Synthetic and mass spectral fragmentation studies on trisubstituted 2H-pyran- 2-ones and comparative EIMS behaviour of biologically active 3,5- disubstituted pyrazoles and isoxazoles

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Apogeotropic posterior semicircular canal BPPV—A case series from South Rajasthan

Apogeotropic variant of posterior semicircular canal benign paroxysmal positional vertigo (apo-PSC-BPPV) is a rare peripheral vestibular disorder, characterized by paroxysms of positionally triggered dizzy spells associated with non-positional disequilibrium. It is diagnosed by observing characteristic diagnostic oculomotor responses (torsional downbeating positional nystagmus) during positional testing (Dix-Hallpike and enhanced straight head hanging tests), in conjunction with a response to physical therapy. Much rarer anterior semicircular canal benign paroxysmal positional vertigo (ASC-BPPV) elicits identical oculomotor responses during positional testing. Propter hoc, response to physical therapy at short-term follow-up is crucial in distinguishing the apo-PSC-BPPV from ASC-BPPV. We are presenting a case series of seven patients of apo-PSC-BPPV (of which three were bilaterally affected), who attended our otoneurology center, between February 1, 2023, and July 31, 2023. Demographic profile, clinical course, and physical therapy with responses at short-term follow-up at 1 hour and after 24 hours are discussed

A rare case of Charlin's syndrome

Charlin's syndrome is an extremely rare condition characterized by pain in the nasal and paranasal areas, which is precipitated by touching the lateral aspect of the ipsilateral nostril. We are presenting one such case of a 42-year-old man who was admitted to Dr. Chaudhary Hospital and Medical Research Centre

Chemical transformations on 6-aryl-3-cyano-4-methylthio-pyran-2(<i>H</i>)-ones: Synthetic and structural studies on novel N-phenylpyrazoles and <i>N-</i>phenylpyrazolylcoumarins

360-367Seven 6-aryl-3-cyano-4-methylthiopyran-2(H)-ones 1-7 have been prepared and used for the efficient synthesis of twelve 1,3-diaryl-5-cyanomethylpyrazoles 8-19, one 3-cyanomethyl-5-(3,4-methylenedioxyphenyl)pyrazole 22 and one 5-cyanomethyl-3-phenylisoxazole 23. Further, two 1,3-diaryl -5-cyanomethylpyrazoles 10 and 11 have been used for the preparation of three novel N-phenylpyrazolylcoumarins 24-26. Structures of 3-cyano-6-(3,4-methylenedioxyphenyl)-4-methylthiopyran-2(H)-one 7, 3-cyanomethyl-5-(3,4-methylenedioxyphenyl)pyrazole 22 and 5-cyanomethyl-3-phenylisoxazole 23 have been confirmed by their X-ray crystallographic studies

Synthesis of novel heterocyclic compounds: Routes to pyrazolyl 1,2,3-triazoles and their biological activity evaluation

1950-1957A series of 5-aryl-3-cyanomethylpyrazoles have been synthesized by refluxing 6-aryl-3-cyano-4-methylthio-2H-pyran-2-ones with hydrazine. The active methylene moiety of these pyrazoles has further been exploited to build 1,4-disubstituted 5-amino-1 ,2,3-triazolcs via their base-catalyzed condensation with 3/4-nitrophenylazides. All these compounds have been characterized by detailed spectral analysis and chemical transformations to confirm their structures unambiguously, which were proposed inconclusively five decades ago. Further, these pyrazolyltriazoles have been tested as antiinvasive agents against solid tumors and as antimycobacterial agents. &nbsp

Synthesis of novel heterocyclic compounds: routes to pyrazolyl 1,2,3-triazoles and their biological activity evaluation

A series of 5-aryl-3-cyanomethylpyrazoles have been synthesized by refluxing 6-aryl-3-cyano-4-methylthio-2H-pyran-2-ones with hydrazine. The active methylene moiety of these pyrazoles has further been exploited to build 1,4-disubstituted 5-amino-1,2,3-triazoles via their base-catalyzed condensation with 3/4-nitrophenyl azides. All these compounds have been characterized by detailed spectral analysis and chemical transformations to confirm their structures unambiguously, which were proposed inconclusively five decades ago. Further, these pyrazolyltriazoles have been tested as antiinvasive agents against solid tumors and as antimycobacterial agents

Synthesis, characterization and in vitro anti-invasive activity screening of polyphenolic and heterocyclic compounds

Invasion is the hallmark of malignant tumors, and is responsible for the bad prognosis of the untreated cancer patients. The search for anti-invasive treatments led us to screen compounds of different classes for their effect in an assay for invasion. Thirty-nine new compounds synthesized in the present study along with 56 already reported compounds belonging mainly to the classes of lactones, pyrazoles, isoxazoles, coumarins, desoxybenzoins, aromatic ketones, chalcones, chromans, isoflavanones have been tested against organotypic confronting cultures of invasive human MCF-7/6 mammary carcinoma cells with embryonic chick heart fragments in vitro. Three of them (a pyrazole derivative, an isoxazolylcoumarin and a prenylated desoxybenzoin) inhibited invasion at concentrations as low as 1 muM; instead of occupying and replacing the heart tissue within 8 days, the MCF-7/6 cells grew around the heart fragments and left it intact, when treated with these compounds. At the anti-invasive concentration of 1 muM, the three compounds did not affect the growth of the MCF-7/6 cells, as shown in the sulforhodamine B assay. Aggregate formation on agar was not stimulated by any of the three anti-invasive compounds, making an effect on the E-cadherin/catenin complex improbable. This is an invasion suppressor that can be activated in MCF-7/6 cells by a number of other molecules. Our data indicate that some polyphenolic and heterocyclic compounds are anti-invasive without being cytotoxic for the cancer cells. (C) 2003 Elsevier Science Ltd. All rights reserved