Category: 438630-64-9

Category: alcohols-buliding-blocks. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 1H-Pyrazole-4-sulfonyl chloride, is researched, Molecular C3H3ClN2O2S, CAS is 438630-64-9, about Potent and Selective Nonpeptidic Inhibitors of Procollagen C-Proteinase.

6-Cyclohexyl-N-hydroxy-3-(1,2,4-oxadiazol-5-yl)hexanamides were previously disclosed as inhibitors of procollagen C-proteinase (PCP) culminating in the identification of amide 1. The objective was to discover a second inhibitor that would have improved affinity for PCP and to optimize properties for transepidermal delivery (TED) to intact skin. Further investigation of this template identified a number of potent PCP inhibitors (IC50 values of 2-6 nM) with improved TED flux. Sulfonamide (I) had excellent PCP enzyme activity when measured with a peptide substrate (Ki 8.7 nM) or with the endogenous substrate procollagen (IC50 3.4 nM) and demonstrates excellent selectivity over MMPs involved in wound healing (>10 000-fold). In the fibroplasia model, I inhibited deposition of insoluble collagen by 76±2% at 10 μM and was very effective at penetrating human skin in vitro with a TED flux of 1.5 μg/cm2/h, which compares favorably with values for agents that are known to penetrate skin well in vivo. Based on this profile, I (UK-421,045) was selected as a candidate for further preclin. evaluation as a topically applied, dermal antiscarring agent.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling, published in 2016-05-15, which mentions a compound: 438630-64-9, Name is 1H-Pyrazole-4-sulfonyl chloride, Molecular C3H3ClN2O2S, COA of Formula: C3H3ClN2O2S.

One of the challenges for targeting B-RafV600E with small mol. inhibitors had been achieving adequate selectivity over the wild-type protein B-RafWT, as inhibition of the latter has been associated with hyperplasia in normal tissues. Recent studies suggest that B-Raf inhibitors inducing the ‘DFG-in/αC-helix-out’ conformation (Type IIB) likely will exhibit improved selectivity for B-RafV600E. To explore this hypothesis, we transformed Type IIA inhibitor (1) into a series of Type IIB inhibitors (sulfonamides and sulfamides 4-6) and examined the SAR. Three selectivity indexes were introduced to facilitate the analyses: the B-RafV600E/B-RafWT biochem. (bS), cellular (cS) selectivity, and the phospho-ERK activation (pA). Our data indicates that α-branched sulfonamides and sulfamides show higher selectivities than the linear derivatives We rationalized this finding based on anal. of structural information from the literature and provided evidence for a monomeric B-Raf-inhibitor complex previously hypothesized to be responsible for the desired B-RafV600E selectivity.

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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 438630-64-9, is researched, SMILESS is ClS(=O)(=O)C1=CNN=C1, Molecular C3H3ClN2O2SJournal, Article, Journal of Medicinal Chemistry called Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist, Author is Hunt, Hazel J.; Belanoff, Joseph K.; Walters, Iain; Gourdet, Benoit; Thomas, Jennifer; Barton, Naomi; Unitt, John; Phillips, Timothy; Swift, Denise; Eaton, Emily, the main research direction is glucocorticoid receptor antagonist CORT125134 preparation Cushing’s.Electric Literature of C3H3ClN2O2S.

The nonselective glucocorticoid receptor (GR) antagonist mifepristone has been approved in the U.S. for the treatment of selected patients with Cushing’s syndrome. While this drug is highly effective, lack of selectivity for GR leads to unwanted side effects in some patients. Optimization of the previously described fused azadecalin series of selective GR antagonists led to the identification of CORT125134, which is currently being evaluated in a phase 2 clin. study in patients with Cushing’s syndrome.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Potent and Selective Nonpeptidic Inhibitors of Procollagen C-Proteinase, published in 2007-07-26, which mentions a compound: 438630-64-9, Name is 1H-Pyrazole-4-sulfonyl chloride, Molecular C3H3ClN2O2S, Computed Properties of C3H3ClN2O2S.

6-Cyclohexyl-N-hydroxy-3-(1,2,4-oxadiazol-5-yl)hexanamides were previously disclosed as inhibitors of procollagen C-proteinase (PCP) culminating in the identification of amide 1. The objective was to discover a second inhibitor that would have improved affinity for PCP and to optimize properties for transepidermal delivery (TED) to intact skin. Further investigation of this template identified a number of potent PCP inhibitors (IC50 values of 2-6 nM) with improved TED flux. Sulfonamide (I) had excellent PCP enzyme activity when measured with a peptide substrate (Ki 8.7 nM) or with the endogenous substrate procollagen (IC50 3.4 nM) and demonstrates excellent selectivity over MMPs involved in wound healing (>10 000-fold). In the fibroplasia model, I inhibited deposition of insoluble collagen by 76±2% at 10 μM and was very effective at penetrating human skin in vitro with a TED flux of 1.5 μg/cm2/h, which compares favorably with values for agents that are known to penetrate skin well in vivo. Based on this profile, I (UK-421,045) was selected as a candidate for further preclin. evaluation as a topically applied, dermal antiscarring agent.

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Reference of 1H-Pyrazole-4-sulfonyl chloride. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 1H-Pyrazole-4-sulfonyl chloride, is researched, Molecular C3H3ClN2O2S, CAS is 438630-64-9, about Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling. Author is Liu, Longbin; Lee, Matthew R.; Kim, Joseph L.; Whittington, Douglas A.; Bregman, Howard; Hua, Zihao; Lewis, Richard T.; Martin, Matthew W.; Nishimura, Nobuko; Potashman, Michele; Yang, Kevin; Yi, Shuyan; Vaida, Karina R.; Epstein, Linda F.; Babij, Carol; Fernando, Manory; Carnahan, Josette; Norman, Mark H..

