58004-79-8Relevant academic research and scientific papers
A 2-amino-thiazole compounds (by machine translation)
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Paragraph 0166; 0181-0183, (2016/10/08)
The present invention relates to the technical field of pharmaceutical chemistry, particularly relates to a 2-amino thiazole compound or its pharmaceutically acceptable salts, its preparation method, and pharmaceutical compositions containing such compounds and its application in the preparation of antineoplastic. (by machine translation)
Discovery of a Novel Series of Imidazo[1,2-a]pyrimidine Derivatives as Potent and Orally Bioavailable Lipoprotein-Associated Phospholipase A2 Inhibitors
Chen, Xinde,Xu, Wenwei,Wang, Kai,Mo, Mingguang,Zhang, Wei,Du, Lili,Yuan, Xiaojing,Xu, Yechun,Wang, Yiping,Shen, Jianhua
, p. 8529 - 8541 (2015/11/24)
Inhibition of lipoprotein-associated phospholipase A2 (Lp-PLA2) has been suggested to be a promising therapeutic strategy for several inflammation-associated diseases, including atherosclerosis, Alzheimer's disease, and diabetic macu
Diarylthiazole: An antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system
Bellale, Eknath,Naik, Maruti,Vb, Varun,Ambady, Anisha,Narayan, Ashwini,Ravishankar, Sudha,Ramachandran, Vasanthi,Kaur, Parvinder,McLaughlin, Robert,Whiteaker, James,Morayya, Sapna,Guptha, Supreeth,Sharma, Sreevalli,Raichurkar, Anandkumar,Awasthy, Disha,Achar, Vijayshree,Vachaspati, Prakash,Bandodkar, Balachandra,Panda, Manoranjan,Chatterji, Monalisa
supporting information, p. 6572 - 6582 (2014/10/15)
Diarylthiazole (DAT), a hit from diversity screening, was found to have potent antimycobacterial activity against Mycobacterium tuberculosis (Mtb). In a systematic medicinal chemistry exploration, we demonstrated chemical opportunities to optimize the potency and physicochemical properties. The effort led to more than 10 compounds with submicromolar MICs and desirable physicochemical properties. The potent antimycobacterial activity, in conjunction with low molecular weight, made the series an attractive lead (antibacterial ligand efficiency (ALE) >0.4). The series exhibited excellent bactericidal activity and was active against drug-sensitive and resistant Mtb. Mutational analysis showed that mutations in prrB impart resistance to DAT compounds but not to reference drugs tested. The sensor kinase PrrB belongs to the PrrBA two component system and is potentially the target for DAT. PrrBA is a conserved, essential regulatory mechanism in Mtb and has been shown to have a role in virulence and metabolic adaptation to stress. Hence, DATs provide an opportunity to understand a completely new target system for antimycobacterial drug discovery.
Indole compounds as COX-2 inhibitors
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, (2008/06/13)
This invention provides a compound of the following formula: and the pharmaceutically acceptable salts thereof, wherein L is oxygen or sulfur; Y is a direct bond or C1-4alkylidene; Q is C1-6alkyl, C3-7cycloalkyl, phenyl, naphthyl, heteroaryl or the like; R1is hydrogen, C1-6alkyl or the like; R2is hydrogen, C1-4alkyl, C(O)R5wherein R5is C1-22alkyl or C2-22alkenyl, halosubstituted C1-8alkyl, halosubstituted C2-8alkenyl, —Y—C3-7cycloalkyl, —Y—C3-7cycloalkenyl, phenyl, naphthyl, heteroaryl or the like; X is halo, C1-4alkyl, hydroxy, C1-4alkoxy or the like; and n is 0, 1, 2 or 3, with the proviso that a group of formula —Y—Q is not methyl or ethyl when X is hydrogen; L is oxygen; R1is hydrogen; and R2is acetyl. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.
