NOPR Community:

Iodine promoted simple synthesis of benzimidazole acyclonucleosides

Sun, 01 Dec 2013 00:00:00 GMT

Title: Iodine promoted simple synthesis of benzimidazole acyclonucleosides Authors: Yadav, Tej Bahadur; Singh, Virendra Abstract: A novel one-pot ecofriendly synthesis of 2,5,6-trisubstituted-1H-benzimidazole nucleoside derivatives have been accomplished stepwise. i.e. substituted o-phenylenediamine and aldoses using iodine as an oxidant or promoter in acetic solution at room temperature. A practical method has been developed for conversion of unprotected and unmodified aldoses to aldo-benzimidazoles. Page(s): 1536-1539

Synthesis, antituberculosis and antimicrobial study of some new aminoacridine linked pyrazoles

Sun, 01 Dec 2013 00:00:00 GMT

Title: Synthesis, antituberculosis and antimicrobial study of some new aminoacridine linked pyrazoles Authors: Kawle, P R; Deohate, P P; Berad, B N; Srivastava, K K; Sharma, P Abstract: Synthesis of heterocycles containing pyrazole linked to acridine chromophore has been studied and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis. Acridin-9-yl-(5-methyl-2-aryl)-2,4-dihydropyrazol-3-ylidene)-amine and [5-(acridin-9-yl-imino)-3-methyl-4,5-dihydro-pyrazol-1-yl]-pyridin-4-yl/aryl-methanone have been prepared by cyclocondensation reaction of N-acridin-9-yl-3-oxo-butyramide with hydrazine hydrate in ethanol at room temperature. The title compounds have been screened for their antimicrobial potency against some selected microorganisms to set-up structure activity relationship. All the compounds are found to have potent antimicrobial response. The structural elucidation of synthesised compounds has been performed by IR, ¹H NMR and mass spectroscopic data besides elemental analysis. The products are obtained by a simple methodology and in good yields. Page(s): 1531-1535

A new friedelane triterpene ester from Pouzolzia indica

Sun, 01 Dec 2013 00:00:00 GMT

Title: A new friedelane triterpene ester from Pouzolzia indica Authors: Sarma, Indrajit Sil; Dinda, Biswanath Abstract: A new friedelane triterpene ester, 7β-hydroxy-3-oxo-28-dodecyl friedelan-28-oate 1 along with known compounds, friedelin 2, myricyl palmitate 3 and myricylalcohol 4 have been isolated from the dried whole plant of Pouzolzia indica. The structure of the new compound 1 has been established by detailed spectroscopic including 2D NMR experiments and chemical studies. Page(s): 1527-1530

In-silico, in-vitro antibacterial activity and toxicity profile of new quinoline derivatives

Sun, 01 Dec 2013 00:00:00 GMT

Title: In-silico, in-vitro antibacterial activity and toxicity profile of new quinoline derivatives Authors: Sambavekar, P P; Aitawade, M M; Patil, D R; Kolekar, G B; Deshmukh, M B; Anbhule, P V Abstract: The new substituted quinoline derivatives have been synthesized and characterized by various spectroscopic techniques. A prediction of activity spectra for substances (PASS) of synthesized quinoline compounds showed their probabilities of being active for the antibacterial activities. Therefore, all the newly synthesized compounds have been evaluated for their in-vitro antibacterial activity against Staphylococcus aureus and Escherichia coli. It has been observed that 6-chloro-4-phenylquinoline-2,3-dicarboxylic acid 4a selectively active against Gram (-)ve E. coli and 8-chloro-10-phenyl-2,3-dihydropyridazino[4,5-b]quinoline-1,4-dione 5a showed selectivity against Gram (+)ve S. aureus. PASS prediction study indicates that the compound 5a as a potential candidate with a Pa 0.671, maximum from the series. According to the results obtained from brine shrimp (Artemia salina) lethality bioassay the compounds prove to be non toxic. The computer aided results are in good agreement with experimental results. Page(s): 1521-1526