93794-39-9

Upstream product

• 13895-04-0 6-methoxybenzo[d]oxazole-2(3H)-thione 
• 13895-04-0 6-methoxybenzo[d]oxazole-2-thiol 
• 40925-70-0 2-amino-5-methoxyphenol 
• 140-90-9 sodium O-ethyl dithiocarbonate 
• 39547-15-4 1-amino-2-hydroxy-4-methoxybenzene hydrochloride 
• 150-19-6 O-methylresorcine 
• 704-14-3 3-methoxy-6-nitro-phenol 

Downstream Products

• 532-91-2 coixol 
• 1334386-03-6 (S)-2-(2-hydroxy-4-methoxyphenylamino)-thiazoline-5,5-dimethyl-4-carboxylic acid trifluoroacetate 
• 1334386-20-7 (R)-2-(2-hydroxy-4-methoxyphenylamino)-thiazoline-4-carboxylic acid hydrochloride 
• 1334386-19-4 (R)-2-(6-methoxybenzoxazol-2-ylamino)-3-tritylsulfanyl-propionic acid 

Relevant academic research and scientific papers

HMOX1 inducers

The present invention is related to compounds of structure (I) as heme oxygenase 1 (HMOX 1) inducers. The present invention is also related a method of controlling the activity or the amount, or both the activity and the amount, of heme-oxygenase 1 in a mammalian subject. The definitions of the variables are provided herein.

Preparation, antibacterial evaluation and preliminary structure-activity relationship (SAR) study of benzothiazol- and benzoxazol-2-amine derivatives

In this study, a novel benzothiazol- and benzooxazol-2-amine scaffold with antibacterial activity was designed and synthesized. Preliminary structure-activity relationship analysis displayed that compound 8t with a 5,6-difluorosubstituted benzothiazole was found to be a potent inhibitor of Gram-positive pathogens, and exhibited some potential against drug-resistant bacteria and without cytotoxicity in therapeutic concentrations. In addition, molecular docking studies indicated that Staphylococcus aureus methionyl-tRNA synthetase might be the possible target of these compounds. Taken together, the present study provides an effective entry to the synthesis of a good lead for subsequent optimization and a new small molecule candidate drug for antibacterial therapeutics.

Analgesic Compounds, Compositions, and Uses Thereof

The invention relates to compounds, compositions, and methods for diminishing pain in a subject in need thereof comprising administering the compounds and compositions herein described.

Piperidinyl and piperazinyl compounds substituted with bicyclo-heterocyclylalkyl groups useful as CCR3 receptor antagonists

Compounds having the Formula (I), are useful as CCR3 receptor antagonists, wherein Ar is aryl or heteroaryl; Q is —C(═O)— or C1-2alkylene; X is N(+)R9a, or N; Y is CR9b, or N; R2 is hydrogen or alkyl; R3 and R4 are as defined in the specification; Uc is a mono- or bicyclic group as defined in the specification; n is 0 or 1; and p is 0, 1, 2, 3 or 4.

A new 5-HT3 receptor ligand. II. Structure-activity analysis of 5-HT3 receptor agonist action in the gut

Several modified 2-piperazinyl benzoxazole derivatives, which exhibit an agonistic effect on gastrointestinal motility, were synthesized and their effects on the contraction of guinea-pig ileum were examined. The quaternary piperazinyl benzoxazole structure has a restricted conformation and stereostructure compared to those of the other 5-HT3 receptor agonists, serotonin and meta-chlorophenylbiguanide. The mutual positions of the aromatic ring, nitrogen atom and terminal amine are considered to form the pharmacophore of the 5-HT3 receptor agonist in the gut. In the serotonin- evoked reflex bradycardia [Bezold-Jarisch (B-J) reflex] inhibition test using rats the B-J reflex-inducing ratio was different for each synthesized compound. These results suggest that, in these 5-HT3 receptor agonists, the substituents of the benzoxazole ring influence the B-J reflex-inducing activity in rats.

BENZOXAZOLE DERIVATIVES

A benzoxazole derivative of the formula (1) or (2) which has an alicyclic diamine group at the 2-position: STR1 wherein R 1, R. sup.2, R 3, R 4, R 5, R 6, X -, m and n are defined herein. The compound shows excellent 5-HT 3 receptor antagonism and is useful as an antiemetic agent, a peristalsis controlling agent, an analgesic agent, an antianxiety agent and a schizophrenia treating agent.

3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: Inhibitors of immune complex induced inflammation

3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives were evaluated in the dermal and pleural reverse passive Arthus reactions in the rat. In the pleural test these compounds were effective in reducing exudate volume and accumulation of white blood cells. This pattern of activity was similar to that of hydrocortisone and different from that of indomethacin. The structural requirements for inhibiting the Arthus reactions were studied by systematic chemical modification of 1. These structure-activity relationship studies revealed that nitrogen 1' of the hydrazino group is essential for activity and must be electron rich, whereas chemical modifications of other sites of 1 had only a modest effect on activity.