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Synthesis of some new N-(alkyl/aralkyl)-N-(2,3-dihydro-1,4-benzodioxan-6-yl)-4-chlorobenzenesulfonamides as possible therapeutic agents for Alzheimer's disease and Type-2 Diabetes.
Abbasi, Muhammad Athar; Rehman, Azizur; Siddiqui, Sabahat Zahra; Hadi, Noorul; Mumtaz, Ayesha; Shah, Syed Adnan Ali; Ashraf, Muhammad; Abbasi, Ghulam Hasan.
Afiliación
  • Abbasi MA; Department of Chemistry, Government College University, Lahore, Pakistan.
  • Rehman A; Department of Chemistry, Government College University, Lahore, Pakistan.
  • Siddiqui SZ; Department of Chemistry, Government College University, Lahore, Pakistan.
  • Hadi N; Department of Chemistry, Government College University, Lahore, Pakistan.
  • Mumtaz A; Department of Chemistry, Government College University, Lahore, Pakistan.
  • Shah SAA; Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia / Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Level 9, FF3, UniversitiTeknologi MARA, Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia.
  • Ashraf M; Department of Chemistry; 5Department of Soil Sciences, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.
  • Abbasi GH; Department of Soil Sciences, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.
Pak J Pharm Sci ; 32(1): 61-68, 2019 Jan.
Article en En | MEDLINE | ID: mdl-30772791
In the current research work, a series of new N-(alkyl/aralkyl)-N-(2,3-dihydro-1,4-benzodioxan-6-yl)-4-chlorobenzenesulfonamides has been synthesized by reacting 1,4-benzozzdioxan-6-amine (1) with 4-chlorobenzenesulfonyl chloride (2) to yield N-(2,3-dihydro-1,4-benzodioxan-6-yl)-4-chlorobenzenesulfonamide (3) which was further reacted with different alkyl/aralkyl halides (4a-n) to afford the target compounds (5a-n). Structures of the synthesized compounds were confirmed by IR, 1H-NMR, EI-MS spectral techniques and CHN analysis data. The results of enzyme inhibition showed that the molecules, N-2-phenethyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-chlorobenzenesulfonamide (5j) and N-(1-butyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-chlorobenzenesulfonamide (5d), exhibited moderate inhibitory potential against acetylcholinesterase with IC50 values 26.25±0.11 µM and 58.13±0.15 µM respectively, whereas, compounds N-benzyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-chlorobenzenesulfonamide (5i) and N-(pentane-2-yl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-chlorobenzenesulfonamide (5f) showed moderate inhibition against α-glucosidase enzyme as evident from IC50 values 74.52±0.07 and 83.52±0.08 µM respectively, relative to standards Eserine having IC50 value of 0.04±0.0001 µM for cholinesterases and Acarbose having IC50 value 38.25±0.12 µM for α-glucosidase, respectively.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Sulfonamidas / Inhibidores de la Colinesterasa / Diabetes Mellitus Tipo 2 / Enfermedad de Alzheimer / Inhibidores de Glicósido Hidrolasas Idioma: En Revista: Pak J Pharm Sci Asunto de la revista: FARMACIA / FARMACOLOGIA / QUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Pakistán Pais de publicación: Pakistán
Buscar en Google
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PubMed Links

Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Sulfonamidas / Inhibidores de la Colinesterasa / Diabetes Mellitus Tipo 2 / Enfermedad de Alzheimer / Inhibidores de Glicósido Hidrolasas Idioma: En Revista: Pak J Pharm Sci Asunto de la revista: FARMACIA / FARMACOLOGIA / QUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Pakistán Pais de publicación: Pakistán