The degradation of sulfonamides has two different pathways: the N-acetylation pathway which is genetically determined and saturable, and the cytochrome P450 pathway which produces toxic hydroxylamine metabolites "detoxified" by glutathione. (A2885)
Studies utilizing radioactive micronized silver sulfadiazine, electron microscopy, and biochemical techniques have revealed that the mechanism of action of silver sulfadiazine on bacteria differs from silver nitrate and sodium sulfadiazine. Silver sulfadiazine acts only on the cell membrane and cell wall to produce its bactericidal effect. A specific mechanism of action has not been determined, but silver sulfadiazine's effectiveness may possibly be from a synergistic interaction, or the action of each component. Silver is a biocide, which binds to a broad range of targets. Silver ions bind to nucleophilic amino acids, as well as sulfhydryl, amino, imidazole, phosphate, and carboxyl groups in proteins, causing protein denaturation and enzyme inhibition.
Silver binds to surface membranes and proteins, causing proton leaks in the membrane, leading to cell death.
Sulfadiazine is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), a substrate of the enzyme dihydropteroate synthetase. The inhibited reaction is necessary in these organisms for the synthesis of folic acid.
来源:Toxin and Toxin Target Database (T3DB)
毒理性
致癌物分类
对人类无致癌性（未列入国际癌症研究机构IARC清单）。
No indication of carcinogenicity to humans (not listed by IARC).
来源:Toxin and Toxin Target Database (T3DB)
毒理性
健康影响
健康影响包括皮肤死亡区域、身体上的红色隆起皮疹和银质沉着症（皮肤变色）。
Health effects include areas of dead skin, red and raised rash on the body, and argyria (Skin discoloration). [Wikipedia]
来源:Toxin and Toxin Target Database (T3DB)
毒理性
暴露途径
非常有限的穿透皮肤。通常只有当涂抹在非常大的烧伤面积上时，吸收到体内才成为一个问题。
Very limited penetration through the skin. Only when applied to very large area burns is absorption into the body generally an issue.
来源:Toxin and Toxin Target Database (T3DB)
毒理性
症状
症状包括灼热感。（维基百科）
Symptoms include burning sensation. [Wikipedia]
来源:Toxin and Toxin Target Database (T3DB)
吸收、分配和排泄
吸收
非常有限的穿透皮肤。通常只有当涂抹在非常大的烧伤面积上时，吸收进体内才成为一个问题。
Very limited penetration through the skin. Only when applied to very large area burns is absorption into the body generally an issue.
在温和的反应条件下，例如大气压和低温下，二氧化碳的化学固定取决于催化剂的能力。在此，描述了磺胺嘧啶银/ n Bu 4 NBr的协同催化方案，用于炔丙醇，CO 2和一元醇的三组分反应。有效地证明了该催化体系可提供优异收率的碳酸β-氧代丙酯（使用5 mol％的催化剂收率可达99％）。该方法在大气CO 2压力和无溶剂条件下可耐受各种炔丙醇和一元醇。出色的催化性能归因于精心的实验证实了协同催化作用。
The present description relates to fused polycyclic 2-pyridinone compounds and forms and pharmaceutical compositions thereof and methods of using such compounds, forms or compositions thereof for treating or ameliorating a wild-type or drug-resistant form of N. gonorrhoeae or N. meningitides. A compound of Formula (la), Formula (lb) or Formula (Ic), or a form thereof, wherein the dashed lines represent one or more double bonds optionally present where allowed by available valences.
[EN] COMPOSITIONS AND METHODS FOR THE TREATMENT OF BACTERIAL INFECTIONS<br/>[FR] COMPOSÉS ET MÉTHODES POUR LE TRAITEMENT D'INFECTIONS BACTÉRIENNES
申请人：CIDARA THERAPEUTICS INC
公开号：WO2018006063A1
公开（公告）日：2018-01-04
Compositions and methods for the treatment of bacterial infections include compounds containing dimers of cyclic heptapeptides conjugated to one or more monosaccharide or oligosaccharide moieties. In particular, compounds can be used in the treatment of bacterial infections caused by Gram-negative bacteria.
Substituted 1,3-thiazole compounds, their production and use
申请人：——
公开号：US20040053973A1
公开（公告）日：2004-03-18
(1) A 1,3-thiazole compound of which the 5-position is substituted with a 4-pyridyl group having a substituent including no aromatic group or (2) a 1,3-thiazole compound of which the 5-position is substituted with a pyridyl group having at the position adjacent to a nitrogen atom of the pyridyl group a substituent including no aromatic group has an excellent p38 MAP kinase inhibitory activity.
[EN] RANDOM COPOLYMER THERAPEUTIC AGENT CARRIERS AND ASSEMBLIES THEREOF<br/>[FR] SUPPORTS POUR AGENTS THÉRAPEUTIQUES À BASE D'UN COPOLYMÈRE ALÉATOIRE ET ENSEMBLES À BASE DE CEUX-CI
申请人：UNIV WASHINGTON CT COMMERCIALI
公开号：WO2015073579A1
公开（公告）日：2015-05-21
Provided herein are particles assemblies including a shell surrounding a core. The shell includes a particle-stabilizing random copolymer. The core includes a core random copolymer. The particle assemblies have a biomimetic design in which the polymeric components containing discrete chemical and biological functionalities are designed to spontaneously self-assemble into particles. Also provided herein are random copolymers having conjugated therapeutic agents that can be cleaved from the copolymers by an enzyme or water.
[EN] COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS<br/>[FR] COMPOSÉS DESTINÉS AU TRAITEMENT DE TROUBLES MÉDICAUX
申请人：ACHILLION PHARMACEUTICALS INC
公开号：WO2017035360A1
公开（公告）日：2017-03-02
Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula (I), or a pharmaceutically acceptable salt or composition thereof The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.
