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3,7-Diarylpyrazolo[1,5-α]pyrimidines의 개선된 One-pot Regioselective 합성과 CB1R 활성
홍용덕 ( Yong Deog Hong ),변경희 ( Kyoung Hee Byoun ),박미영 ( Miyoung Park ),박준성 ( Jun Seong Park ),신송석 ( Song Seok Shin ) 대한화장품학회 2015 대한화장품학회지 Vol.41 No.2
본 연구는 3,7-diarylpyrazolo [1,5-α]pyrimidines의 효과적인 one-pot regioselective 합성을 보여준다. 더욱이, 그 유도체는 뛰어난 CB1R 저해 활성을 나타냈다. 3,7-position에 diaryl group이 치환된 pyrazolo [1,5-α]pyrimidine은 CB1R 후보로서 가능성 있는 pharmacophore이다. This study demonstrates an effective one-pot regioselective synthesis of 3,7-diarylpyrazolo [1,5-α]pyrimidines. Moreover, the derivatives obtained were effective CB1R antagonists. These pyrazolo [1,5-α]pyrimidines with diaryl groups at the 3,7-positions are potential pharmacophores for CB1R candidates.
Synthesis of Thiazolo[4,5-d]pyrimidine Derivatives as Potential Antimicrobial Agents
Nargues S. Habib,Raafat Soliman,Alaa A. El-Tombary,Soad A. El-Hawash,Omaima G. Shaaban 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.12
In this study, we report the synthesis and antimicrobial evaluation of several new thiazolo[4,5- d]pyrimidine derivatives, namely 7-substituted amino-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine- 2(3H)-thiones 4a-e, 8, 13, 15, ethyl 2-cyano-2-(7-substituted-5-methyl-3-phenylthiazolo [4,5-d]-pyrimidin-2(3H)-ylidene)acetates 5a-b, 2-(7-substituted-5-methyl-3-phenylthiazolo[4,5- d]pyrimidin-2(3H)-ylidene)malononitriles 6a-b, 5-methyl-7-morpholino-3-phenylthiazolo[4,5-d] pyrimidine-2(3H)-one 7, and 7-[4-(1-substituted-5-phenyl-4,5-dihydro-1H-pyrazolin-3-yl)anilino]-5- methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 10-12. Some of the tested compounds were more active against C. albicans than E. coli and P. aeruginosa, and all were inactive against S. aureus.
Synthesis of Thiazolo[4,5-d]pyrimidine Derivatives as Potential Antimicrobial Agents
Habib, Nargues S.,Soliman, Raafat,El-Tombary, Alaa A.,El-Hawash, Soad A.,Shaaban, Omaima G. 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.12
In this study, we report the synthesis and antimicrobial evaluation of several new thiazolo[4,5-d]pyrimidine derivatives, namely 7-substituted amino-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 4a-e, 8, 13, 15, ethyl 2-cyano-2-(7-substituted-5-methyl-3-phenylthiazolo [4,5-d]-pyrimidin-2(3H)-ylidene)acetates 5a-b, 2-(7 -substituted-5-methyl-3-phenylthiazolo[4,5-d]pyrimidin-2(3H)-ylidene)malononitriles 6a-b, 5-methyl-7-morpholino-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-one 7, and 7-[4-(1-substituted-5-phenyl-4,5-dihydro-1H-pyrazolin-3-yl)anilino]-5-methyl-3-phenylthiazolo[4,5-d]pyrimidine-2(3H)-thiones 10-12. Some of the tested compounds were more active against C. albicans than E. coli and P. aeruginosa, and all were inactive against S. aureus.
Synthesis of a DNA-Encoded Library of Pyrrolo[2,3-d]pyrimidines
박준형,왕희명,신민현,임현석 대한화학회 2021 Bulletin of the Korean Chemical Society Vol.42 No.4
Developing DNA-encoded libraries of privileged scaffolds, such as pyrrolopyrimidines, is of great interest in drug discovery and chemical biology as a powerful tool to rapidly and inexpensively discover potent drug candidates. However, it is often challenging to construct such DNA-encoded libraries because many reaction conditions are not compatible with DNA. Here, we describe the development of a convenient solid-phase synthetic strategy that overcomes the current limitations and allows the efficient synthesis of a DNA-encoded combinatorial library of structurally diverse tetra-substituted pyrrolo[2,3-d]pyrimidines.
