01236nas a2200157 4500008004100000245007900041210006900120260000800189490000700197520067300204100001800877700002600895700002000921700002700941856011000968 2019 eng d00aSynthesis of hexaphenylbenzene-based template assembled synthetic proteins0 aSynthesis of hexaphenylbenzenebased template assembled synthetic cAUG0 v603 a

Template-assembled synthetic proteins (TASPs) synthesized from rigid templates have attracted attention due to their interesting structural architectures and potential biomedical applications. Herein, we report the design, synthesis and characterizations of TASPs based on hexaphenylbenzene template (HPB) having twelve peptide attachable axial-arms in its structure. The peptides were attached to all the axial-arms of the template in a single step using simple solution phase peptide coupling strategy. The reaction conditions were standardized systematically using simple amines from smaller size to larger ones. (C) 2019 Elsevier Ltd. All rights reserved.

1 aMadhu, Suresh1 aMadica, Krishnaprasad1 aGonnade, Rajesh1 aSanjayan, Gangadhar, J uhttp://library.ncl.res.in/content/synthesis-hexaphenylbenzene-based-template-assembled-synthetic-proteins02004nas a2200253 4500008004100000022001400041245007700055210006900132260000900201300001400210490000700224520117700231100002201408700002701430700002701457700002201484700002201506700002401528700002401552700002101576700002601597700002001623856010701643 2020 eng d a1144-054600aSynthesis and biological activity of imidazole based 1,4-naphthoquinones0 aSynthesis and biological activity of imidazole based 14naphthoqu cMAY  a6889-69010 v443 a

Design and development of drugs in multi-drug resistant (MDR) infections have been of growing interest. We report the syntheses, and antibacterial and antifungal activities of imidazole-based 1,4-naphthoquinones (I-1 to I-4; 1-alkyl-2-methyl-1H-naphtho[2,3-d]imidazole-4,9-dione (alkyl = methyl to butyl)) and their precursors (B-3; N-(3-chloro-1,-dioxo-1,4-dihydronaphthalen-2-yl)acetamide) and A-1 to A-4; N-(3-(alkylamino)-1,4-dioxo-1,4-dihydronaphthalen-2-yl)acetamide (alkyl = methyl to butyl). Crystal structures of B-3, A-1 to A-3 and I-2 to I-4 were obtained through single crystal X-ray diffraction experiments. Electronic structure and charge distribution have further been characterized with the use of Density Functional Theory. Seven of these derivatives display a broad spectrum of antibacterial activity against few selected bacterial strains (Gram-positive and Gram-negative). As demonstrated MIC values with B-2 and B-3 against bacterial isolates were 8-64 mu g ml(-1) and those against pathogenic yeast, C. albicans, were observed in the range of 128-256 mu g ml(-1). MIC data of these derivatives suggest them to be promising against pathogens.

1 aChoudhari, Dinkar1 aSalunke-Gawali, Sunita1 aChakravarty, Debamitra1 aShaikh, Samir, R.1 aLande, Dipali, N.1 aGejji, Shridhar, P.1 aRao, Pradeep, Kumar1 aSatpute, Surekha1 aPuranik, Vedavati, G.1 aGonnade, Rajesh uhttp://library.ncl.res.in/content/synthesis-and-biological-activity-imidazole-based-14-naphthoquinones01271nas a2200181 4500008004100000022001400041245007600055210006900131260000900200300001400209490000700223520066100230100002700891700002500918700002000943700002300963856010300986 2024 eng d a1463-907600aSolid-state NMR method for characterization of pharmaceutical eutectics0 aSolidstate NMR method for characterization of pharmaceutical eut cJAN  a3800-38030 v263 a

Pharmaceutical eutectics are extremely useful for designing formulations, and currently, there are no techniques other than differential scanning calorimetry (DSC) that can confirm their formation. In this study, we demonstrate that 1H fast magic angle spinning (MAS) solid-state NMR (SSNMR) experiments can confirm the formation of eutectics by detecting their intermolecular hydrogen bonding interactions. 2D 1H-1H double quantum single quantum (DQSQ) correlation SSNMR experiment is demonstrated which can confirm the formation of pharmaceutical eutectics for which there are no techniques other than differential scanning calorimetry (DSC).

1 aHareendran, Chaithanya1 aShaligram, Parth, S.1 aGonnade, Rajesh1 aAjithkumar, T., G. uhttp://library.ncl.res.in/content/solid-state-nmr-method-characterization-pharmaceutical-eutectics