Jianmei Wei - Academia.edu (original) (raw)

Papers by Jianmei Wei

Research paper thumbnail of Serendipitous synthesis of a cyclopropane-containing taxol analog via anchimeric participation of an unactivated angular methyl group

Journal of Organic Chemistry, 1993

... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett.... more ... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett. 1992, 33, 7679. ... 17, 1993 4521 C7; Le., the geometry is ideal for Clg participation. (3) Participation of a vicinal methyl group usually manifests itself in a 1,2 Wagner-Meerwein shift. ...

Research paper thumbnail of Synthesis of 7-deoxy- and 7,10-dideoxytaxol via radical intermediates

Journal of Organic Chemistry, 1993

... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,&#x... more ... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,' Stella Huang, Joydeep Kant, Craig Fairchild, Jianmei Wei, and Vittorio Farina. ... Also: GuBritte-Voegelein, F.; GuBnard, D.; Lavelle, F.; Le Goff, MT; Mangatat, L.; Potier, P. J. Med. Chem. ...

Research paper thumbnail of Serendipitous synthesis of a cyclopropane-containing taxol analog via anchimeric participation of an unactivated angular methyl group

Journal of Organic Chemistry, 1993

... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett.... more ... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett. 1992, 33, 7679. ... 17, 1993 4521 C7; Le., the geometry is ideal for Clg participation. (3) Participation of a vicinal methyl group usually manifests itself in a 1,2 Wagner-Meerwein shift. ...

Research paper thumbnail of Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors

Bioorganic & Medicinal Chemistry Letters, 2005

A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimi... more A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimized. The 4-(2-keto-1benzimidazolinyl)-piperidin-1-yl moiety was found to be an effective replacement for the 4-arylpiperazin-1-yl group found in our earlier series of CatS inhibitors. This replacement imparted improved PK properties as well as decreased off-target activity. Optimization of the ketobenzimidazole moiety led to the discovery of the lead compound JNJ 10329670, which represents a novel class of selective, noncovalent, reversible, and orally bioavailable inhibitors of cathepsin S.

Research paper thumbnail of Serendipitous synthesis of a cyclopropane-containing taxol analog via anchimeric participation of an unactivated angular methyl group

Journal of Organic Chemistry, 1993

... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett.... more ... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett. 1992, 33, 7679. ... 17, 1993 4521 C7; Le., the geometry is ideal for Clg participation. (3) Participation of a vicinal methyl group usually manifests itself in a 1,2 Wagner-Meerwein shift. ...

Research paper thumbnail of Synthesis of 7-deoxy- and 7,10-dideoxytaxol via radical intermediates

Journal of Organic Chemistry, 1993

... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,&#x... more ... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,' Stella Huang, Joydeep Kant, Craig Fairchild, Jianmei Wei, and Vittorio Farina. ... Also: GuBritte-Voegelein, F.; GuBnard, D.; Lavelle, F.; Le Goff, MT; Mangatat, L.; Potier, P. J. Med. Chem. ...

Research paper thumbnail of ChemInform Abstract: Synthesis, Utility, and X-Ray Crystal Structure of Novel Complexes of Baccatin III with Imidazole and 2Propanol

Cheminform, 2001

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Research paper thumbnail of Synthesis of 7-deoxy- and 7,10-dideoxytaxol via radical intermediates

Journal of Organic Chemistry, 1993

... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,&#x... more ... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,' Stella Huang, Joydeep Kant, Craig Fairchild, Jianmei Wei, and Vittorio Farina. ... Also: GuBritte-Voegelein, F.; GuBnard, D.; Lavelle, F.; Le Goff, MT; Mangatat, L.; Potier, P. J. Med. Chem. ...

Research paper thumbnail of Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors

Bioorganic & Medicinal Chemistry Letters, 2005

A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimi... more A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimized. The 4-(2-keto-1benzimidazolinyl)-piperidin-1-yl moiety was found to be an effective replacement for the 4-arylpiperazin-1-yl group found in our earlier series of CatS inhibitors. This replacement imparted improved PK properties as well as decreased off-target activity. Optimization of the ketobenzimidazole moiety led to the discovery of the lead compound JNJ 10329670, which represents a novel class of selective, noncovalent, reversible, and orally bioavailable inhibitors of cathepsin S.

