38239-45-1 Archives - Bromides-buliding-blocks

Cao, Xufeng et al. published their research in European Journal of Medicinal Chemistry in 2015 | CAS: 38239-45-1

5-Bromo-3-methylthiophene-2-carboxylic acid (cas: 38239-45-1) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Product Details of 38239-45-1

Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates was written by Cao, Xufeng;Xu, Yuanyuan;Cao, Yongbing;Wang, Ruilian;Zhou, Ran;Chu, Wenjing;Yang, Yushe. And the article was included in European Journal of Medicinal Chemistry in 2015.Product Details of 38239-45-1 This article mentions the following:

In order to further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compounds, two series of novel azoles I [ R¹ = Ph, 4-pyridyl, 2-CN-5-pyridyl, etc.]and II [R¹ = Ph, 4-Me-C₆H₄, 4-F-C₆H₄, etc.], featuring thieno[2,3-c]pyrrolidone and thieno[3,2-c]pyrrolidone nuclei were designed and evaluated for their in vitro activity on the basis of the binding mode of albaconazole using mol. docking, along with SARs of antifungal triazoles. Most of target compounds exhibited excellent activity against Candida and Cryptococcus spp., with MIC values in the range of 0.0625 婵炴挾鎸?mL to 0.0156 婵炴挾鎸?mL. The thieno[3,2-c]pyrrolidone unit was more suited for improving activity against Aspergillus spp. The most potent compound, II [R¹ = Br], was selected for further development due to its significant in vitro activity against Aspergillus spp. (MIC = 0.25 婵炴挾鎸?mL), as well as its high metabolic stability in human liver microsomes. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-methylthiophene-2-carboxylic acid (cas: 38239-45-1Product Details of 38239-45-1).

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Varney, Michael D. et al. published their research in Journal of Medicinal Chemistry in 1997 | CAS: 38239-45-1

5-Bromo-3-methylthiophene-2-carboxylic acid (cas: 38239-45-1) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Product Details of 38239-45-1

Protein Structure-Based Design, Synthesis, and Biological Evaluation of 5-Thia-2,6-diamino-4(3H)-oxopyrimidines: Potent Inhibitors of Glycinamide Ribonucleotide Transformylase with Potent Cell Growth Inhibition was written by Varney, Michael D.;Palmer, Cindy L.;Romines, William H. III;Boritzki, Theodore;Margosiak, Stephen A.;Almassy, Robert;Janson, Cheryl A.;Bartlett, Charlotte;Howland, Eleanor J.;Ferre, Rosanne. And the article was included in Journal of Medicinal Chemistry in 1997.Product Details of 38239-45-1 This article mentions the following:

The design, synthesis, biochem., and biol. evaluation of a novel series of 5-thia-2,6-diamino-4(3H)-oxopyrimidine inhibitors of glycinamide ribonucleotide transformylase (GART) are described. The compounds were designed using the X-ray crystal structure of human GART. The monocyclic 5-thiapyrimidinones were synthesized by coupling an alkyl thiol with 5-bromo-2,6-diamino-4(3H)-pyrimidinone. The bicyclic compounds were prepared in both racemic and diastereomerically pure forms using two distinct synthetic routes. The compounds were found to have human GART K_is ranging from 30 婵炴挾鎷?to 2 nM. The compounds inhibited the growth of both L1210 and CCRF-CEM cells in culture with potencies down to the low nanomolar range and were found to be selective for the de novo purine biosynthesis pathway. The most potent inhibitors had 2,5-disubstituted thiophene rings attached to the glutamate moiety. Placement of a Me substituent at the 4-position of the thiophene ring resulted in inhibitors with significantly decreased mFBP (human folate-binding protein) affinity. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-methylthiophene-2-carboxylic acid (cas: 38239-45-1Product Details of 38239-45-1).

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Cao, Xufeng et al. published their research in European Journal of Medicinal Chemistry in 2015 | CAS: 38239-45-1

In order to further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compounds, two series of novel azoles I [ R¹ = Ph, 4-pyridyl, 2-CN-5-pyridyl, etc.]and II [R¹ = Ph, 4-Me-C₆H₄, 4-F-C₆H₄, etc.], featuring thieno[2,3-c]pyrrolidone and thieno[3,2-c]pyrrolidone nuclei were designed and evaluated for their in vitro activity on the basis of the binding mode of albaconazole using mol. docking, along with SARs of antifungal triazoles. Most of target compounds exhibited excellent activity against Candida and Cryptococcus spp., with MIC values in the range of 0.0625 娓璯/mL to 0.0156 娓璯/mL. The thieno[3,2-c]pyrrolidone unit was more suited for improving activity against Aspergillus spp. The most potent compound, II [R¹ = Br], was selected for further development due to its significant in vitro activity against Aspergillus spp. (MIC = 0.25 娓璯/mL), as well as its high metabolic stability in human liver microsomes. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-methylthiophene-2-carboxylic acid (cas: 38239-45-1Product Details of 38239-45-1).

