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Kumar M Rawat P Khan MF Rawat AK Srivastava AK Maurya R 《Bioorganic & medicinal chemistry letters》2011,21(8):2232-2237
16-Dehydropregnenolone undergoes a smooth annulation with propan-1-amine and aromatic aldehydes. Several amine derivatives of 16- dehydropregnenolone were synthesized and evaluated as inhibitors of DPP-IV. The structures of compounds were confirmed by 1H, 13C, NMR and mass spectral analysis. Among 17 compounds evaluated only five compounds 1, 9, 13, 15 and 16 demonstrated significant inhibition of DPP. This study suggest that introduction of appropriate substituents in the 16-dehydropregnenolone plays an important role in DPP-IV inhibitory activity. 相似文献
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Stephanie Cronje 《Inorganica chimica acta》2005,358(5):1581-1594
Anionic Fischer-type aminocarbene complexes, [(CO)5MC(NMe2)CH2]Li (M = Cr or W) react with Ph2PCl and [Me2(MeS)S][BF4] - a source of SMe+ - to afford acyclic complexes (CO)5MC(NMe2)CH2X (X = PPh2, SMe2) and (CO)5MC(NMe2)CHX2 X = SMe), the chelates and , and the bridged compounds (CO)5MC(NMe2)CH2XM(CO)5 (X = PPh2, SMe). Cyclisation occurs much faster for Cr than for W. Crystal structures illustrate the bonding behaviour in the new complexes and especially characterise carbene-phosphine and carbene-thioether four-membered chelates for the first time. The sulfur-donor in the tetracarbonyl complexes , and shows an exceptionally weak trans influence. 相似文献
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A series of novel 7-aminoalkyl substituted pyrazolo[1,5-a]pyrimidine derivatives were synthesized and tested for inhibition of cathepsin K. The synthetic methodology comprises cyclization of 5-aminopyrazoles with N-Boc-α-amino acid-derived ynones followed by transformation of the ester and the Boc-amino functions. It allows for easy diversification of the pyrazolo[1,5-a]pyrimidine scaffold at various positions. Molecular docking studies with pyrazolo[1,5-a]pyrimidine derivatives were also performed to elucidate the binding mode in the active site of cathepsin K. The synthesized compounds exhibited moderate inhibition activity (Ki ≥ 77 μM). 相似文献
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Di-O-isopropylidene- and O-methanesulfonyl-protected 1-C-(6-chloro-1,2,4-triazolo[4,3-b]pyridazin-3-yl)pentitols were prepared in three to four steps from D-galactose, D-glucose, D-mannose, and 2,3:5,6-di-O-isopropylidene-alpha-D-mannofuranose. Acid-catalysed treatment of (1S)- and (1R)-1-C-(6-chloro-1,2,4-triazolo[4,3-b]-pyridazin-3-yl)-2,3:4,5-di-O-isopropylidene-1-O-methanesulfonyl-D-arabinitols in refluxing 1,2-dimethoxyethane furnished 3-(alpha- and beta-D-arabinofuranosyl)-6-chloro-1,2,4-triazolo[4,3-b]pyridazine, respectively. Several structures, including the structure of the 3-(beta-D-arabinofuranosyl)-6-chloro-1,2,4-triazolo[4,3-b]pyridazine, were also determined by single-crystal X-ray diffraction analysis. 相似文献
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