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Furanone, a five-membered heteroaromatic ring containing oxygen atom, is of immense pharmaceutical importance. Presence of this nucleus in biologically active compounds of natural and synthetic origin has made it an indispensable motif for design and development of new therapeutic agents. In recent years synthesis of furanone derivatives and exploring their therapeutic actions has been the prime interest amongst researchers. Furanone containing compounds cover numerous therapeutic categories viz. Analgesic and anti-inflammatory, anticancer, anticonvulsant, antibacterial and antifungal, antioxidant, antiulcer and anti-TB, etc. There is a need to couple recent work done with previously available information on furanone, a well acknowledged scaffold, to help scientists to develop novel and new furanone based therapeutic agents at a faster pace. This updated review highlights the worth of numerous therapeutically active furanone based compounds developed by the medicinal chemists. SAR studies have also been derived which may be useful for rational designing of furanone derivatives with improved therapeutic index. Image 1 • 2(5H) furanone derivatives emerged as the most promising anti-inflammatory, anti-cancer and anti-microbial agents. • The review covers useful pharmacological activities of furanone derivatives along with SAR studies. • It provides an overview of research work carried out on furanones in past three decades. • Enlist the patents granted on furanones and drugs containing furanone nucleus. [ABSTRACT FROM AUTHOR]

Abstract: We present a 27-year-old man with pure anterior dislocation of the ankle joint following a fall from height. There were no accompanying fractures in and around the ankle joint. The injury was initially missed on clinical examination in view of minimal ankle deformity. The patient was managed conservatively with closed reduction and plaster immobilisation. The case report highlights the importance of early diagnosis and management of anterior ankle dislocation to obtain good functional outcome. A review of the literature on this rare injury is also presented. [Copyright &y& Elsevier]

Several generations of antiepileptic drugs (AEDs) are available in the market for the treatment of seizures, but these are amalgamated with acute to chronic side effects. The most common side effects of AEDs are dose-related, but some are idiosyncratic adverse drug reactions (ADRs) that transpire due to the formation of reactive metabolite (RM) after the bioactivation process. Because of the adverse reactions patients usually discontinue the medication in between the treatment. The AEDs such as valproic acid, lamotrigine, phenytoin etc., can be categorized under such types because they form the RM which may prevail with life-threatening adverse effects or immune-mediated reactions. Hepatotoxicity, teratogenicity, cutaneous hypersensitivity, dizziness, addiction, serum sickness reaction, renal calculi, metabolic acidosis are associated with the metabolites of drugs such as arene oxide, N -desmethyldiazepam, 2-(1-hydroxyethyl)-2-methylsuccinimide, 2-(sulphamoy1acetyl)-phenol, E−2-en-VPA and 4-en-VPA and carbamazepine-10,11-epoxide, etc. The major toxicities are associated with the moieties that are either capable of forming RM or the functional groups may itself be too reactive prior to the metabolism. These functional groups or fragment structures are typically known as structural alerts or toxicophores. Therefore, minimizing the bioactivation potential of lead structures in the early phases of drug discovery by a modification to low-risk drug molecules is a priority for the pharmaceutical companies. Additionally, excellent potency and pharmacokinetic (PK) behaviour help in ensuring that appropriate (low dose) candidate drugs progress into the development phase. The current review discusses about RMs in the anticonvulsant drugs along with their mechanism vis -a- vis research efforts that have been taken to minimize the toxic effects of AEDs therapy. [Display omitted] • Reactive metabolites of established antiepileptic drugs (AEDs) with their acute/chronic side-effects are reported. • Various synthetic strategies to minimize the toxicity under each category of AEDs are discussed. • Preclinical data for the synthesized derivatives is represented as compared to standard AEDs. • Structural activity relationship has been discussed for various synthesized derivatives. [ABSTRACT FROM AUTHOR]

