- Application of "hydrogen bonding interaction" in new drug development: Design, synthesis, antiviral activity, and sars of thiourea derivatives
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A series of simple thiourea derivatives were designed based on the structure of natural product harmine and lead compound and synthesized from amines in one step. The antiviral activity of these thiourea derivatives was evaluated. Most of them exhibited significantly higher anti-TMV activity than commercial plant virucides ribavirin, harmine, and lead compound. The hydrogen bond was found to be important but not the more the better. The optimal compound (R,R)-20 showed the best anti-TMV activity in vitro and in vivo (in vitro activity, 75%/500 a??g/mL and 39%/100 a??g/mL; inactivation activity, 71%/500 a??g/mL and 35%/100 a??g/mL; curative activity, 73%/500 a??g/mL and 37%/100 a??g/mL; protection activity, 69%/500 a??g/mL and 33%/100 a??g/mL), which is significantly higher than that of Ningnanmycin. The systematic study provides strong evidence that these simple thiourea derivatives could become potential TMV inhibitors.
- Lu, Aidang,Wang, Ziwen,Zhou, Zhenghong,Chen, Jianxin,Wang, Qingmin
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p. 1378 - 1384
(2015/03/05)
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- CHIRAL ANALYSIS OF THE REACTION STAGES IN THE EDMAN METHOD FOR SEQUENCING PEPTIDES
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Chiral isothiocyanate reagents suitable for 'Edman sequencing' have been synthesised and used to assess the chiral features of individual stages in the Edman method.Using h.p.l.c. analysis of the diastereoisomeric thiohydantoins obtained, it has been deduced that the cyclisation and cleavage of thiazolinone step is the likely source of racemisation of the chiral centre derived from the N-terminal amino acid.
- Davies, John S.,Mohammed, Karim A.
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p. 1723 - 1728
(2007/10/02)
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- KINETICS OF REACTION OF ISOTHIOCYANATE DERIVATIVES OF STILBENE WITH GLYCINE AND OF PHENYLISOTHIOCYANATE WITH ALANINE ETHYL ESTER
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The kinetics of reaction of isothiocyanate derivatives of trans-stilbene with glycine, the kinetics of cyclization reaction of derivatives of stilbenethiocarbamylglycine to thiohydantoins and the kinetics of reaction of phenylisothiocyanate with alanine ethyl ester were studied.
- Kuczek, Marian,Nowak, Kornel
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p. 1691 - 1696
(2007/10/02)
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