01792nas a2200313   4500008004100000022001400041245012100055210006900176260007100245300001400316490000600330520070200336653001801038653001901056653001401075653001801089653001801107100002301125700001801148700002801166700002501194700001901219700002001238700002701258700002401285700002401309700002101333856012401354       2015                        eng d  a1948-587500aDesign, synthesis, and identification of silicon incorporated oxazolidinone antibiotics with improved brain exposure0 aDesign synthesis and identification of silicon incorporated oxaz  a1155 16TH ST, NW, WASHINGTON, DC 20036 USAbAMER CHEMICAL SOCcNOV  a1105-11100 v63 a<p>Therapeutic options for brain infections caused by pathogens with a reduced sensitivity to drugs are limited. Recent reports on the potential use of linezolid in treating brain infections prompted us to design novel compounds around this scaffold. Herein, we describe the design and synthesis of various oxazolidinone antibiotics with the incorporation of silicon. Our findings in preclinical species suggest that silicon incorporation is highly useful in improving brain exposures. Interestingly, three compounds from this series demonstrated up to a 30-fold higher brain/plasma ratio when compared to linezolid thereby indicating their therapeutic potential in brain associated disorders.</p>10aAntibacterial10abrain exposure10alinezolid10aoxazolidinone10asila analogue1 aSeetharamsingh, B.1 aRamesh, Remya1 aDange, Santoshkumar, S.1 aKhairnar, Pankaj, V.1 aSinghal, Smita1 aUpadhyay, Dilip1 aVeeraraghavan, Sridhar1 aViswanadha, Srikant1 aVakkalanka, Swaroop1 aReddy, Srinivasa  uhttps://library.ncl.res.in/content/design-synthesis-and-identification-silicon-incorporated-oxazolidinone-antibiotics-001069nas a2200169   4500008004100000022001400041245008500055210006900140260007100209300001200280490000700292520041500299100002300714700002500737700002100762856011600783       2016                        eng d  a0022-326300aFirst total synthesis of gliomasolide C and formal total synthesis of sch-7256740 aFirst total synthesis of gliomasolide C and formal total synthes  a1155 16TH ST, NW, WASHINGTON, DC 20036 USAbAMER CHEMICAL SOCcJAN  a290-2960 v813 a<p>Syntheses of two 14-membered macrolides Sch-725674 and Gliomasolide C are described here. The first total synthesis of Gliomasolide C, the short synthesis of Sch-725674, and regios elective Wacker oxidation of internal olefin are the highlights of this disclosure. In addition, a key macrocyde with orthogonal functionalities was designed and synthesized on a gram scale for the generation of analogues.</p>1 aSeetharamsingh, B.1 aKhairnar, Pankaj, V.1 aReddy, Srinivasa  uhttps://library.ncl.res.in/content/first-total-synthesis-gliomasolide-c-and-formal-total-synthesis-sch-725674-001669nas a2200217   4500008004100000245012500041210006900166260000800235300001400243490000700257520088500264100002101149700002301170700002201193700002101215700002501236700001901261700002101280700002001301856013001321       2017                        eng d00aIdentification and synthesis of mycalol analogues with improved potency against anaplastic thyroid carcinonia cell lines0 aIdentification and synthesis of mycalol analogues with improved   cAPR  a1125-11330 v803 aThe marine metabolite mycalol (1) has a specific inhibitory activity on cells of anaplastic thyroid carcinoma (ATC), a very aggressive and rare cancer that does not have effective conventional therapy. In this study, we describe six new related analogues (2-7) that differ in the length of the terminal alkyl residue and the presence of acetate or 3S-hydroxybutyrate (3S)-3HB as a substituent at C-19. Despite the structural' analogies, some of the new members were significantly more-cytotokic than 1 on cell lines,derivecl from human ATC. Structures inclusive of the 2'R,3R,4S,7R,8S,19R absolute configuration were asigned to 2-7 on the basis of detailed spectroscopic analysis, synthesis of different isomers, and application of ECD and Mosher's methods. This work led to the identification of mycal61-578 (3) as the most potent analogue, with an IC50 of 2.3 mu M on FRO cells:1 aCutignano, Adele1 aSeetharamsingh, B.1 aD'Angelo, Daniela1 aNuzzo, Genoveffa1 aKhairnar, Pankaj, V.1 aFusco, Alfredo1 aReddy, Srinivasa1 aFontana, Angelo  uhttps://library.ncl.res.in/content/identification-and-synthesis-mycalol-analogues-improved-potency-against-anaplastic-thyroid