• Recent developments of nitrogen-containing heterocyclic compounds as antidepressant have been discussed. • The antidepressant profile of the potent derivatives along with structural insights is presented. • The SAR studies of recently developed compounds are discussed in details for providing key structural features. • The lead compounds for further development are identified and discussed in the perspective part of this review. According to the World Health Organization (WHO), depression is a common mental disorder and includes complex interaction between social and psychological behaviour affecting 264 million people worldwide. The review aims to highlight the role and importance of nitrogen-based heterocyclics in the development of antidepressant compounds. Many research groups have attempted to design drug candidates capable of binding within the receptors. The commonest drug design strategy includes the incorporation of different structural features widely recognized as an antidepressant in the synthesized derivatives to enhance their CNS antidepressant effects. In this review, we have shed light on nitrogenous heterocyclic moieties such as quinazoline, pyridine, pyrimidine, pyrrolidine, imidazole, pyrazole, piperidine, oxadiazole, benzimidazole, benzothiazole, piperazine, triazine, purine, benzoxazole, and isoxazole as core nucleus and/or in combination as an antidepressant compound. These molecules with different structural features were noted to exert their antidepressant effects by multiple mechanisms viz., selective serotonin reuptake inhibitors (SSRIs), monoamine oxidase (MAO) inhibitors, and Catechol- O -methyltransferase (COMT) inhibitors. The review focuses on the selection of these heterocyclic moieties for the further design and development of promising antidepressants by taking a clue from the earlier reported potent antidepressant compounds or from the marketed products. The results have been correlated with their structural activity relationship (SAR) to identify the substituents for the potency and selectivity within the receptors. This review might help the researchers working in the antidepressant field to develop more novel molecules that could fill the gap by improving potency and reducing toxicity. [Display omitted] [ABSTRACT FROM AUTHOR]

Abstract: Low grade central osteosarcoma is a rare primary bone tumor. This fibro-osseous lesion shares some radiological and histopathological resemblance with fibrous dysplasia, which is a more common entity. Thus it may be mistaken as fibrous dysplasia and may receive inadequate treatment resulting in a more malignant recurrent bone tumor. We present a case of low grade central osteosarcoma of the right tibia, which was initially treated as fibrous dysplasia with curettage and bone grafting. Three years later the tumor recurred with greater soft tissue and bony involvement but without metastasis. The patient was treated with above knee amputation and has been asymptomatic for the last two years. [Copyright &y& Elsevier]

Résumé: L’ostéosarcome central de faible malignité est une tumeur osseuse primitive rare. En raison de certaines caractéristiques radiographiques et histologiques communes, cette tumeur fibro-osseuse peut être confondue avec la dysplasie fibreuse (lésion osseuse bénigne plus fréquente) et entraîner un traitement inadapté, à l’origine d’une récidive tumorale osseuse de malignité plus élevée. Nous présentons le cas d’un ostéosarcome central de faible malignité du tibia droit, initialement traité comme une dysplasie fibreuse par curetage et greffe osseuse. Trois ans plus tard, la tumeur a récidivé avec un envahissement plus important des parties molles et de l’os, mais sans dissémination métastatique. Le patient a été traité par une amputation au-dessus du genou. Il est resté asymptomatique au cours des deux dernières années. [Copyright &y& Elsevier]

Abstract: Kimura''s disease is a rare, chronic inflammatory disorder, presenting usually as head and neck swellings and regional cervical lymphadenopathy. The disease is more often described from oriental literature but the osseous manifestations and involvement of extremity are rare and unidentified in literature. We present an unusual case of long bone periosteal reaction in a patient of Kimura''s disease of extremity. This potentially innocuous disorder must be kept in mind as a radiological differential of periosteal reaction. [Copyright &y& Elsevier]

