Abstract：
:Novel, quinolone-fluoroquinolone conjugates 10a-f, 11a-f, 13a-f and 14a-f with amino acid linkers were synthesized in good yields utilizing benzotriazole chemistry. Antibacterial bioassay showed the synthesized bis-conjugates exhibit anti-bacterial properties comparable with the parent drugs.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Panda SS,Liaqat S,Girgis AS,Samir A,Hall CD,Katritzky ARdoi
10.1016/j.bmcl.2015.07.077subject
Has Abstractpub_date
2015-09-15 00:00:00pages
3816-21issue
18eissn
0960-894Xissn
1464-3405pii
S0960-894X(15)00781-7journal_volume
25pub_type
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journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/j.bmcl.2012.12.086
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journal_title：Bioorganic & medicinal chemistry letters
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journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/s0960-894x(99)00604-6
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abstract：:Human kallikrein 1 (KLK1) is the most extensively studied member of this family and plays a major role in inflammation processes. From Ugi multicomponent reactions, isomannide-based peptidomimetic 10 and 13 where synthesized and showed low micromolar values of IC50 for KLK1 The most active compound (10) presented comp...
journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/j.bmcl.2016.11.051
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abstract：:Selective inhibitors of protein tyrosine phosphatases (PTPases) are of great interest as therapeutic agents and research tools. Several phenylalanine derivatives (1, 2) designed as phosphotyrosine mimetics or irreversible active site inhibitors were successfully synthesized, then incorporated into a combinatorial libr...
journal_title：Bioorganic & medicinal chemistry letters
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abstract：:The peptidomimetic, LLP2A, is a specific, high-affinity ligand for α4β1 integrin receptors. Previously, several PEGylated LLP2A conjugates were evaluated in vivo as imaging agents for the detection of lymphoma, leukemia, multiple myeloma and melanoma tumours via NIR-fluorescence, 111In-SPECT, and 64Cu- and 68Ga-PET im...
journal_title：Bioorganic & medicinal chemistry letters
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abstract：:Considering the therapeutic potential of fatty acid amides, the present study aimed to evaluate their in vitro activity against Toxocara canis larvae and their cytotoxicity for the first time. Linoleylpyrrolidilamide was the most potent, with a minimal larvicidal concentration (MLC) of 0.05 mg/mL and 27% cytotoxicity ...
journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/j.bmcl.2016.01.002
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journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/j.bmcl.2015.02.004
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journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/j.bmcl.2016.11.077
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abstract：:The use of cell-membrane translocating sequences for intracellular delivery of peptides can be a powerful approach to validate drug discovery targets in cellular settings. To accomplish this, a protocol has been implemented to couple the antennapedia third helix (residues 43-58) to a potent antagonist of the p53/hdm2 ...
journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/s0960-894x(01)00394-8
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abstract：:Maleimides are often used for biomolecular conjugation with thiols. An underappreciated aspect of the imido group in a maleimide conjugate is its susceptibility to spontaneous hydrolysis, resulting in undesirable heterogeneity. Here, a chromophoric maleimide is used to demonstrate that both molybdate and chromate cata...
journal_title：Bioorganic & medicinal chemistry letters
pub_type： 杂志文章
doi：10.1016/j.bmcl.2007.09.002
更新日期：2007-11-15 00:00:00
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journal_title：Bioorganic & medicinal chemistry letters
pub_type： 杂志文章
doi：10.1016/j.bmcl.2015.12.059
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abstract：:Several derivatives of hadacidin have been developed and evaluated for activity against adenylosuccinate synthetase. ...
journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/j.bmcl.2010.10.088
更新日期：2011-01-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/j.bmcl.2009.07.094
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journal_title：Bioorganic & medicinal chemistry letters
pub_type： 杂志文章
doi：10.1016/j.bmcl.2013.08.103
更新日期：2013-11-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/j.bmcl.2004.09.023
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journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/j.bmcl.2012.10.134
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journal_title：Bioorganic & medicinal chemistry letters
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journal_title：Bioorganic & medicinal chemistry letters
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journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/s0960-894x(03)00586-9
更新日期：2003-09-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry letters
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journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/j.bmcl.2005.06.002
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journal_title：Bioorganic & medicinal chemistry letters
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journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/j.bmcl.2004.04.069
更新日期：2004-07-05 00:00:00
abstract：:A series of novel spiroketal-based NK(1) antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration. ...
journal_title：Bioorganic & medicinal chemistry letters
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doi：10.1016/s0960-894x(02)00506-1
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journal_title：Bioorganic & medicinal chemistry letters
pub_type： 杂志文章
doi：10.1016/j.bmcl.2013.02.068
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abstract：:A new route to 17 beta-substituted-6-azaandrost-4-en-3-ones, potent dual inhibitors of type 1 and 2 steroidal 5 alpha-reductase, is described. ...
journal_title：Bioorganic & medicinal chemistry letters
pub_type： 杂志文章
doi：10.1016/s0960-894x(98)00611-8
更新日期：1998-12-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry letters
pub_type： 杂志文章
doi：10.1016/j.bmcl.2015.05.041
更新日期：2015-08-01 00:00:00
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journal_title：Bioorganic & medicinal chemistry letters
pub_type： 杂志文章
doi：10.1016/j.bmcl.2012.10.069
更新日期：2013-01-01 00:00:00
