25699-87-0

Upstream product

• 288-88-0 1,2,4-Triazole 
• 394-47-8 2-fluorobenzonitrile 
• 41253-21-8 sodium triazole 

Downstream Products

• 138479-54-6 2-(1',2',4'-triazol-1'-yl)benzoic acid 
• 449756-97-2 2-(1,2,4-triazol-1-yl)-benzylamine 
• 724710-05-8 {1-(R)-benzyl-2-oxo-2-[2-(2-[1,2,4]triazol-1-yl-benzyl-carbamoyl)pyrrolidin-1-(S)-yl]-ethyl}carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

2-(1,2,4-triazolyl)benzoyl arylamine active compound for inhibiting pathogens causing take-all disease of wheat

The invention discloses a 2-(1,2,4-triazolyl)benzoyl arylamine active compound for inhibiting pathogens causing the take-all disease of wheat. The active compound is characterized in that the active compound has a structure shown as a formula I which is d

HIV integrase inhibitors

The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

HIV INTEGRASE INHIBITORS

The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

HIV INTEGRASE INHIBITORS: CYCLIC PYRIMIDINONE COMPOUNDS

The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed. Formula: (I).

BICYCLIC HETEROCYCLES AS HIV INTEGRASE INHIBITORS

The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

Preparation of highly potent and selective non-peptide antagonists of the arginine vasopressin V1A receptor by introduction of a 2-ethyl-1H-1-imidazolyl group

To find a new series of arginine vasopressin (AVP) V1A receptor antagonists, the influence of the 2-phenyl group of 2-phenyl-4′-[(2,3,4,5- tetrahydro-1H-1-benzazepin-1-yl)carbonyl]benzanilide (7) was investigated. Replacement of the 2-phenyl group by a 2-ethyl-1H-imidazol-1-yl group was effective in yielding a V1A-selective compound. Moreover, this imidazolyl group was introduced in the same position in YM-35471 (6), and further studies of these compounds were performed. Consequently, we found that the (Z)-4′-({4,4-difluoro-5-[(N-cyclo-propylcarbamoyl) methylene]-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl}carbonyl)-2-(2-ethyl-1H-1- imidazol-1-yl)benzanilide (9f) exhibited highly potent affinity and selectivity, and was the most potent antagonist for the V1A receptor among our compounds. The synthesis and pharmacological evaluation of these compounds are described in this paper

HIV integrase inhibitors: cyclic pyrimidinone compounds

The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed.

Bicyclic heterocycles as HIV integrase inhibitors

The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors

In an effort to discover potent, clinically useful thrombin inhibitors, a rapid analogue synthetic approach was used to explore the P1 region. Various benzylamines were coupled to a pyridine/pyrazinone P2-P 3 template. One compound with an o-thiadiazole benzylic substitution was found to have a thrombin Ki of 0.84 nM. A study of ortho-substituted five-membered-ring heterocycles was undertaken and subsequently demonstrated that the o-triazole and tetrazole rings were optimal. Combination of these potent P1 aryl heterocycles with a variety of P2-P3 groups produced a compound with an extraordinary thrombin inhibitory activity of 1.4 pM. It is hoped that this potency enhancement in P1 will allow for more diversification in the P 2-P3 region to ultimately address additional pharmacological concerns.

Cyclization Reactions in Azole Chemistry: The Reaction of Some Azoles with o-Fluoroacetophenone, o-Fluorobenzaldehyde and o-Fluorobenzophenone

The reactions of some azoles with o-fluoro-acetophenone, -benzaldehyde and -benzophenone in dimethyl sulfoxide solution in the presence of anhydrous potassium carbonate have been investigated.In addition to the expected substitution products, cyclization