Natural Products Journal, The - Volume 4, Issue 2, 2014

Natural Products Journal is one of the extremely important journals of Bentham Science Publishers. The current issue has been focused on to uncover many physico-chemical interactions persisting with regards to structural-function relationships of azole compounds and more importantly their therapeutic potential. Efforts have been made to find a link between natural and synthetic azoles’ composition and structure with their physiological or therapeutic role through various articles contributed by diverse range of authors. Here is the brief summary of the articles: Kim et al., emphasized upon Pyrazoline heterocycles which occupy a distinct attention in the field of synthetic and medicinal chemistry exhibiting a wide spectrum of biological activities including anti-inflammatory, anti-microbial, cytotoxic, anticonvulsant etc. [1-3]. Authors have made a sincere effort to review the synthetic and biological significance of Pyrazoline derivatives bringing together most of the recent studies. Varughese et al., shed light on the broad-spectrum antimicrobial and therapeutic role of azole compounds in treating cancer linked fungal infections like candidiasis and aspergillosis. Authors have drawn comparisons between first First generation azoles with that of newer azoles in terms of their action potential and activity against resistant organisms. The role of azoles has been further extended to prostate cancer and breast cancer therapy through this article [4-6]. Sandhu et al., have shown promise in Azoles as effective antifungal agents. Authors are concerned about the growing resistance against azoles in fungal pathogens and side effects accompanied with the use of synthetic azoles which makes it necessary to search for some natural and effective azoles [6-10]. Authors have shown structure-function analysis of clinically important antifungal azoles derivatives through the collection of studies and also reviewed some important patents related to them. Malik et al., mainly gained insight into the mechanistic preview as to how azole compounds bind to lanosterol 14α- demethylase and prevent the demethylation of lanosterol, thereby inhibitiing the fungal growth. Authors have focused their attention on antifungal potential of azole compounds with an emphasis on the corresponding drug resistance episode complemented with novel strategies for the development of new generation of azole compounds [11-14]. Gupta et al., reviewed the antimicrobial importance of natural imidazoles, their mode of actions and structure-activity relationship. The article would certainly help scientific community to bring further modifications or developments in the synthetic methodologies to biologically active compounds based on natural products containing imidazole moiety [15]. Thus natural imidazoles could be used as effective chemotherapeutics in future. Another article by Gupta et al., emphasized upon the effective use of second and third generation azole compounds against systemic fungal infections [16]. Given their toxicity profile being better than that of the first-generation triazoles and drug interactions remain manageable; these compounds represent a true expansion of antifungal arsenal for the future. Kumar and Kaur emphasized upon the use of Triazoles and Oxadiazoles which are nitrogen and nitrogen-oxygen containing heterocycles, for the development of effective chemotherapeutic candidates. The article not only focuses on the biological importance of triazole and oxadiazole derivatives but also highlights synthetic pathways to achieve such compounds which would certainly help the scientific community to bring further developments in the isolation and synthetic methodologies for azole- based novel bioactive agents [17-21]. The continued success of the Journal is the result of a joint effort by a dedicated editorial team under the leadership of Dr. Naeem and we will continue to evolve progressively for the benefit of our contributors and readers. While thanking all the editorial members for their continued support and cohesive interactions, we reiterate our commitment for ethical and quality publications in frontier areas of Natural Product research. The lead guest editors and the executive editor would like to extend their gratitude to authors of this issue for their valuable scientific contributions. We simultaneously thank the valuable comments and suggestions of the reviewers to further improve the quality and scientific perspective of the articles. We eagerly look forward to receiving hot novel areas for contribution to The Natural Products Journal in future. In the end, if you have any questions or suggestions to further improve the journal, please feel free to drop a line to the executive editor of NPJ.

Imidazoles, natural or synthetic constitute an important class of bioactive heterocycles which have been found more effective in the treatment of various infectious and life threatening diseases. They exhibit a broad spectrum of biological activities such as anti-diabetic, antiviral, anticancer, anti-inflammatory, antibacterial and antifungal etc. The purpose of this review is to provide an overall update of the imidazole containing natural products mainly possessing antifungal and antibacterial activities till 2014.

