CAS: 1219-77-8; 2-(5-Benzyl-6-Thioxo-1,3,5-Thiadiazinan-3-yl)Acetic Acid

📜苄胺置于potassium Hydroxide体系中,用 Aq. Phosphate Buffer,水 用作溶剂,化学反应 12.0H,反应生成苄硫嗪酸
参考文献:含有酰肼部分的新型1,3,5-噻二嗪-2-硫酮衍生物:体外和体内对植物病原真菌的设计,合成和生物活性评估
标题:含有酰肼部分的新型1,3,5-噻二嗪-2-硫酮衍生物:体外和体内对植物病原真菌的设计,合成和生物活性评估
摘要:摘要设计,合成并评估了一系列带有酰肼部分的新型1,3,5-噻二嗪-2-硫酮衍生物,它们对茄形枯萎病菌,禾谷镰刀菌(fg),灰葡萄孢(bc)和菜青虫具有抗真菌活性.辣椒炭疽病菌(cc).体外抗真菌生物测定表明,大多数标题化合物相对于fg,Bc和cc表现出非常好的选择性和特异性.引人注目的是,标题化合物n'-(4-氯苯基)-2-(5-苯基-6-Thioxo-1,3,5-噻二嗪基-3-基)乙酰肼(5B)明显抑制了rs的体外生长. Ec50值为0.24μg/ Ml,比商品化的杀菌剂多菌灵(0.55μg/ Ml)高约2倍.在稻叶上进一步评估了标题化合物5B的体内抗rs效应,控制效力为98.在200μg/ Ml下为58%,在100μg/ Ml下为61.27%.上述研究为进一步研究结构为酰肼部分的1,3,5-噻二嗪-2-硫酮衍生物作为潜在的杀菌剂提供了重要参考.
Doi:10.1016/j.Cclet.2019.03.038

专利信息

专利号:US-7199128-B2
优先权日:2005-02-02
标题 :8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents
发明人：BRADBURY BARTON J; WILES JASON ALLAN; DESHPANDE MILIND; WANG QIUPING; HASHIMOTO AKIHIRO; LUCIEN EDLAINE
权利人:ACHILLION PHARMACEUTICALS INC
摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.

专利号:US-2009012071-A1
优先权日:2007-04-23
标 题 :4-substituted-1h-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2h,9h)-diones and related compounds as anti-infective agents
发明人：BRADBURY BARTON JAMES; DESHPANDE MILIND; HASHIMOTO AKIHIRO; KIM HA YOUNG; LUCIEN EDLAINE; PAIS GODWIN; PUCCI MICHAEL JOHN; WANG QIUPING; WILES JASON ALLAN
权利人:ACHILLION PHARMACEUTICALS INC
摘要:The present invention provides compounds of the formula that possess antimicrobial activity. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity. Particular compounds provided herein are also potent and/or selective inhibitors of microbial DNA synthesis and reproduction. The invention provides anti-microbial compositions, including pharmaceutical compositions, containing a compound of the invention and one or more or more carriers. The invention provides pharmaceutical compositions containing a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound as the only active agent or in combination with one or more other active agents. The invention provides methods for treating or preventing microbial infections, preferably animals, by administering an effective amount of a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound to an organism suffering from or susceptible to microbial infection. The invention also provides methods of inhibiting microbial growth and survival by applying an effective amount of a 4-substituted- 1 H-isothiazolo[5,4-b][1,4]oxazino[2,3,4-ij]quinoline-7,8(2H,9H)-dione or related compound.

专利号:US-8946422-B2
优先权日:2005-07-27
标题:8-methoxy-9H-isothiazolo[5,4-B]quinoline-3,4-diones and related compounds as anti-infective agents
发明人：BRADBURY BARTON JAMES; WILES JASON ALLAN; WANG QIUPING; HASHIMOTO AKHIRO; LUCIEN EDLAINE; PAIS GODWIN CLARENCE GILROY; DESHPANDE MILIND; PUCCI MICHEAL JOHN; KIM HA YOUNG
权利人:BRADBURY BARTON JAMES; WILES JASON ALLAN; WANG QIUPING; HASHIMOTO AKHIRO; LUCIEN EDLAINE; PAIS GODWIN CLARENCE GILROY; DESHPANDE MILIND; PUCCI MICHEAL JOHN; KIM HA YOUNG; ACHILLION PHARMACEUTICALS INC
摘要:The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R2, R3, R5, R6, R7, and R9 shown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

专利号:US-7659399-B2
优先权日:2005-01-05
标 题 :1-thia-2,4a-diaza-cyclopenta[b]napththalene-3,4-diones and related compounds as anti-infective agents
发明人：BRADBURY BARTON JAMES; WILES JASON ALLAN
权利人:ACHILLION PHARMACEUTICALS INC
摘要:The invention provides compounds and salts of Formula I and Formula II: n nwhich possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A 1 , A 8 , R 2 , R 3 , R 5 , R 6 , R 7 , and R 9 are defined herein.n n Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

专利号:EP-1809639-B1
优先权日:2004-11-11
标 题 :8a, 9-dihydro-4a-h-isothiazolo[5,4-b] quinoline-3, 4-diones and related compounds as anti-infective agents
发明人：BRADBURY BARTON JAMES; DESHPANDE MILIND; PUCCI MICHAEL JOHN; WANG QIUPING; WILES JASON ALLAN; SONG YONGSHENG; HASHIMOTO AKIHIRO; LUCIEN EDLAINE
权利人:ACHILLION PHARMACEUTICALS INC
摘要:The invention provides compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables n, m, p, R_A, R_B, A₁, R₂, R₃, R₅, R₆, R₇, A₈ and R₉ are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in eukaryotes.

专利号:CN-101208345-B
优先权日:2005-05-25
标 题 :(S) -N-methylnaltrexone, method of synthesis and pharmaceutical use thereof