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Varney, Michael D. et al. published their research in Journal of Medicinal Chemistry in 1997 | CAS: 38239-45-1

The design, synthesis, biochem., and biol. evaluation of a novel series of 5-thia-2,6-diamino-4(3H)-oxopyrimidine inhibitors of glycinamide ribonucleotide transformylase (GART) are described. The compounds were designed using the X-ray crystal structure of human GART. The monocyclic 5-thiapyrimidinones were synthesized by coupling an alkyl thiol with 5-bromo-2,6-diamino-4(3H)-pyrimidinone. The bicyclic compounds were prepared in both racemic and diastereomerically pure forms using two distinct synthetic routes. The compounds were found to have human GART K_is ranging from 30 娓璏 to 2 nM. The compounds inhibited the growth of both L1210 and CCRF-CEM cells in culture with potencies down to the low nanomolar range and were found to be selective for the de novo purine biosynthesis pathway. The most potent inhibitors had 2,5-disubstituted thiophene rings attached to the glutamate moiety. Placement of a Me substituent at the 4-position of the thiophene ring resulted in inhibitors with significantly decreased mFBP (human folate-binding protein) affinity. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-methylthiophene-2-carboxylic acid (cas: 38239-45-1Product Details of 38239-45-1).

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Varney, Michael D. et al. published their research in Journal of Medicinal Chemistry in 1997 | CAS: 38239-45-1

The design, synthesis, biochem., and biol. evaluation of a novel series of 5-thia-2,6-diamino-4(3H)-oxopyrimidine inhibitors of glycinamide ribonucleotide transformylase (GART) are described. The compounds were designed using the X-ray crystal structure of human GART. The monocyclic 5-thiapyrimidinones were synthesized by coupling an alkyl thiol with 5-bromo-2,6-diamino-4(3H)-pyrimidinone. The bicyclic compounds were prepared in both racemic and diastereomerically pure forms using two distinct synthetic routes. The compounds were found to have human GART K_is ranging from 30 渭M to 2 nM. The compounds inhibited the growth of both L1210 and CCRF-CEM cells in culture with potencies down to the low nanomolar range and were found to be selective for the de novo purine biosynthesis pathway. The most potent inhibitors had 2,5-disubstituted thiophene rings attached to the glutamate moiety. Placement of a Me substituent at the 4-position of the thiophene ring resulted in inhibitors with significantly decreased mFBP (human folate-binding protein) affinity. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-methylthiophene-2-carboxylic acid (cas: 38239-45-1Product Details of 38239-45-1).

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Cao, Xufeng et al. published their research in European Journal of Medicinal Chemistry in 2015 | CAS: 38239-45-1

In order to further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compounds, two series of novel azoles I [ R¹ = Ph, 4-pyridyl, 2-CN-5-pyridyl, etc.]and II [R¹ = Ph, 4-Me-C₆H₄, 4-F-C₆H₄, etc.], featuring thieno[2,3-c]pyrrolidone and thieno[3,2-c]pyrrolidone nuclei were designed and evaluated for their in vitro activity on the basis of the binding mode of albaconazole using mol. docking, along with SARs of antifungal triazoles. Most of target compounds exhibited excellent activity against Candida and Cryptococcus spp., with MIC values in the range of 0.0625 μg/mL to 0.0156 μg/mL. The thieno[3,2-c]pyrrolidone unit was more suited for improving activity against Aspergillus spp. The most potent compound, II [R¹ = Br], was selected for further development due to its significant in vitro activity against Aspergillus spp. (MIC = 0.25 μg/mL), as well as its high metabolic stability in human liver microsomes. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-methylthiophene-2-carboxylic acid (cas: 38239-45-1Product Details of 38239-45-1).

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Varney, Michael D. et al. published their research in Journal of Medicinal Chemistry in 1997 | CAS: 38239-45-1

The design, synthesis, biochem., and biol. evaluation of a novel series of 5-thia-2,6-diamino-4(3H)-oxopyrimidine inhibitors of glycinamide ribonucleotide transformylase (GART) are described. The compounds were designed using the X-ray crystal structure of human GART. The monocyclic 5-thiapyrimidinones were synthesized by coupling an alkyl thiol with 5-bromo-2,6-diamino-4(3H)-pyrimidinone. The bicyclic compounds were prepared in both racemic and diastereomerically pure forms using two distinct synthetic routes. The compounds were found to have human GART K_is ranging from 30 μM to 2 nM. The compounds inhibited the growth of both L1210 and CCRF-CEM cells in culture with potencies down to the low nanomolar range and were found to be selective for the de novo purine biosynthesis pathway. The most potent inhibitors had 2,5-disubstituted thiophene rings attached to the glutamate moiety. Placement of a Me substituent at the 4-position of the thiophene ring resulted in inhibitors with significantly decreased mFBP (human folate-binding protein) affinity. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-methylthiophene-2-carboxylic acid (cas: 38239-45-1Product Details of 38239-45-1).

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary