162504-85-0Relevant academic research and scientific papers
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.
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
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.