Résumé: La maladie de Kimura est une affection chronique inflammatoire rare qui se traduit habituellement par des masses sous-cutanées à la tête et au cou, accompagnées d’adénopathies cervicales. La plupart des cas décrits à ce jour ont été observés en Asie. L’atteinte des membres et les lésions osseuses sont rares. Nous décrivons une observation inhabituelle de maladie de Kimura responsable d’une réaction périostée le long du fémur gauche. Cette maladie bénigne doit faire partie des diagnostics évoqués devant une réaction périostée radiologique. [Copyright &y& Elsevier]

• Hybridization drug design strategies with rationale to obtain multi target directed ligands (MTDLs) as anti-Alzheimer drugs. • The review covers SAR studies for further development of coumarin-hybrids as therapeutic agents for the Alzheimer's disease (AD). • It provides an overview of research work carried out on di and tri-hybridized coumarin conjugates during 2010–2020. • Chemical structure and biochemical targets of naturally occurring coumarin derivatives with anti-AD properties. • Patents granted to coumarin derivatives for AD treatment. Alzheimer's disease (AD) is a major progressive and perplexing cortical degenerative disease of the brain in the elderly. It contributes to a significant socioeconomic burden on patients, families, and care providers in comparison to cancer, cardiovascular diseases, and stroke in general. Recently, a hybridized approach based on multi-target directed ligands (MTDLs) has received considerable attention to develop therapeutic agents for AD which act at multiple targets. Approximately 20% of the drugs approved in the past couple of years were developed using the same strategy and thus it seems to be the right approach to develop AD therapy. The comprehensive and updated review on coumarin hybrids as MTDLs in AD therapy is compiled using several electronic databases such as Scopus, Google Scholar, SciFinder, Mendeley, and PubMed. The research studies published on coumarin hybrids in the last decade (2010- 2020) have been covered in this review article. This updated review highlights the importance of coupling (hybridization) coumarin scaffold with other bioactive pharmacophores to develop MTDLs for AD therapy. It also covers the patents granted to coumarin derivatives for AD treatment, natural products containing coumarin scaffold with anti-Alzheimer spectrum, the rationale for coupling pharmacophore fragments, detailed structure activity relationship (SAR), and molecular docking studies. The most potent and promising hybrid compounds have also been identified for further development of AD drugs. Authors are of the opinion that hybridization strategy would soon yield drug candidates for the treatment of AD. [ABSTRACT FROM AUTHOR]

Abstract: Desmoplastic fibroma of bone is an extremely rare locally aggressive primary bone tumour. Diagnosis is tricky and treatment experience limited with tumor surgeons. We studied three rare cases of desmoplastic fibroma arising primarily in bone at unusual sites. Diagnosis was established by radio-histopathologic correlation. Patients were operated with various modalities. Results were evaluated over long term follow-up (6–9years). The disease was eradicated in all the three cases and no recurrence was seen over long term follow-up. Functional outcome was good and no complications were encountered. Wide resection of the tumor is favoured as the recurrence rates after surgical treatment are high. [Copyright &y& Elsevier]

Résumé: Le fibrome desmoplastique de l’os est une tumeur osseuse primaire, extrêmement rare et agressive localement. Le diagnostic en est difficile et l’expérience thérapeutique limitée pour les chirurgiens spécialistes dans l’excision des tumeurs. Nous avons étudié trois cas rares de fibromes desmoplastiques survenant au niveau de l’os à des localisations inhabituelles. Le diagnostic a été établi grâce à la radiographie et à l’histopathologie. Les patients ont subi une intervention chirurgicale selon diverses modalités. Les résultats ont été évalués sur une longue période de suivi (six à neuf ans). La pathologie a été éradiquée dans les trois cas et aucune récidive n’a été observée pendant la longue période de suivi. L’évolution fonctionnelle a été bonne et aucune complication n’a été observée. Une résection large de la tumeur est préconisée, car sinon, le taux de récidive après la chirurgie est élevé. [Copyright &y& Elsevier]

