162504-85-0Relevant articles and documents
Pleuromutilin derivatives having a purine ring. Part 2: Influence of the central spacer on the antibacterial activity against Gram-positive pathogens
Hirokawa, Yoshimi,Kinoshita, Hironori,Tanaka, Tomoyuki,Nakamura, Takanori,Fujimoto, Koichi,Kashimoto, Shigeki,Kojima, Tsuyoshi,Kato, Shiro
scheme or table, p. 170 - 174 (2009/05/07)
Structural modification of the 4-piperidinethio moiety, as a spacer of the first pleuromutilin analogues 2A and 2B having a purine ring, led to discovery of the novel pleuromutilin derivatives 14B and 17B. These compounds with good solubility in water showed promising in vitro antibacterial activity against various Gram-positive bacteria including MRSA, PRSP, and VRE and have potent in vivo efficacy.
MUTILIN DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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Page/Page column 94, (2010/11/26)
The invention is intended to provide a novel compound which is useful as an antibacterial agent and a manufacturing intermediate thereof and relates to a mutilin derivative represented by the formula (I) which is useful as an antibacterial agent against a multidrug resistant organism, a manufacturing intermediate thereof and the like. In the formula (I), R1 represents an ethyl group or a vinyl group, P1 represent H or a protecting group for a hydroxy group, R2 and R3 represent H or the like, G represents CH2 or the like, A represents -S-, -SO2-, -O- or the like, m represents an integer of 0 to 4, the Q1 ring represents a saturated heterocyclic group, R4 represents H, a lower alkyl group or the like, and W represents a group represented by the formula (W-1) or an amino protection group. In the formula (W-1), X represents a lower alkylene chain, a single bond or the like, Z1 represents CH or the like, Z2, Z3 and Z4 represent N or the like, and Y1 and Y2 represent H, an amino group, a group represented by the formula (Y-1) or the like. In the formula (Y-1), the Q2 ring represents a saturated heterocyclic group, and R9 and R10 represents H, a lower alkyl group or the like. (I) (W-1) (Y-1)
Heterocyclic compounds as inhibitors of rotomase enzymes
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, (2008/06/13)
Compounds of the formula: wherein R1, Y, W, A and R2are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.
Synthesis of a novel cyclic prodrug of RGD peptidomimetic to improve its cell membrane permeation
Song, Xiaoping,Xu, Christine R.,He, Henry T.,Siahaan, Teruna J.
, p. 285 - 301 (2007/10/03)
The objective of this work was to synthesize cyclic prodrug 2 derived from the parent RGD peptidomimetic 1 and to evaluate its chemical and enzymatic stabilities and antithrombic activity. Cyclic prodrug 2 was formed to improve the cell membrane permeation of RGD peptidomimetic 1 by transiently masking the unfavorable physicochemical properties of compound 1. Cyclic prodrug 2 was synthesized by linking the amino and carboxylic acid groups of parent 1 via the (acyloxy)alkoxy promoiety. The prodrug-to-drug conversion of cyclic prodrug 2 was evaluated in isolated esterase and human plasma in the absence and presence of the esterase inhibitor paraoxon. The rate of hydrolysis of cyclic prodrug 2 was significantly faster in plasma (t1/2 = 33.5 ± 0.6 min) than in PBS (t1/2 = 314 ± 11 min). Cyclic prodrug 2 was converted by esterase to the parent compound 1 and this conversion was inhibited by an esterase inhibitor, paraoxon. The IC50 (4 μM) of cyclic prodrug 2 was higher than the IC50 (1.9 μM) of parent drug 1. The antithrombic activity of cyclic prodrug 2 depends on the incubation time in platelet-rich plasma; the activity increases with incubation time, suggesting that the prodrug-to-drug conversion is time-dependent and mediated by esterase. Cyclic prodrug 2 was more stable under acidic and neutral conditions than under basic conditions, suggesting that handling and formulation of this prodrug should be undertaken under acidic conditions.
2,3-diaminopropionic acid derivative
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, (2008/06/13)
The present invention relates to a 2,3-diaminopropionic acid derivative of the formula (1): STR1 or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful as a platelet aggregation inhibitor, a cancer metastasis inhibitor, a wound healing agent or a bone resorption inhibitor.
Dipiperidine derivatives
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, (2008/06/13)
The present invention relates to an novel dipiperidine derivative represented by formula (1), or a pharmaceutically acceptable salt thereof; STR1 wherein R1 represents a hydrogen atom or a lower alkyl group; Y represents a single bond or an oxygen atom; n represents 1, 2 or 3; W represents a methylene group or an oxygen atom; R2 represents a hydrogen atom or a carboxyl modifying group which can be eliminated in vivo; X1 and X3 are the same or different and each represents a hydrogen atom or a lower alkyl group. This compound is useful as platelet aggregation inhibitors, cancer metastasis inhibitors, wound remedies or bone resorption inhibitors.
CARBOXYLIC ACID COMPOUND HAVING CONDENSED RING, SALT THEREOF AND PHARMACEUTICAL USE THEREOF
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, (2008/06/13)
A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases