176178-87-3

Upstream product

• 58997-11-8 3-methylisonicotinic acid ethyl ester 
• 116985-92-3 Methyl 3-methylpyridine-4-carboxylate 
• 4021-12-9 3-methyl-isonicotinic acid 

Downstream Products

• 4497-17-0 3-methyl-isonicotinic acid vanillylidenehydrazide 
• 883557-46-8 {5-[3-((E)-2-Benzo[1,3]dioxol-5-yl-vinyl)-pyridin-4-yl]-[1,3,4]oxadiazol-2-yl}-(3-trifluoromethyl-phenyl)-amine 
• 883557-80-0 {5-[3-((E)-2-Pyridin-4-yl-vinyl)-pyridin-4-yl]-[1,3,4]oxadiazol-2-yl}-(3-trifluoromethyl-phenyl)-amine 
• 883557-63-9 {5-[3-((E)-2-Pyridin-4-yl-vinyl)-pyridin-4-yl]-[1,3,4]oxadiazol-2-yl}-(4-trifluoromethyl-phenyl)-amine 
• 883557-62-8 {5-[3-((E)-2-Pyridin-4-yl-vinyl)-pyridin-4-yl]-[1,3,4]oxadiazol-2-yl}-(4-trifluoromethoxy-phenyl)-amine 
• 883557-61-7 [4-(Chloro-difluoro-methoxy)-phenyl]-{5-[3-((E)-2-pyridin-4-yl-vinyl)-pyridin-4-yl]-[1,3,4]oxadiazol-2-yl}-amine 
• 883557-68-4 {5-[3-((E)-2-Pyridin-4-yl-vinyl)-pyridin-4-yl]-[1,3,4]oxadiazol-2-yl}-(3-trifluoromethoxy-phenyl)-amine 
• 883557-54-8 (4-tert-butyl-phenyl)-{5-[3-(2-pyridin-4-yl-vinyl)-pyridin-4-yl]-[1,3,4]oxadiazol-2-yl}-amine 
• 883557-55-9 (4-Isopropyl-phenyl)-{5-[3-((E)-2-pyridin-4-yl-vinyl)-pyridin-4-yl]-[1,3,4]oxadiazol-2-yl}-amine 

Relevant academic research and scientific papers

Reinvestigation of the structure-activity relationships of isoniazid

Isoniazid (INH) remains a cornerstone for treatment of drug susceptible tuberculosis (TB), yet the quantitative structure-activity relationships for INH are not well documented in the literature. In this paper, we have evaluated a systematic series of INH analogs against contemporary Mycobacterium tuberculosis strains from different lineages and a few non-tuberculous mycobacteria (NTM). Deletion of the pyridyl nitrogen atom, isomerization of the pyridine nitrogen to other positions, replacement of the pyridine ring with isosteric heterocycles, and modification of the hydrazide moiety of INH abolishes antitubercular activity. Similarly, substitution of the pyridine ring at the 3-position is not tolerated while substitution at the 2-position is permitted with 2-methyl-INH 9 displaying antimycobacterial activity comparable to INH. To assess the specific activity of this series of INH analogs against mycobacteria, we assayed them against a panel of gram-positive and gram-negative bacteria, as well as a few fungi. As expected INH and its analogs display a narrow spectrum of activity and are inactive against all non-mycobacterial strains evaluated, except for 4, which has modest inhibitory activity against Cryptococcus neoformans. Our findings provide an updated analysis of the structure-activity relationship of INH that we hope will serve as useful resource for the community.

ANTIBIOTIC COMPOUNDS

The present invention relates to antibiotic compounds of formula (I), to compositions containing these compounds and to methods of treating bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Gram-positive and/or Gram-negative bacteria, and in particular in the treatment of infection with, and diseases caused by, Neisseria gonorrhoeae.

Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl) pyridine template

We have developed a series of novel potent ((pyridin-4-yl)ethyl)pyridine derivatives active against kinases VEGFR-1 and -2. Both specific and dual ATP-competitive inhibitors of VEGFR-2 were identified. Kinase selectivity could be controlled by varying the