One of the challenges for targeting B-RafV600E with small mol. inhibitors had been achieving adequate selectivity over the wild-type protein B-RafWT, as inhibition of the latter has been associated with hyperplasia in normal tissues. Recent studies suggest that B-Raf inhibitors inducing the ‘DFG-in/αC-helix-out’ conformation (Type IIB) likely will exhibit improved selectivity for B-RafV600E. To explore this hypothesis, we transformed Type IIA inhibitor (1) into a series of Type IIB inhibitors (sulfonamides and sulfamides 4-6) and examined the SAR. Three selectivity indexes were introduced to facilitate the analyses: the B-RafV600E/B-RafWT biochem. (bS), cellular (cS) selectivity, and the phospho-ERK activation (pA). Our data indicates that α-branched sulfonamides and sulfamides show higher selectivities than the linear derivatives We rationalized this finding based on anal. of structural information from the literature and provided evidence for a monomeric B-Raf-inhibitor complex previously hypothesized to be responsible for the desired B-RafV600E selectivity.

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Formula: C3H3ClN2O2S. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 1H-Pyrazole-4-sulfonyl chloride, is researched, Molecular C3H3ClN2O2S, CAS is 438630-64-9, about Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist. Author is Hunt, Hazel J.; Belanoff, Joseph K.; Walters, Iain; Gourdet, Benoit; Thomas, Jennifer; Barton, Naomi; Unitt, John; Phillips, Timothy; Swift, Denise; Eaton, Emily.

The nonselective glucocorticoid receptor (GR) antagonist mifepristone has been approved in the U.S. for the treatment of selected patients with Cushing’s syndrome. While this drug is highly effective, lack of selectivity for GR leads to unwanted side effects in some patients. Optimization of the previously described fused azadecalin series of selective GR antagonists led to the identification of CORT125134, which is currently being evaluated in a phase 2 clin. study in patients with Cushing’s syndrome.

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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 438630-64-9, is researched, SMILESS is ClS(=O)(=O)C1=CNN=C1, Molecular C3H3ClN2O2SJournal, Organic Chemistry Frontiers called A robust and facile method for desulfonation to amines, Author is Li, Chen; Huang, Yilei; Cao, Sheng; Luo, Yunhao; Zhang, Ying; Yang, Guang, the main research direction is amine preparation; aromatic aliphatic sulfonamide desulfonation.Product Details of 438630-64-9.

In this study, a robust and facile method for desulfonation to achieve secondary amines is demonstrated. Diphenylphosphine (Ph2PH) was shown to significantly expedite the cleavage of sulfonamides under basic conditions. Aromatic and aliphatic sulfonamides were cleanly converted, with a rapid reaction time, into the required amines with good to excellent chem. yields. Moreover, the functional groups tested were generally well tolerated.

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COA of Formula: C3H3ClN2O2S. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 1H-Pyrazole-4-sulfonyl chloride, is researched, Molecular C3H3ClN2O2S, CAS is 438630-64-9, about A robust and facile method for desulfonation to amines. Author is Li, Chen; Huang, Yilei; Cao, Sheng; Luo, Yunhao; Zhang, Ying; Yang, Guang.

In this study, a robust and facile method for desulfonation to achieve secondary amines is demonstrated. Diphenylphosphine (Ph2PH) was shown to significantly expedite the cleavage of sulfonamides under basic conditions. Aromatic and aliphatic sulfonamides were cleanly converted, with a rapid reaction time, into the required amines with good to excellent chem. yields. Moreover, the functional groups tested were generally well tolerated.

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Product Details of 438630-64-9. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 1H-Pyrazole-4-sulfonyl chloride, is researched, Molecular C3H3ClN2O2S, CAS is 438630-64-9, about A robust and facile method for desulfonation to amines. Author is Li, Chen; Huang, Yilei; Cao, Sheng; Luo, Yunhao; Zhang, Ying; Yang, Guang.

In this study, a robust and facile method for desulfonation to achieve secondary amines is demonstrated. Diphenylphosphine (Ph2PH) was shown to significantly expedite the cleavage of sulfonamides under basic conditions. Aromatic and aliphatic sulfonamides were cleanly converted, with a rapid reaction time, into the required amines with good to excellent chem. yields. Moreover, the functional groups tested were generally well tolerated.

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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Hunt, Hazel J.; Belanoff, Joseph K.; Walters, Iain; Gourdet, Benoit; Thomas, Jennifer; Barton, Naomi; Unitt, John; Phillips, Timothy; Swift, Denise; Eaton, Emily researched the compound: 1H-Pyrazole-4-sulfonyl chloride( cas:438630-64-9 ).Product Details of 438630-64-9.They published the article 《Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist》 about this compound( cas:438630-64-9 ) in Journal of Medicinal Chemistry. Keywords: glucocorticoid receptor antagonist CORT125134 preparation Cushing’s. We’ll tell you more about this compound (cas:438630-64-9).

The nonselective glucocorticoid receptor (GR) antagonist mifepristone has been approved in the U.S. for the treatment of selected patients with Cushing’s syndrome. While this drug is highly effective, lack of selectivity for GR leads to unwanted side effects in some patients. Optimization of the previously described fused azadecalin series of selective GR antagonists led to the identification of CORT125134, which is currently being evaluated in a phase 2 clin. study in patients with Cushing’s syndrome.

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