Research paper thumbnail of An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology

Bioorganic & Medicinal Chemistry Letters, 2001

Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusi... more Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusion, BMY-27709, were examined using a parallel synthesis approach. This SAR survey led to the discovery of potent influenza inhibitory activity in a series of aromatic amides and thioamides derived from 1,3,3-trimethyl-5-hydroxycyclohexylmethylamine. Select compounds were characterized as inhibitors of the H1 subtype of influenza A viruses that act by preventing the pH-induced fusion process, thereby blocking viral entry into host cells. In a plaque-reduction assay, the most potent inhibitors displayed EC 50 values of 0.02-0.14 mg/ mL. #

Research paper thumbnail of Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors

Bioorganic & Medicinal Chemistry Letters, 2005

A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimi... more A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimized. The 4-(2-keto-1benzimidazolinyl)-piperidin-1-yl moiety was found to be an effective replacement for the 4-arylpiperazin-1-yl group found in our earlier series of CatS inhibitors. This replacement imparted improved PK properties as well as decreased off-target activity. Optimization of the ketobenzimidazole moiety led to the discovery of the lead compound JNJ 10329670, which represents a novel class of selective, noncovalent, reversible, and orally bioavailable inhibitors of cathepsin S.

Research paper thumbnail of ChemInform Abstract: Synthesis, Utility, and X-Ray Crystal Structure of Novel Complexes of Baccatin III with Imidazole and 2Propanol

Cheminform, 2001

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Research paper thumbnail of The First Potent and Selective Non-Imidazole Human Histamine H 4 Receptor Antagonists

Journal of Medicinal Chemistry, 2003

Following the discovery of the human histamine H4 receptor, a high throughput screen of our corpo... more Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.

Research paper thumbnail of ChemInform Abstract: Synthesis, Utility, and X-Ray Crystal Structure of Novel Complexes of Baccatin III with Imidazole and 2Propanol

Cheminform, 2001

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Research paper thumbnail of An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology

Bioorganic & Medicinal Chemistry Letters, 2001

Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusi... more Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusion, BMY-27709, were examined using a parallel synthesis approach. This SAR survey led to the discovery of potent influenza inhibitory activity in a series of aromatic amides and thioamides derived from 1,3,3-trimethyl-5-hydroxycyclohexylmethylamine. Select compounds were characterized as inhibitors of the H1 subtype of influenza A viruses that act by preventing the pH-induced fusion process, thereby blocking viral entry into host cells. In a plaque-reduction assay, the most potent inhibitors displayed EC 50 values of 0.02-0.14 mg/ mL. #

Research paper thumbnail of Dual binding site inhibitors of B-RAF kinase

Bioorganic & Medicinal Chemistry Letters, 2008

Computer aided modeling guided the design of a series of diarylimidazole compounds (11-22) intend... more Computer aided modeling guided the design of a series of diarylimidazole compounds (11-22) intended to interact with both the ATP and adjacent allosteric binding domains of B-RAF kinase. Their ability to inhibit the function of B-RAF kinase and intracellular ERK1/2 phosphorylation were evaluated.

Research paper thumbnail of An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology

Bioorganic & Medicinal Chemistry Letters, 2001

Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusi... more Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusion, BMY-27709, were examined using a parallel synthesis approach. This SAR survey led to the discovery of potent influenza inhibitory activity in a series of aromatic amides and thioamides derived from 1,3,3-trimethyl-5-hydroxycyclohexylmethylamine. Select compounds were characterized as inhibitors of the H1 subtype of influenza A viruses that act by preventing the pH-induced fusion process, thereby blocking viral entry into host cells. In a plaque-reduction assay, the most potent inhibitors displayed EC 50 values of 0.02-0.14 mg/ mL. #

Research paper thumbnail of The First Potent and Selective Non-Imidazole Human Histamine H 4 Receptor Antagonists

Journal of Medicinal Chemistry, 2003

Following the discovery of the human histamine H4 receptor, a high throughput screen of our corpo... more Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.

Research paper thumbnail of The First Potent and Selective Non-Imidazole Human Histamine H 4 Receptor Antagonists

Journal of Medicinal Chemistry, 2003

Following the discovery of the human histamine H4 receptor, a high throughput screen of our corpo... more Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.

Research paper thumbnail of Salicylamide inhibitors of influenza virus fusion

Bioorganic & Medicinal Chemistry Letters, 2000

AbstractÐStructural variation of the quinolizidine heterocycle of the in¯uenza fusion inhibitor B... more AbstractÐStructural variation of the quinolizidine heterocycle of the in¯uenza fusion inhibitor BMY-27709 was examined by several topological dissections in order to illuminate the critical features of the ring system. This exercise resulted in the identi®cation of a series of synthetically more accessible decahydroquinolines that retained the structural elements of BMY-27709 important for antiviral activity. The 2-methyl-cis-decahydroquinoline 6f was the most potent in¯uenza inhibitor identi®ed that demonstrated an EC 50 of 90 ng/mL in a plaque reduction assay. #

Research paper thumbnail of Serendipitous synthesis of a cyclopropane-containing taxol analog via anchimeric participation of an unactivated angular methyl group

Journal of Organic Chemistry, 1993

... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett.... more ... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett. 1992, 33, 7679. ... 17, 1993 4521 C7; Le., the geometry is ideal for Clg participation. (3) Participation of a vicinal methyl group usually manifests itself in a 1,2 Wagner-Meerwein shift. ...