The different extracts of Apium graveolens Linn. (Apiaceae) and Croton oblongifolius Roxb. (Euphorbiaceae) were tested for their hepatoprotective activity against CCl4 induced hepatotoxicity in albino rats. The degree of protection was measured by using biochemical parameters like serum transaminases (SGOT and SGPT), alkaline phosphatase, total protein and albumin. The methanolic extracts showed the most significant hepatoprotective activity comparable with standard drug silymarin. Other extracts namely petroleum ether and acetone also exhibited a potent activity. [Copyright &y& Elsevier]

Low grade central osteosarcoma is a rare primary bone tumor. This fibro-osseous lesion shares some radiological and histopathological resemblance with fibrous dysplasia, which is a more common entity. Thus it may be mistaken as fibrous dysplasia and may receive inadequate treatment resulting in a more malignant recurrent bone tumor. We present a case of low grade central osteosarcoma of the right tibia, which was initially treated as fibrous dysplasia with curettage and bone grafting. Three years later the tumor recurred with greater soft tissue and bony involvement but without metastasis. The patient was treated with above knee amputation and has been asymptomatic for the last two years. [ABSTRACT FROM AUTHOR]

Abstract: Spinal tuberculosis constitutes 50% of all musculoskeletal tuberculosis. However, literature regarding congenital spinal tuberculosis is very scanty. Congenital spinal tuberculosis was diagnosed in a two-month-old child on the basis of age at presentation (gibbus since three weeks of age), hepatomegaly, raised ESR, radiological destruction of D10–D11 vertebrae, asymptomatic maternal endometrial tuberculosis and tuberculous histopathology from CT guided biopsy specimen from D10 vertebra. Both child and mother were treated by antitubercular treatment. Child improved symptomatically, gibbus became less prominent and ESR became normal at the end of one year of treatment. Patient had no recurrence during last two years of follow-up. This is the first case of congenital tuberculosis of spine with a documented source of infection from asymptomatic maternal endometrial tuberculosis. CT guided core biopsy from vertebra/aspiration from the paravertebral abscess help in early diagnosis and treatment to reduce neurological morbidity and mortality. Endometrial biopsy help in establishing the diagnosis of congenital tuberculosis and adequate antitubercular treatment in such cases may provide protection to fetus in subsequent pregnancy. [Copyright &y& Elsevier]

Résumé: La tuberculose vertébrale représente la moitié des cas de tuberculose de l’appareil locomoteur. Toutefois, les publications sur la tuberculose vertébrale congénitale sont très rares. Une tuberculose vertébrale congénitale a été diagnostiquée chez un enfant de deux mois en se basant sur l’âge à la présentation d’une bosse (depuis l’âge de trois semaines), la présence d’une hépatomégalie, une vitesse de sédimentation (VS) élevée, l’observation radiographique de la destruction des vertèbres D10–D11, une tuberculose de l’endomètre asymptomatique chez la mère et des résultats anatomopathologiques en faveur de la tuberculose sur les échantillons prélevés par une biopsie scanoguidée au niveau de la vertèbre D10. L’enfant et la mère ont été traités avec un traitement antituberculeux. Les symptômes de l’enfant se sont améliorés, la bosse est devenue moins saillante et la VS s’est normalisée après un an de traitement. Il n’y a eu aucune récidive pendant la période de suivi de deux ans. Il s’agit du premier cas de tuberculose vertébrale congénitale avec comme source infectieuse documentée une tuberculose de l’endomètre asymptomatique maternelle. Le cylindre osseux prélevé par biopsie scanoguidée et l’aspiration de l’abcès paravertébral aident à poser un diagnostic précoce et à traiter rapidement pour réduire la morbidité et la mortalité neurologiques. La biopsie de l’endomètre aide à établir le diagnostic de tuberculose congénitale et l’institution d’un traitement antituberculeux adéquat assure la protection du fœtus pendant les grossesses ultérieures. [Copyright &y& Elsevier]