Design and synthesis of novel 2- substituted benzothiazole compounds as PTP1B inhibitors

Arun P. Chandrasekharappa; Sangamesh E. Badiger; Pramod K. Dubey; Sunil K. Panigrahi; Sekhar Reddy V.V.V. Manukonda

doi:10.2174/15701808113106660076

Design and synthesis of novel 2- substituted benzothiazole compounds as PTP1B inhibitors

Arun P. Chandrasekharappa, Sangamesh E. Badiger, Pramod K. Dubey, Sunil K. Panigrahi, Sekhar Reddy V.V.V. Manukonda

Research output: Contribution to journal › Article › peer-review

6 Scopus citations

Abstract

Protein tyrosine phosphatase 1B (PTP1B) is a well known drug target for the treatment of type 2 diabetes mellitus (T2DM). Diverse inhibitors have been reported in literature that inhibit PTP1B. We have reported 2-substituted benzoxazole class of In PTP1B inhibitors earlier. Present work describes 2-substituted benzothiazole compounds as PTP1B inhibitor as an extension of our previous study. Compound 23c, a disubstituted para-Bromobenzyl sulfonamide compound, exhibited moderate biochemical potency (Ki) of 1.4 μM. SAR on synthesized compounds was explained using molecular modeling study.

Original language	English (US)
Pages (from-to)	444-453
Number of pages	10
Journal	Letters in Drug Design and Discovery
Volume	11
Issue number	4
DOIs	https://doi.org/10.2174/15701808113106660076
State	Published - May 2014
Externally published	Yes

Keywords

Benzothiazoles
Disubstituted sulfonamides
Oxamic acids
PTP1B
PTyr mimetics
Type 2 Diabetes

ASJC Scopus subject areas

Molecular Medicine
Pharmaceutical Science
Drug Discovery

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10.2174/15701808113106660076

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title = "Design and synthesis of novel 2- substituted benzothiazole compounds as PTP1B inhibitors",

abstract = "Protein tyrosine phosphatase 1B (PTP1B) is a well known drug target for the treatment of type 2 diabetes mellitus (T2DM). Diverse inhibitors have been reported in literature that inhibit PTP1B. We have reported 2-substituted benzoxazole class of In PTP1B inhibitors earlier. Present work describes 2-substituted benzothiazole compounds as PTP1B inhibitor as an extension of our previous study. Compound 23c, a disubstituted para-Bromobenzyl sulfonamide compound, exhibited moderate biochemical potency (Ki) of 1.4 μM. SAR on synthesized compounds was explained using molecular modeling study.",

keywords = "Benzothiazoles, Disubstituted sulfonamides, Oxamic acids, PTP1B, PTyr mimetics, Type 2 Diabetes",

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T1 - Design and synthesis of novel 2- substituted benzothiazole compounds as PTP1B inhibitors

AU - Chandrasekharappa, Arun P.

AU - Badiger, Sangamesh E.

AU - Dubey, Pramod K.

AU - Panigrahi, Sunil K.

AU - Manukonda, Sekhar Reddy V.V.V.

PY - 2014/5

Y1 - 2014/5

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AB - Protein tyrosine phosphatase 1B (PTP1B) is a well known drug target for the treatment of type 2 diabetes mellitus (T2DM). Diverse inhibitors have been reported in literature that inhibit PTP1B. We have reported 2-substituted benzoxazole class of In PTP1B inhibitors earlier. Present work describes 2-substituted benzothiazole compounds as PTP1B inhibitor as an extension of our previous study. Compound 23c, a disubstituted para-Bromobenzyl sulfonamide compound, exhibited moderate biochemical potency (Ki) of 1.4 μM. SAR on synthesized compounds was explained using molecular modeling study.

KW - Benzothiazoles

KW - Disubstituted sulfonamides

KW - Oxamic acids

KW - PTP1B

KW - PTyr mimetics

KW - Type 2 Diabetes

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Design and synthesis of novel 2- substituted benzothiazole compounds as PTP1B inhibitors

Abstract

Keywords

ASJC Scopus subject areas

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