Research paper thumbnail of Synthesis of 7-deoxy- and 7,10-dideoxytaxol via radical intermediates

Journal of Organic Chemistry, 1993

... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,&#x... more ... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,' Stella Huang, Joydeep Kant, Craig Fairchild, Jianmei Wei, and Vittorio Farina. ... Also: GuBritte-Voegelein, F.; GuBnard, D.; Lavelle, F.; Le Goff, MT; Mangatat, L.; Potier, P. J. Med. Chem. ...

Research paper thumbnail of Serendipitous synthesis of a cyclopropane-containing taxol analog via anchimeric participation of an unactivated angular methyl group

Journal of Organic Chemistry, 1993

... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett.... more ... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett. 1992, 33, 7679. ... 17, 1993 4521 C7; Le., the geometry is ideal for Clg participation. (3) Participation of a vicinal methyl group usually manifests itself in a 1,2 Wagner-Meerwein shift. ...

Research paper thumbnail of Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors

Bioorganic & Medicinal Chemistry Letters, 2005

A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimi... more A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimized. The 4-(2-keto-1benzimidazolinyl)-piperidin-1-yl moiety was found to be an effective replacement for the 4-arylpiperazin-1-yl group found in our earlier series of CatS inhibitors. This replacement imparted improved PK properties as well as decreased off-target activity. Optimization of the ketobenzimidazole moiety led to the discovery of the lead compound JNJ 10329670, which represents a novel class of selective, noncovalent, reversible, and orally bioavailable inhibitors of cathepsin S.

Research paper thumbnail of Serendipitous synthesis of a cyclopropane-containing taxol analog via anchimeric participation of an unactivated angular methyl group

Journal of Organic Chemistry, 1993

... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett.... more ... 1992,33.3979. Chen, S. H.; Combs, CM; Hill, S. E.; Farina, V.; Doyle, T. W. Tetrahedron Lett. 1992, 33, 7679. ... 17, 1993 4521 C7; Le., the geometry is ideal for Clg participation. (3) Participation of a vicinal methyl group usually manifests itself in a 1,2 Wagner-Meerwein shift. ...

Research paper thumbnail of Synthesis of 7-deoxy- and 7,10-dideoxytaxol via radical intermediates

Journal of Organic Chemistry, 1993

... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,&#x... more ... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,' Stella Huang, Joydeep Kant, Craig Fairchild, Jianmei Wei, and Vittorio Farina. ... Also: GuBritte-Voegelein, F.; GuBnard, D.; Lavelle, F.; Le Goff, MT; Mangatat, L.; Potier, P. J. Med. Chem. ...

Research paper thumbnail of ChemInform Abstract: Synthesis, Utility, and X-Ray Crystal Structure of Novel Complexes of Baccatin III with Imidazole and 2Propanol

Cheminform, 2001

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Research paper thumbnail of Synthesis of 7-deoxy- and 7,10-dideoxytaxol via radical intermediates

Journal of Organic Chemistry, 1993

... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,&#x... more ... Synthesis of 7-Deoxy-and 7,lO-Dideoxytaxol via Radical Intermediates Shu-Hui Chen,' Stella Huang, Joydeep Kant, Craig Fairchild, Jianmei Wei, and Vittorio Farina. ... Also: GuBritte-Voegelein, F.; GuBnard, D.; Lavelle, F.; Le Goff, MT; Mangatat, L.; Potier, P. J. Med. Chem. ...

Research paper thumbnail of Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors

Bioorganic & Medicinal Chemistry Letters, 2005

A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimi... more A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimized. The 4-(2-keto-1benzimidazolinyl)-piperidin-1-yl moiety was found to be an effective replacement for the 4-arylpiperazin-1-yl group found in our earlier series of CatS inhibitors. This replacement imparted improved PK properties as well as decreased off-target activity. Optimization of the ketobenzimidazole moiety led to the discovery of the lead compound JNJ 10329670, which represents a novel class of selective, noncovalent, reversible, and orally bioavailable inhibitors of cathepsin S.

