42182-65-0Relevant articles and documents
Benzothiazole-oxazole type alpha-glucosidase inhibitor and preparation method and application thereof
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Paragraph 0022; 0024, (2018/10/19)
The invention discloses a benzothiazole-oxazole type alpha-glucosidase inhibitor and a preparation method and application thereof. The method comprises the following steps: adding a compound (II) andhydroxylamine hydrochloride in a methanol aqueous solution and a sodium carbonate aqueous solution to obtain a compound (III); adding the compound (III), zinc powder and ammonium formate in methanol and reacting to obtain a compound (IV); and adding the compound (IV), a compound (V), iodine and potassium carbonate in DMF and reacting to obtain a compound (I). The chemical formula of the compound (I) is as shown in specification, the chemical formula of the compound (II) is as shown in specification, the chemical formula of the compound (III) is as shown in specification, the chemical formula of the compound (IV) is as shown in specification, and the chemical formula of the compound (V) is as shown in specification. The benzothiazole-oxazole type compound has obvious inhibition effect on alpha-glucosidase, the preparation method is simple, reaction conditions are gentle, and thus, the benzothiazole-oxazole type alpha-glucosidase inhibitor is suitable for being industrially produced on alarge scale.
Role of benzimidazole (Bid) in the δ-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH2-Bid (UFP-502)
Salvadori, Severo,Fiorini, Stella,Trapella, Claudio,Porreca, Frank,Davis, Peg,Sasaki, Yusuke,Ambo, Akihiro,Marczak, Ewa D.,Lazarus, Lawrence H.,Balboni, Gianfranco
, p. 3032 - 3038 (2008/09/19)
H-Dmt-Tic-NH-CH2-Bid (UFP-502) was the first δ-opioid agonist prepared from the Dmt-Tic pharmacophore. It showed interesting pharmacological properties, such as stimulation of mRNA BDNF expression and antidepression. To evaluate the importance of 1H-benzimidazol-2-yl (Bid) in the induction of δ-agonism, it was substituted by similar heterocycles: The substitution of NH(1) by O or S transforms the reference δ-agonist into δ-antagonists. Phenyl ring of benzimidazole is not important for δ-agonism; in fact 1H-imidazole-2-yl retains δ-agonist activity.
Phenylimidazole derivatives as specific inhibitors of bacterial enoyl-acyl carrier protein reductase FabK
Ozawa, Tomohiro,Kitagawa, Hideo,Yamamoto, Yasuo,Takahata, Sho,Iida, Maiko,Osaki, Yumi,Yamada, Keiko
, p. 7325 - 7336 (2008/04/05)
Bacterial enoyl-acyl carrier protein (ACP) reductases (FabI and FabK) catalyze the final step in each cycle of bacterial fatty acid biosynthesis and are attractive targets for the development of new antibacterial agents. Here, we report the development of novel FabK inhibitors with antibacterial activity against Streptococcus pneumoniae. Based on structure-activity relationship (SAR) studies of our screening hits, we have developed novel phenylimidazole derivatives as potent FabK inhibitors.
Thiazole derivative
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, (2008/06/13)
A thiazole compound of the formula: STR1 wherein T is lower alkylene; u is 0 or 1; R1 and R2 are the same or different and are each H, or lower alkyl, etc.; R3 is STR2 R4 is H or lower alkanoyloxy-lower alkyl, which shows inhibitory activity on protein kinase C (PKC, Ca2+ /phospholipid-depending serine/threonine protein phosphatase), and are useful as a protein kinase C inhibitor.