resistance. Therefore, the development of novel antimalarial and leishmanicidal drugs remains a critical topic to combat against these diseases. Five-membered heterocyclic systems have possess ...[more]

PMID: 28868117

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Project description:BackgroundMalaria still constitutes a major public health menace, especially in tropical and subtropical countries. Close to half a million people mainly children in Africa, die every year from the disease. With the rising resistance to frontline drugs (artemisinin-based combinations), there is a need to accelerate the discovery and development of newer anti-malarial drugs. A systematic review was conducted to identify the African medicinal plants with significant antiplasmodial and/or anti-malarial activity, toxicity, as wells as assessing the variation in their activity between study designs (in vitro and in vivo).MethodsKey health-related databases including Google Scholar, PubMed, PubMed Central, and Science Direct were searched for relevant literature on the antiplasmodial and anti-malarial activities of African medicinal plants.ResultsIn total, 200 research articles were identified, a majority of which were studies conducted in Nigeria. The selected research articles constituted 722 independent experiments evaluating 502 plant species. Of the 722 studies, 81.9%, 12.4%, and 5.5% were in vitro, in vivo, and combined in vitro and in vivo, respectively. The most frequently investigated plant species were Azadirachta indica, Zanthoxylum chalybeum, Picrilima nitida, and Nauclea latifolia meanwhile Fabaceae, Euphorbiaceae, Annonaceae, Rubiaceae, Rutaceae, Meliaceae, and Lamiaceae were the most frequently investigated plant families. Overall, 248 (34.3%), 241 (33.4%), and 233 (32.3%) of the studies reported very good, good, and moderate activity, respectively. Alchornea cordifolia, Flueggea virosa, Cryptolepis sanguinolenta, Zanthoxylum chalybeum, and Maytenus senegalensis gave consistently very good activity across the different studies. In all, only 31 (4.3%) of studies involved pure compounds and these had significantly (p = 0.044) higher antiplasmodial activity relative to crude extracts. Out of the 198 plant species tested for toxicity, 52 (26.3%) demonstrated some degree of toxicity, with toxicity most frequently reported with Azadirachta indica and Vernonia amygdalina. These species were equally the most frequently inactive plants reported. The leaves were the most frequently reported toxic part of plants used. Furthermore, toxicity was observed to decrease with increasing antiplasmodial activity.ConclusionsAlthough there are many indigenous plants with considerable antiplasmodial and anti-malarial activity, the progress in the development of new anti-malarial drugs from African medicinal plants is still slothful, with only one clinical trial with Cochlospermum planchonii (Bixaceae) conducted to date. There is, therefore, the need to scale up anti-malarial drug discovery in the African region.

Project description:ObjectivesPlants have been used as traditional medicine (TM) since ancient times and TM remains an effective treatment option in the primary health care system in developing countries, including Bangladesh. There are several reasons to use plants as TM, which are cheaply and easily available and have a cultural heritage of their uses across generations. Leea, a genus of the Vitaceae family, possesses a large number of medicinal plants. In this review, the literature data on the traditional uses and pharmacological activities of Leea species and their phytochemicals are compiled. All the information was collected from the scientific databases.ResultsLeea species are endemic that have opened a promising research field to identify new leads against different diseases. Leea contains approximately 70 species, which are widely distributed throughout the Northern and Eastern Australia, South and Southeast Asia and parts of Africa. The Leea plants are used traditionally in different ailments such as fever, diarrhea, dysentery, joint pain, rheumatism, diabetes, bone fracture, body ache, wound, sexual disorders, and so on. The majority of the Leea species are the medicinal plants, which have anticancer, cytotoxic, antimicrobial, antidiabetic, hepatoprotective, cardiovascular, and CNS activity. Moreover, phytochemicals such as flavonoids, glycosides, phenols, terpenoids, steroids, volatile oils, alkaloids, proteins, quinine derivatives, tannins, saponins, and many other organic compounds have been reported in the Leea species (Leea indica, Leea macrophylla, Leea asiatica, Leea aequata, Leea rubra and Leea guineensis). The presence of phytochemicals and the in vitro and in vivo biological activities reported of these plants support their use as TM. Though original research articles related to the Leea genus are available, supportive reviews on phytochemicals and pharmacological activities remain scarce.ConclusionLeea species are used as TM in different ailments and have a real interest in their diverse pharmacological properties. Also, Leea species contain a remarkable number of bioactive compounds. This review has provided a comprehensive report on the plants of Leea genus to identify its therapeutic potential and future prospects for betterment research. However, chemical and biological investigations of several species of Leea genus remain unexplored. Therefore, further studies on these species are necessary, especially regarding pharmacological properties, isolation of the compounds and mechanism of action for the development of new drugs.

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Thiadiazoles: the appropriate pharmacological scaffolds with leishmanicidal and antimalarial activities: a review.

Publications

Thiadiazoles: the appropriate pharmacological scaffolds with leishmanicidal and antimalarial activities: a review.

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