- The synthesis and biological evaluation of nucleobases/tetrazole hybrid compounds: A new class of phosphodiesterase type 3 (PDE3) inhibitors
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Spired by the chemical structure of Cilostazol, a selective phosphodiesterase 3A (PDE3A) inhibitor, several novel hybrid compounds of nucleobases (uracil, 6-azauracil, 2-thiuracil, adenine, guanine, theophylline and theobromine) and tetrazole were designe
- Shekouhy, Mohsen,Karimian, Somaye,Moaddeli, Ali,Faghih, Zeinab,Delshad, Yousef,Khalafi-Nezhad, Ali
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- ANALOGUES OF PENTAMIDINE AND USES THEREFOR
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The present disclosure provides a group of aromatic (e.g., pyridinyl, pyrimidinyl, pyrazinyl, or phenyl) diamidine analogs and pharmaceutically acceptable salts that are useful for treating a proliferative disease. The proliferative disease may include solid cancer or blood cancer. Compositions, methods of synthesizing the same and methods for treating various cancer using the analogs are disclosed herein. The present disclosure also provides pharmaceutical formulations comprising at least one of the compounds with a pharmaceutically acceptable carrier, diluent or excipient therefor.
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Paragraph 0192
(2020/07/14)
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- gem-Dithioacetylated indole derivatives as novel antileishmanial agents
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In this communication we report a serendipitously discovered hybrid molecule 1, combining fragment of 3 (an in vivo active antileishmanial molecule) with H2S donor moiety (known for bimodal behavior of cytoprotection and apoptosis), as antileis
- Porwal, Sharad,Gupta, Suman,Chauhan, Prem M.S.
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p. 4643 - 4646
(2017/09/29)
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- Synthesis and antiprotozoal properties of pentamidine congeners bearing the benzofuran motif
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Forty-eight cationically substituted pentamidine congeners possessing benzofuran rings were synthesized by a copper mediated heteroannulation of substituted o-iodophenols with phenyl acetylenes. Activities of compounds 1-48 against Trypanosoma brucei rhod
- Bakunov, Stanislav A.,Bakunova, Svetlana M.,Bridges, Arlene S.,Wenzler, Tanja,Barszcz, Todd,Werbovetz, Karl A.,Brun, Reto,Tidwell, Richard R.
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p. 5763 - 5767
(2010/02/28)
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- Design and synthesis of amidino-tyrosine derivatives as non-peptide fibrinogen receptor antagonists
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The design, synthesis and antiaggregation activity of amidino-tyrosine derivatives based on Arg-Gly-Asp (RGD) tripepride sequence as non-peptide fibrinogen receptor antagonists is described. Optimization of the spacer and the substituent at the C-terminal is reported.
- Xu, Tian-Lin,Jiang, Xun-Tian,Hua, Wei-Yi,Ni, Pei-Zhou,Pei, Yong-Mei
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p. 1933 - 1936
(2007/10/03)
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- 2,3-diketopiperazine derivatives or their salts
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The present invention relates to a 2,3-diketopiperazine derivative or a salt thereof, which has inhibitory effect on platelet aggregation because of glycoprotein IIb/IIIa receptor antagonism and hence is useful as a prophylactic and therapeutic agent for diseases associated with platelet aggregation. General formula: STR1 wherein R1 represents a protected or unprotected amidino group; R2 represents a hydrogen atom or a carboxyl-protecting group; A represents a substituted or unsubstituted lower alkylene group; B represents --O--, --CONH--, --NHCO--or --SO2 NH--; Y represents a substituted or unsubstituted lower alkylene group; and the broken line represents a single bond or a double bond.
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