Samia M. Rida,Soad A. M. El-Hawash,Hesham T. Y. Fahmy,Aly A. Hazza,Mostafa M. M. El-Meligy 대한약학회 2006 Archives of Pharmacal Research Vol.29 No.1
A novel series of 1-(1-benzofuran-2-yl-ethylidene)-4-substituted thiosemicarbazides (2a-d) along with some derived ring systems: substituted-2,3-dihydro-thiazoles (3a-c, 4a-f) and thiazolidin- 4-ones (5a-d and 6a-d), were synthesized. In addition, cyanoacetic acid-(1-benzofuran- 2-yl-ethylidene) hydrazide (7) was used to prepare another new series of compounds consisting of substituted pyridin-2(1H)-ones (8a-c); 2-thioxo-2,3-dihydro-thiazoles (9a-d) and 2-thioxo-2,3-dihydro-6H-thiazolo[4,5-d]pyrimidin-7-ones (10a-c, 11a-c). The absolute configuration of compound 5c was determined by X-ray crystallography. The compounds prepared were evaluated for their in vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds 5c and 9a produced a significant reduction ㅐㄹ the viral cytopathic effect (93.19% and 59.55%) at concentrations >2.0×10-4 M and 2.5×10-5 M respectively. Compound 9a was confirmed to have moderate anti-HIV activity. Compounds 2a, 2d, and 5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.
Rida, Samia M.,EI-Hawash, Soad A.M.,Fahmy, Hesham T.Y.,Hazza, Aly A.,EI-Meligy, Mostafa M.M. The Pharmaceutical Society of Korea 2006 Archives of Pharmacal Research Vol.29 No.1
A novel series of 1-(1-benzofuran-2-yl-ethylidene)-4-substituted thiosemicarbazides (2a-d) along with some derived ring systems: substituted-2,3-dihydro-thiazoles(3a-c, 4a-f) and thiazolidin-4-ones(5a-d and 6a-d), were synthesized. In addition, cyanoacetic acid-(1-benzofuran-2-yl-ethylidene) hydrazide(7) was used to prepare another new series of compounds consisting of substituted pyridin-2(1H)-ones(8a-c); 2-thioxo-2,3-dihydro-thiazoles(9a-d) and 2-thioxo-2,3-dihydro-6H-thiazolo[4,5-d]pyrimidin-7-ones (10a-c, 11a-c). The absolute configuration of compound 5c was determined by X-ray crystallography. The compounds prepared were evaluated for their in vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds 5c and 9a produced a significant reduction ㅐ ㄹ the viral cytopathic effect (93.19% and 59.55%) at concentrations $>2.0{\times}10^{-4}\;M\;and\;2.5{\times}10^{-5}\;M$respectively. Compound 9a was confirmed to have moderate anti-HIV activity. Compounds 2a, 2d, and 5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.
Kim, Jack-C.,Dong, Eun-Soo,Park, Jin-Il,Bae, Sang-Duk,Kim, Seon-Hee The Pharmaceutical Society of Korea 1994 Archives of Pharmacal Research Vol.17 No.6
A number of 5-substituted pyrimidine acyclic nucleosides were synthesized and tested for invitor cytotoxicity against four cell lines (j-82 cell, p-388 cell, FM-3A cell and U-938 cell lines). Synthesis of 1-cyanomethyl-5-substituted pyrimidines (1a-e) and 1-(4-cyanobutyl)-5-substituted pyrimidines (2a-e) was acomplished from the series of alkylation reactions ofl 5-substituted uracils with the corresponding chloacetonitrile and 5-chlorovaleronitile in DMSO under $50^{\circ}C$ temperature. These 5-substituted pyrimidine acylic nucleosides (1a-e and 2a-e) exhibited moderate to significant acitivity aginst four cell lines.
Antimicrobial Activity of New 4,6-Disubstituted Pyrimidine, Pyrazoline, and Pyran Derivatives
Mahmoud M. M. Ramiz,Wael A. El-Sayed,Asmaa I. El-Tantawy,Adel A. H. Abdel-Rahman 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.5
A number of new 2,6-didisubstituted pyrimidine, pyrazoline, and pyran derivatives were synthesized starting from their chalcone derivative. The synthesized compounds displayed different degrees of antimicrobial activity against Bscillus subtilis (Gram-positive), Pseudomonas aeruginosa (Gram-negative), and Streptomyces species (Actinomycetes).