Avinash Tiwari

Publications (8) View all

• Article: Synthesis and biological evaluation of a novel series of aryl S,N-ketene acetals as antileishmanial agents.

  S N Suryawanshi, Santosh Kumar, Avinash Tiwari, Rahul Shivahare, Yashpal Singh Chhonker, Susmita Pandey, Nishi Shakya, Rabi Sankar Bhatta, Suman Gupta
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  ABSTRACT: A series of aryl S,N-ketene acetals 7(a-f) was synthesized and evaluated for their in vitro and in vivo antileishmanial activity against Leishmania donovani. All the 6 compounds exhibited significant in vitro activity against intracellular amastigotes of L. donovani with IC50 values ranging from 1.2 to 3.5μM and were found promising as compared with reference drugs, sodium stibogluconate (SSG) and paromomycin. On the basis of good selectivity indices (SI), they were further tested for their in vivo potential against L. donovani/hamster model. Two compounds 7a and 7b showed significant inhibition of parasite multiplication, 72% and 83%, respectively. These compounds were comparable with SSG and superior to paromomycin. Preliminary in vitro metabolic investigations were also performed to assess the metabolic stability and in vitro hepatic intrinsic clearance (Clint) of compound 7b in hamster liver microsomes.
  Bioorganic & medicinal chemistry letters 04/2013; · 2.65 Impact Factor
• Source

  Available from: Rahul Shivhare

  Article: Chemotherapy of leishmaniasis. Part XII: Design, synthesis and bioevaluation of novel triazole integrated phenyl heteroterpenoids as antileishmanial agents.

  S N Suryawanshi, Avinash Tiwari, Santosh Kumar, Rahul Shivahare, Monika Mittal, Padam Kant, Suman Gupta
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  ABSTRACT: A novel series of triazole integrated phenyl heteroterpenoids have been synthesized and screened for their in vitro activity against intracellular amastigote form of Leishmania donovani. Among all tested compounds, compound 3a was found to be the most active with IC50 6.4μM and better selectivity index (SI) 18 as compared to reference drugs, miltefosine and miconazole. When evaluated in vivo in L. donovani/hamster model, 3a has exhibited 79±11% inhibition of parasite multiplication at 50mgkg(-1)×5days on day 7 post treatment.
  Bioorganic & medicinal chemistry letters 03/2013; · 2.65 Impact Factor
• Conference Proceeding: Novel retinoic acid prototype and bisenzylidine ketone hybrids as antileishmanial agents.

  Avinash Tiwari, S.N. Suryawanshi, Rahul Shivahare, Suman Gupta
  5th CDRI-NIPER (RBL) Symposium on Chemical and Biological Approaches in Drug Development & Delivery Strategies, CSIR-Central Drug Research Institute, Lucknow; 03/2013
• Conference Proceeding: Design, synthesis and biological evaluation of chalcone based pyrimidine derivatives as potential leishmanicidal agents

  Santosh Kumar, S. N. Suryawanshi, Avinash Tiwari, Rahul Shivahare, Susmita Pandey, Suman Gupta
  5th International symposium on Drug Development for Orphan-Neglected Diseases (CTDDR-2013), CSIR-Central Drug Research Institute, Lucknow; 02/2013
• Article: Chemotherapy of leishmaniasis part X: Synthesis and bioevaluation of novel terpenyl heterocycles.

  Avinash Tiwari, Santosh Kumar, S N Suryawanshi, Monika Mittal, Preeti Vishwakarma, Suman Gupta
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  ABSTRACT: Some novel α and β ionone based chalcones and their dihydropyrazolidines/pyrazolidines have been synthesized and evaluated for their in vitro and in vivo antileishmanial activities against Leishmania donovani. Amongest all, one compound (4d) exhibited significant in vitro activity against intracellular amastigotes of Leishmania donovani with IC(50) values of 7.49μM and was found promising as compared to reference drug, miltefosine. On the basis of good Selectivity Index (S.I.), the compound was further tested for its in vivo response against Leishmania donovani/hamster model and has shown significant inhibition of parasite multiplication (81%). The present study has helped us in identifying a new lead that could be exploited as a potential antileishmanial agent.
  Bioorganic & medicinal chemistry letters 11/2012; · 2.65 Impact Factor