- Thiazole-diamides as potent γ-secretase inhibitors
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The thiazole-diamide series (1) has been identified as highly potent γ-secretase inhibitors. Several representative compounds showed IC50 values of 3H]-2a, are d
- Chen, Yuhpyng L.,Cherry, Kevin,Corman, Michael L.,Ebbinghaus, Charles F.,Gamlath, Chandra B.,Liston, Dane,Martin, Barbara-Anne,Oborski, Christine E.,Sahagan, Barbara G.
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p. 5518 - 5522
(2008/03/14)
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- Phenyl thiazolyl urea and carbamate derivatives as new inhibitors of bacterial cell-wall biosynthesis
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Over 50 phenyl thiazolyl urea and carbamate derivatives were synthesized for evaluation as new inhibitors of bacterial cell-wall biosynthesis. Many of them demonstrated good activity against MurA and MurB and gram-positive bacteria including MRSA, VRE and
- Francisco, Gerardo D.,Li, Zhong,Albright, J. Donald,Eudy, Nancy H.,Katz, Alan H.,Petersen, Peter J.,Labthavikul, Pornpen,Singh, Guy,Yang, Youjun,Rasmussen, Beth A.,Lin, Yang-I.,Mansour, Tarek S.
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p. 235 - 238
(2007/10/03)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- H2-antagonists: Synthesis and activity of 2-Amino-5-thiazolyl derivatives
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2-Amino- and 2-guanidinothiazole derivatives having in position 5 a methylthioalkyl side-chain with urea-equivalent moieties were prepared for comparison with H2-antagonists of cimetidine and tiotidine series. Examination of the pharmacological results obtained from experiments on guinea pig atria and in cat gastric fistula, suggests some general observations about the structure-activity relationship of the compounds synthesized. The activity trend of these products is different from that of H2-imidazole antagonists while it is similar to that of the tiotidine series. Unlike the tiotidine similar compounds, the 2-guanidino-5-thiazolyl derivatives are less potent than the corresponding 2-amino-5-thiazolyl products. The activity of the latter ones is reduced in comparison to that of tiotidine or cimetidine.
- Plazzi,Bordi,Silva,Morini,Catellani,Vaona,Impicciatore
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p. 1011 - 1030
(2007/10/02)
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- Process for preparing 2-amino-5-formylthiazole and its hydrobromide salt
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Process for the preparation of 5-formyl-2-aminothiazole hydrobromide and 2-amino-5-formylthiazole which comprises reacting bromomalonaldehyde and thiourea in the substantial absence of acid or base to form the 5-formyl-2-aminothiazole hydrobromide, and then treating the same with base to form the aminothiazole.
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