Research paper thumbnail of An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology

Bioorganic & Medicinal Chemistry Letters, 2001

Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusi... more Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusion, BMY-27709, were examined using a parallel synthesis approach. This SAR survey led to the discovery of potent influenza inhibitory activity in a series of aromatic amides and thioamides derived from 1,3,3-trimethyl-5-hydroxycyclohexylmethylamine. Select compounds were characterized as inhibitors of the H1 subtype of influenza A viruses that act by preventing the pH-induced fusion process, thereby blocking viral entry into host cells. In a plaque-reduction assay, the most potent inhibitors displayed EC 50 values of 0.02-0.14 mg/ mL. #

Research paper thumbnail of Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors

Bioorganic & Medicinal Chemistry Letters, 2005

A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimi... more A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimized. The 4-(2-keto-1benzimidazolinyl)-piperidin-1-yl moiety was found to be an effective replacement for the 4-arylpiperazin-1-yl group found in our earlier series of CatS inhibitors. This replacement imparted improved PK properties as well as decreased off-target activity. Optimization of the ketobenzimidazole moiety led to the discovery of the lead compound JNJ 10329670, which represents a novel class of selective, noncovalent, reversible, and orally bioavailable inhibitors of cathepsin S.

Research paper thumbnail of ChemInform Abstract: Synthesis, Utility, and X-Ray Crystal Structure of Novel Complexes of Baccatin III with Imidazole and 2Propanol

Cheminform, 2001

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Research paper thumbnail of The First Potent and Selective Non-Imidazole Human Histamine H 4 Receptor Antagonists

Journal of Medicinal Chemistry, 2003

Following the discovery of the human histamine H4 receptor, a high throughput screen of our corpo... more Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.

Research paper thumbnail of ChemInform Abstract: Synthesis, Utility, and X-Ray Crystal Structure of Novel Complexes of Baccatin III with Imidazole and 2Propanol

Cheminform, 2001

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Research paper thumbnail of An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology

Bioorganic & Medicinal Chemistry Letters, 2001

Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusi... more Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusion, BMY-27709, were examined using a parallel synthesis approach. This SAR survey led to the discovery of potent influenza inhibitory activity in a series of aromatic amides and thioamides derived from 1,3,3-trimethyl-5-hydroxycyclohexylmethylamine. Select compounds were characterized as inhibitors of the H1 subtype of influenza A viruses that act by preventing the pH-induced fusion process, thereby blocking viral entry into host cells. In a plaque-reduction assay, the most potent inhibitors displayed EC 50 values of 0.02-0.14 mg/ mL. #

Research paper thumbnail of Dual binding site inhibitors of B-RAF kinase

Bioorganic & Medicinal Chemistry Letters, 2008

Computer aided modeling guided the design of a series of diarylimidazole compounds (11-22) intend... more Computer aided modeling guided the design of a series of diarylimidazole compounds (11-22) intended to interact with both the ATP and adjacent allosteric binding domains of B-RAF kinase. Their ability to inhibit the function of B-RAF kinase and intracellular ERK1/2 phosphorylation were evaluated.

Research paper thumbnail of An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology

Bioorganic & Medicinal Chemistry Letters, 2001

Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusi... more Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusion, BMY-27709, were examined using a parallel synthesis approach. This SAR survey led to the discovery of potent influenza inhibitory activity in a series of aromatic amides and thioamides derived from 1,3,3-trimethyl-5-hydroxycyclohexylmethylamine. Select compounds were characterized as inhibitors of the H1 subtype of influenza A viruses that act by preventing the pH-induced fusion process, thereby blocking viral entry into host cells. In a plaque-reduction assay, the most potent inhibitors displayed EC 50 values of 0.02-0.14 mg/ mL. #

Research paper thumbnail of The First Potent and Selective Non-Imidazole Human Histamine H 4 Receptor Antagonists

Journal of Medicinal Chemistry, 2003

Following the discovery of the human histamine H4 receptor, a high throughput screen of our corpo... more Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.

Research paper thumbnail of The First Potent and Selective Non-Imidazole Human Histamine H 4 Receptor Antagonists

Journal of Medicinal Chemistry, 2003

Following the discovery of the human histamine H4 receptor, a high throughput screen of our corpo... more Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.

Research paper thumbnail of Salicylamide inhibitors of influenza virus fusion

Bioorganic & Medicinal Chemistry Letters, 2000

AbstractÐStructural variation of the quinolizidine heterocycle of the in¯uenza fusion inhibitor B... more AbstractÐStructural variation of the quinolizidine heterocycle of the in¯uenza fusion inhibitor BMY-27709 was examined by several topological dissections in order to illuminate the critical features of the ring system. This exercise resulted in the identi®cation of a series of synthetically more accessible decahydroquinolines that retained the structural elements of BMY-27709 important for antiviral activity. The 2-methyl-cis-decahydroquinoline 6f was the most potent in¯uenza inhibitor identi®ed that demonstrated an EC 50 of 90 ng/mL in a plaque reduction assay. #