Tag: M.W=150-200

Hintermann, Samuel published the artcileIdentification of a series of highly potent activators of the Nurr1 signaling pathway, Application In Synthesis of 100377-32-0, the publication is Bioorganic & Medicinal Chemistry Letters (2007), 17(1), 193-196, database is CAplus and MEDLINE.

The nuclear receptor Nurr1 (NR4A2) is critically involved in the development and maintenance of midbrain dopaminergic neurons and is believed to function independently of endogenous activation. The hit identification and SAR studies leading to isoxazolo-pyridinone 7e (I), a highly potent, brain penetrable activator of the Nurr1 signaling pathway, are described.

Bioorganic & Medicinal Chemistry Letters published new progress about 100377-32-0. 100377-32-0 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N-Methoxy-N-methylisonicotinamide, and the molecular formula is C8H10N2O2, Application In Synthesis of 100377-32-0.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Drsata, J. published the artcileBiological side-effects of potential antituberculotic agents. XIII. Use of serum aspartate aminotransferase for the examination of organ toxicity of thiobenzamides, Formula: C8H9NOS, the publication is Cesko-Slovenska Farmacie (1988), 37(6), 243-5, database is CAplus and MEDLINE.

Ten title compounds (I; R¹ = H, 4-Br, 3-Cl, 4-Cl, 3-Me, 4-Me, 3-MeO, 4-MeO, 4-NMe₂; R² = H, 4-Cl) were screened for hepatotoxicity as indicated by blood serum levels of aspartate aminotransferase (AST). An equation is derived relating the values of Hammett’s constants for I and log AST. The hepatotoxicity of I decreases with an increase in the value of Hammett’s constant

Cesko-Slovenska Farmacie published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, Formula: C8H9NOS.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Sledzinski, B. published the artcileStudies on the reaction of dialkyl phosphites with α-chloroacetophenones in the presence of ammonia, COA of Formula: C7H5Cl2NO, the publication is Organika (1979), 1-8, database is CAplus.

An extensive study showed that only RR¹CHCOC₆H₃Cl₂-2,4 (I; R = Br or Cl, R¹ = H, or R = R¹ = Cl) reacted with dialkyl phosphites in the presence of NH₃ to give the corresponding enol phosphates, whose importance as pesticides is steadily increasing. Under the same reaction conditions, I (R = R¹ = Br) yielded a complex mixture of at least 5 products, of which only I (R = Br, R¹ = H) and 2,4-Cl₂C₆H₃CONH₂ were identified. R₃CCOC₆H₃Cl₂-2,4 (R = Br or Cl) produced the corresponding benzamide and haloforms.

Organika published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C13H10O2, COA of Formula: C7H5Cl2NO.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Tucker, J. A. published the artcileStructure-activity relationships of acyloxyamidine cytomegalovirus DNA polymerase inhibitors, Synthetic Route of 2447-79-2, the publication is Bioorganic & Medicinal Chemistry (2000), 8(3), 601-615, database is CAplus and MEDLINE.

This paper describes the structure-activity relationships of a new class of cytomegalovirus DNA polymerase inhibitors having two aryl groups joined by an acyloxyamidine linker. Examination of a series of analogs in which the terminal groups are varied revealed a very narrow SAR around the 2,4-dichlorophenyl group of the lead compound, but a variety of replacements for the benzothiazole ring are compatible with activity. The most notable of these is the compound with isoxazole ring, which provides a 30-fold enhancement in potency compared to the lead compound We also describe the design, synthesis and evaluation of 10 analogs in which the acyloxyamidine linker is modified or replaced by an isosteric group. Structure-activity relationship studies identified the linker -NH₂group as a critical pharmacophoric element. Ab initio MO calculations combined with qual. estimates of steric interaction energies suggest that the lowest energy conformations of the acyloxyamidine linker are characterized by an extended planar C_Ar-C=N-O-C arrangement and either a syn-periplanar or anti-periplanar N-O-C-C_Ar’ arrangement. Only the anti-periplanar conformation was observed in the crystal structures of three acyloxyamidines. The most active of the linker-modified compounds designed on the basis of these studies is the amidine carbamate compound, which is approx. one-third as potent in the cytomegalovirus DNA polymerase inhibition assay as the comparator acyloxyamidine. The activity of the amidine carbamate compound suggests that acyloxyamidines may bind to the cytomegalovirus DNA polymerase via an anti-periplanar conformation.

Bioorganic & Medicinal Chemistry published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C4Br2N2O4S, Synthetic Route of 2447-79-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Czaplewski, Lloyd G. published the artcileAntibacterial alkoxybenzamide inhibitors of the essential bacterial cell division protein FtsZ, Synthetic Route of 64559-06-4, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(2), 524-527, database is CAplus and MEDLINE.

3-Methoxybenzamide is a weak inhibitor of the essential bacterial cell division protein FtsZ. Exploration of the structure-activity relationships of 3-methoxybenzamide analogs led to the identification of potent anti-staphylococcal compounds

Bioorganic & Medicinal Chemistry Letters published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, Synthetic Route of 64559-06-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Hintermann, Samuel published the artcileIdentification of a series of highly potent activators of the Nurr1 signaling pathway, Application In Synthesis of 100377-32-0, the publication is Bioorganic & Medicinal Chemistry Letters (2007), 17(1), 193-196, database is CAplus and MEDLINE.