Fungal infection is one of the most common infections affecting millions of people every year. Moreover, it is quiet prevalent in immuno-compromised patients. The recent expansion of antifungal drug research is gaining momentum continuously for the development of new and less toxic antifungals which further gave us an azole group. Nowadays, Azole containing drugs are having immense therapeutic potential with many properties including anti carcinogenic, antibacterial, and antiviral. Current review is mainly focused on the recent trends in efficacy of antifungal property of Azole containing drugs and their further scope and relevance in today’s context.

Among azole heterocycles, Pyrazolines have gained much attention in the field of synthetic and medicinal chemistry. They exhibit a wide spectrum of biological activities such as anti-inflammatory, anti-microbial, cytotoxic, anticonvulsant etc. In view of immense applications, particularly in pharmaceutical sector, here an effort has been made to review the results related to their synthetic and biological significance disclosed after year 2001-2013.

Triazoles and oxadiazoles are nitrogen and nitrogen-oxygen containing heterocycles, respectively that belong to the azoles family. They have gained much attention of the synthetic and medicinal chemists as some of the natural products containing azole moiety contribute towards the development of some effective chemotherapeutic candidates. Therefore, this review mainly focuses on the existence of triazole and oxadiazole derivatives in natural sources, their isolation and biological importance besides highlighting the synthetic pathways to achieve these compounds. It covers the literature upto 2014 and would certainly provide a great insight to scientific community to bring further developments in the isolation and synthetic methodologies for triazole and oxadiazole based novel bioactive agents.

Azoles have consistently been recognized as the mainstays of antifungal drugs, amongst which ergosterol prevails as an integral component of fungal plasma membrane. It is most commonly produced via demethylation of lanosterol by the cytochrome P450-dependent enzyme lanosterol 14α-demethylase. Azoles exert their antifungal activities via binding to lanosterol 14 α-demethylase and thereby preventing the demethylation of lanosterol. This leads to the depletion of demethylated lanosterol (ergosterol) with the concomitant accumulation of methylated sterol precursors (lanosterol, 4,14-dimethylzymosterol, and 24-methylenedihydrolanosterol) and deterioration of the membrane integrity, resulting in fungal growth inhibition. Resistance to azoles is a concern, particularly during the long-term treatment of fungus mediated cellular complications. To combat azole resistance and to extend the spectrum of treatable pathogens, the development of novel and more potent azoles, with alteration in active sites has attracted worldwide scientific attention. With such an insight, this review focuses on antifungal potentials of azole compounds with an emphasis on the corresponding drug resistance episodes complemented with novel strategies for the development of new generation of azole compounds.

Despite numerous efforts by researchers the increasing fungal infections are still a major threat to the society. To combat this dilemma several antifungal drugs have come up through extensive research. Azoles are one of the most promising antifungal agents of them. They are heterocyclic five membered organic compounds which show activity against hazardous fungal pathogens. But the growing resistance against azoles in fungal pathogens and side effects accompanied with the use of synthetic azoles has generated an urgent need to search for natural and eco-friendly azoles. The present review provides a detailed account about the structure and function of clinically important antifungal azole derivatives and some patents related to them. This article also gives a brief overview about some naturally derived antifungal azoles.

Presently, azoles have emerged as excellent antifungal agents. Their broad-spectrum activity and ability to treat superficial as well as invasive infections have gained them incredible repute in antimicrobial therapy. Azoles inhibit the synthesis of ergosterol in fungi, which is important for maintaining the cell wall. This review briefly portrays the relevance of azoles in treating cancer linked fungal infections like candidiasis and aspergillosis. First generation azoles like itraconazole and fluconazole are preferred over other drugs like amphotericin B. Newer azoles (triazoles like voriconazole, posaconazole and ravuconazole) have been synthesized to oust the earlier varieties by being more potent and active against resistant organisms. Patients with lymphoma or leukemia undergoing chemotherapy or stem cell transplantation have weak immune status which makes them susceptible hosts of fungal infections. Azoles are used currently for antitumor therapy because of their specificity towards human cytochrome P-450 dependent enzymes which synthesize cholesterol. This review also attempts to point out how their applications in prostate cancer and breast cancer therapy are indispensable. But along with its advantages, it is necessary to look into the sinister role it plays in creating toxic side effects for patients. Disruption of the endocrine functioning and hepatotoxicity result in manifestations like vomiting, nausea and fatigue. Even though these complications are reversible, the full-fledged practicability of these drugs in cancer treatment is yet to be considered.