Anti-HIV activity of new pyrazolobenzothiazine 5,5-dioxide-based acetohydrazides [0.03%]
基于吡唑并苯并噻嗪5,5-二氧化物的乙酰肼类抗HIV活性研究
Zunera Khalid,Sana Aslam,Matloob Ahmad et al.
Zunera Khalid et al.
A series of fifteen new 2-[3-(3-chlorophenyl)-5,5-dioxidobenzo[e]pyrazolo[4,3-c][1,2]thiazin-4(2H)-yl]-N'-arylmethyleneacetohydrazides (5a-o) were synthesized and screened for their anti-HIV-1 and cytotoxicity activity. Out of fifteen pyraz...
Anti-human immunodeficiency activity of novel 2-arylpyrrolidine analogs [0.03%]
新型2-芳基吡咯烷类似物的抗人类免疫缺陷病毒活性
Ashot H Martirosyan,Sahak P Gasparyan,Marina V Alexanyan et al.
Ashot H Martirosyan et al.
A series of 26 new compounds were synthesized and screened for their anti-human immunodeficiency virus-1 and cytotoxicity activity. Of these, 14 were found to be inhibitors of human immunodeficiency virus replications in primary human lymph...
Synthesis, structural characterization and antimycobacterial evaluation of several halogenated non-nitro benzothiazinones [0.03%]
几种卤代非硝基苯并噻嗪酮的合成、结构表征及抗分枝杆菌活性评估
Balungile Madikizela,Tamira Eckhardt,Richard Goddard et al.
Balungile Madikizela et al.
8-Nitro-1,3-benzothiazin-4-ones (BTZs), with BTZ043 and PBTZ169 as the most advanced compounds, represent a new class of potent antitubercular agents, which irreversibly inhibit decaprenylphosphoryl-β-d-ribose-2'-epimerase (DprE1), an enzy...
4-Benzylideneisoquinoline-1,3(2H, 4H)-diones as tyrosyl DNA phosphodiesterase 2 (TDP2) inhibitors [0.03%]
4-苯基烯丙基异喹啉-1,3(2H, 4H)-二酮类酪氨酰-DNA磷酸酯酶2(TDP2)抑制剂
Sameera Senaweera,Tianyu He,Haixi Cui et al.
Sameera Senaweera et al.
Tyrosyl-DNA phosphodiesterase 2 (TDP2) repairs topoisomerase II (Top2) mediated DNA damages, including double-strand breaks (DSBs) that underpin the anticancer mechanism of clinical TOP2 poisons such as etoposide (ETP). Inhibition of TDP2 c...
First In Class (S, E)-11-[2-(Arylmethylene)Hydrazono]-PBD Analogs As Selective CB2 Modulators Targeting Neurodegenerative Disorders [0.03%]
一类(S,E)-11-[2-(芳甲烯基)腙基]-PBD衍生物作为选择性CB₂调制剂靶向神经退行性疾病
David Mingle,Meirambek Ospanov,Mohamed O Radwan et al.
David Mingle et al.
Newly designed pyrrolo[2,1-c][1,4]benzodiazepines tricyclic skeleton has shown potential clusters of cannabinoid receptors CB1/CB2 selective ligands. CB2 plays a critical role in microglial-derived neuroinflammation, where it modulates cell...
n-Propyl 6-amino-2,6-dideoxy-2,2-difluoro-β-d-glucopyranoside is a good inhibitor for the β-galactosidase from E. coli [0.03%]
6-氨基-2,6-二脱氧-2,2-二氟-β-D-葡萄吡喃糖基-n-丙胺是E.coli β-半乳糖苷酶的良好抑制剂
Immo Serbian,Erik Prell,Claudia Fischer et al.
Immo Serbian et al.
A convenient route has been developed for the synthesis of novel 6-amino-2,2-(or 3,3-difluoro)-2-(or 3),6-dideoxy-hexopyranoses. Biological screening showed these compounds as good inhibitors for several glycosidases. Especially n-propyl 6-...
Discovery of sultam-containing small-molecule disruptors of the huntingtin-calmodulin protein-protein interaction [0.03%]
小分子猎取蛋白-蛋白相互作用中断剂的发现
Nicholas J Klus,Khushboo Kapadia,Peter McDonald et al.
Nicholas J Klus et al.
The aberrant protein-protein interaction between calmodulin and mutant huntingtin protein in Huntington's disease patients has been found to contribute to Huntington's disease progression. A high-throughput screen for small molecules capabl...
Haizhou Zhu,Venkateshwara Dronamraju,Wei Xie et al.
Haizhou Zhu et al.
Sulfur is widely existent in natural products and synthetic organic compounds as organosulfur, which are often associated with a multitude of biological activities. OBenzothiazole, in which benzene ring is fused to the 4,5-positions of the ...
Exploring 1-adamantanamine as an alternative amine moiety for metabolically labile azepane ring in newly synthesized benzo[ d]thiazol-2(3 H)one σ receptor ligands [0.03%]
作为新合成的苯并[d]噻唑-2(3H)酮σ受体配体中代谢不稳定的氮杂环庚烷环的替代胺基团研究1-adamantanamine的作用
Sebastiano Intagliata,Hebaalla Agha,Theresa A Kopajtic et al.
Sebastiano Intagliata et al.
In this work we report the structure-activity relationships, binding properties, and metabolic stability studies of a series of benzo[d]thiazol-2(3H)one as sigma receptors (σRs) ligands. Specifically, to improve the metabolic stability of ...
Screening Trimethoprim Primary Metabolites for Covalent Binding to Albumin [0.03%]
筛选能够与白蛋白共价结合的甲氧苄氨嘧啶初级代谢物
Whitney M Nolte,Robert T Tessman,Jennifer L Goldman
Whitney M Nolte
Modification of endogenous proteins by drugs and drug metabolites are thought to be a cause of idiosyncratic adverse drug reactions (IADRs). Trimethoprim (TMP) is a commonly prescribed antibiotic that has been implicated in IADRs; however, ...