The nuclear receptor Nurr1 (NR4A2) is critically involved in the development and maintenance of midbrain dopaminergic neurons and is believed to function independently of endogenous activation. The hit identification and SAR studies leading to isoxazolo-pyridinone 7e (I), a highly potent, brain penetrable activator of the Nurr1 signaling pathway, are described.

Bioorganic & Medicinal Chemistry Letters published new progress about 100377-32-0. 100377-32-0 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N-Methoxy-N-methylisonicotinamide, and the molecular formula is C8H10N2O2, Application In Synthesis of 100377-32-0.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Drsata, J. published the artcileBiological side-effects of potential antituberculotic agents. XIII. Use of serum aspartate aminotransferase for the examination of organ toxicity of thiobenzamides, Formula: C8H9NOS, the publication is Cesko-Slovenska Farmacie (1988), 37(6), 243-5, database is CAplus and MEDLINE.

Ten title compounds (I; R¹ = H, 4-Br, 3-Cl, 4-Cl, 3-Me, 4-Me, 3-MeO, 4-MeO, 4-NMe₂; R² = H, 4-Cl) were screened for hepatotoxicity as indicated by blood serum levels of aspartate aminotransferase (AST). An equation is derived relating the values of Hammett’s constants for I and log AST. The hepatotoxicity of I decreases with an increase in the value of Hammett’s constant

Cesko-Slovenska Farmacie published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, Formula: C8H9NOS.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Sledzinski, B. published the artcileStudies on the reaction of dialkyl phosphites with α-chloroacetophenones in the presence of ammonia, COA of Formula: C7H5Cl2NO, the publication is Organika (1979), 1-8, database is CAplus.

An extensive study showed that only RR¹CHCOC₆H₃Cl₂-2,4 (I; R = Br or Cl, R¹ = H, or R = R¹ = Cl) reacted with dialkyl phosphites in the presence of NH₃ to give the corresponding enol phosphates, whose importance as pesticides is steadily increasing. Under the same reaction conditions, I (R = R¹ = Br) yielded a complex mixture of at least 5 products, of which only I (R = Br, R¹ = H) and 2,4-Cl₂C₆H₃CONH₂ were identified. R₃CCOC₆H₃Cl₂-2,4 (R = Br or Cl) produced the corresponding benzamide and haloforms.

Organika published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C13H10O2, COA of Formula: C7H5Cl2NO.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Tucker, J. A. published the artcileStructure-activity relationships of acyloxyamidine cytomegalovirus DNA polymerase inhibitors, Synthetic Route of 2447-79-2, the publication is Bioorganic & Medicinal Chemistry (2000), 8(3), 601-615, database is CAplus and MEDLINE.

This paper describes the structure-activity relationships of a new class of cytomegalovirus DNA polymerase inhibitors having two aryl groups joined by an acyloxyamidine linker. Examination of a series of analogs in which the terminal groups are varied revealed a very narrow SAR around the 2,4-dichlorophenyl group of the lead compound, but a variety of replacements for the benzothiazole ring are compatible with activity. The most notable of these is the compound with isoxazole ring, which provides a 30-fold enhancement in potency compared to the lead compound We also describe the design, synthesis and evaluation of 10 analogs in which the acyloxyamidine linker is modified or replaced by an isosteric group. Structure-activity relationship studies identified the linker -NH₂group as a critical pharmacophoric element. Ab initio MO calculations combined with qual. estimates of steric interaction energies suggest that the lowest energy conformations of the acyloxyamidine linker are characterized by an extended planar C_Ar-C=N-O-C arrangement and either a syn-periplanar or anti-periplanar N-O-C-C_Ar’ arrangement. Only the anti-periplanar conformation was observed in the crystal structures of three acyloxyamidines. The most active of the linker-modified compounds designed on the basis of these studies is the amidine carbamate compound, which is approx. one-third as potent in the cytomegalovirus DNA polymerase inhibition assay as the comparator acyloxyamidine. The activity of the amidine carbamate compound suggests that acyloxyamidines may bind to the cytomegalovirus DNA polymerase via an anti-periplanar conformation.

Bioorganic & Medicinal Chemistry published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C4Br2N2O4S, Synthetic Route of 2447-79-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Czaplewski, Lloyd G. published the artcileAntibacterial alkoxybenzamide inhibitors of the essential bacterial cell division protein FtsZ, Synthetic Route of 64559-06-4, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(2), 524-527, database is CAplus and MEDLINE.

3-Methoxybenzamide is a weak inhibitor of the essential bacterial cell division protein FtsZ. Exploration of the structure-activity relationships of 3-methoxybenzamide analogs led to the identification of potent anti-staphylococcal compounds

Bioorganic & Medicinal Chemistry Letters published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, Synthetic Route of 64559-06-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics