Pyrazole containing natural products: Synthetic preview and biological significance
TL;DR: The present review is an attempt to understand the chemistry along with medicinal importance of pyrazole containing natural products reported till date which would certainly help the scientific community to bring further developments in the isolation and synthetic methodologies for pyrazoles based novel bioactive compounds.
About: This article is published in European Journal of Medicinal Chemistry.The article was published on 2013-11-01. It has received 426 citations till now.
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TL;DR: In this article, the authors summarize strategies to synthesize pyrazole derivatives and demonstrate that this class of compounds can be targeted for the discovery of new drugs and can be readily prepared owing to recent advances in synthetic medicinal chemistry.
Abstract: Nitrogen-containing heterocyclic compounds and their derivatives have historically been invaluable as a source of therapeutic agents. Pyrazole, which has two nitrogen atoms and aromatic character, provides diverse functionality and stereochemical complexity in a five-membered ring structure. In the past decade, studies have reported a growing body of data on different pyrazole derivatives and their innumerable physiological and pharmacological activities. In part, such studies attempted to reveal the wide range of drug-like properties of pyrazole derivatives along with their structure–activity relationships in order to create opportunities to harness the full potentials of these compounds. Here, we summarize strategies to synthesize pyrazole derivatives and demonstrate that this class of compounds can be targeted for the discovery of new drugs and can be readily prepared owing to recent advances in synthetic medicinal chemistry.
460 citations
TL;DR: Owing to the development of novel and new pyrazole based therapeutic agents at a faster pace, there is a need to couple the latest information with previously available information to understand status of this moiety in medicinal chemistry research.
286 citations
TL;DR: Progress is made in the catalytic asymmetric synthesis of pyrazoles and pyrazolones using pyrazolin-5-one derivatives using organo- and metal-catalysts.
215 citations
TL;DR: This review mainly focuses on the existence of isoxazoline derivatives in natural sources, their isolation and uses there of as anticancer agents besides highlighting the synthetic pathways to achieve these compounds.
190 citations
TL;DR: A series of forty different pyrazole containing benzimidazole hybrids have been designed, synthesized and evaluated for their potential anti-proliferative activity against three human tumor cell lines - lung, breast, and cervical.
149 citations
References
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TL;DR: A great number of structurally diverse natural products containing five-membered heterocyclic subunits, such as imidazoles, oxazole, thiazole, and their saturated congeners, are abundant in nature and exhibit extensive and pharmacologically important biological activities.
398 citations
TL;DR: The structure, biosynthesis and analysis of artemisinin and its mode of action are described, and the production strategies including organic synthesis, extraction from plants, in vitro cultures and alternative strategies for enhancing the yields are discussed.
250 citations
TL;DR: The results revealed that the compound 11c having 2,5-dichlorothiophene substituent on pyrazole moiety and a triazole ring showed significant analgesic and antimicrobial activity.
246 citations
TL;DR: Slight prolongation in the survival period of mice inoculated with lymphatic leukemia L1210 was observed by intraperitoneal injection of bredinin, however, it was not effective on P388 leukemia or EHRLICH ascites tumor.
Abstract: Bredinin, C9H13N3O6, is, a novel imidazole nucleoside with an immunosbppressive activity. It was isolated from the culture filtrate of Eupenicillium brefeldianum M-2166 by means of ion-exchange or partition chromatography. Bredinin shows selective cytotoxicity against L5178Y cells derived from malignant lymphoma of the mouse. As an immunosuppressant, it has favorable characteristics, namely, a potent activity, low acute toxicity, and a slight effect on a decrease of peripheral leukocytes. Bredinin inhibits the growth of vaccinia virus but not that of bacteria or fungi except for Candida albicans in vitro.Slight prolongation in the survival period of mice inoculated with lymphatic leukemia L1210 was observed by intraperitoneal injection of bredinin, however, it was not effective on P388 leukemia or EHRLICH ascites tumor.
232 citations