149267-65-2Relevant articles and documents
Design, synthesis and antiviral activity of novel pyridazines
Wang, Ziwen,Wang, Mingxiao,Yao, Xue,Li, Yue,Tan, Juan,Wang, Lizhong,Qiao, Wentao,Geng, Yunqi,Liu, Yuxiu,Wang, Qingmin
experimental part, p. 33 - 41 (2012/09/08)
A series of pyridazines were prepared and evaluated for their anti-HIV activity. The new synthetic route involving a novel rearrangement reaction provided a practical method for the preparation of 5-hydroxypyridazines. The primary bioassay results indicated that most of the pyridazines possess anti-HIV activity. It ought to been mentioned that the rearranged compounds 35 and 39 exhibited relatively higher HIV inhibitory effect. Most of the synthesized compounds were also found to possess good anti-TMV activity, of which compound 9 showed similar in vivo anti-TMV activity to commercial plant virucide Ribavirin. This work provides a new and efficient approach to evolve novel multi-functional antiviral agents by rational integration and optimization of previously reported antiviral agents.
PYRAZOLE COMPOUNDS
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, (2010/04/30)
The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineralocorticoid receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of a disease or condition mediated by the mineralocorticoid receptor activation.
Antiretroviral hydrazine derivatives
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, (2008/06/13)
The invention relates to compounds of formula STR1 and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.
Aza-peptide analogs as potent human immunodeficiency virus type-1 protease inhibitors with oral bioavailability
F?ssler, Alexander,Bold, Guido,Capraro, Hans-Georg,Cozens, Robert,Mestan, Jürgen,Poncioni, Bernard,R?sel, Johannes,Tintelnot-Blomley, Marina,Lang, Marc
, p. 3203 - 3216 (2007/10/03)
A series of aza-peptide analogs with a (hydroxyethyl)hydrazine isostere has been synthesized as HIV-1 protease inhibitors using a simple synthetic scheme. Structure-activity studies based on the X-ray of a previously described inhibitor-enzyme complex led to potent inhibitors with antiviral activity in the low-nanomolar range. The S-configuration of the transition- state hydroxyl group was preferred in this series. Small modifications of the P2P3 and P2'P3' substituents had little effect on enzyme inhibition but greatly influenced the pharmacokinetic profile. As a result of these studies, the symmetrically acylated compound 8a and its close analog 24a bearing a methyl carbamate in P3 and an ethyl carbamate in P3' position were identified as potent inhibitors with plasma concentrations exceeding antiviral ED50 values 150-fold following oral application in mice.
RETROVIRAL PROTEASE INHIBITING COMPOUNDS
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, (2008/06/13)
A retroviral protease inhibiting compound of the formula: STR1 is disclosed wherein R 1, R 2, R 5, R 6, Y m and Y' n are herein defined.
Facile Synthesis of Potent HIV-1 Protease Inhibitors containing a Novel Pseudo-symmetric Dipeptide Isostere
Sham, Hing L.,Betebenner, David A.,Zhao, Chen,Wideburg, Norman E.,Saldivar, Ayda,et al.
, p. 1052 - 1053 (2007/10/02)
A series of potent inhibitors of the HIV-1 protease containing a novel pseudo-symmetric dipeptide isostere 3 was synthesized via ring opening of a protected epoxide with various substituted hydrazines.
