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Year 2018, Volume: 48 Issue: 2, 28 - 31, 31.08.2018

Abstract

References

  • Patel VR, Patel CN, Sen DJ (2011). Synthesis and Biological evaluation of some 5-[(substituted)-Phenyl]-3-(4-Chlorophenyl)-4,5-Dihydro-1H-Pyrazole-1 Carbathiomide Derivatives. Internationale Pharmaceutica Sciencia 1(1): 133-136.
  • Sarkar S, Pasha TY, Shivakumar B, Reddy VM (2008). Synthesis and Evaluation of Antibacterial and Antiinflammatory Activity of 7-Alkyl/Aryl amino-6-fluoro-2- phenyl Carboxamido-1,3-benzothiazoles. Asian J Chem 20(4): 3227-3230.
  • Sarkar S, Pasha TY, Shivakumar B, Chimkode R (2008). Synthesis of benzothiazole derivatives and study of their anti-fungal activities. Oriantal J Chem 24(2): 705-708.
  • Sarkar S, Pasha TY, Shivakumar B, Chimkode R (2008). Synthesis of new 7-alkyl /aryl amino –6-fluro 2 substituated phenyl carboxamido (1,3 ) benzothiazoles as anthelmintic agents. Indian J Heterocycl. Chem 24(7): 383-388.
  • Sarkar S (2011). Synthesis and Pharmacological evaluation of New 7 alkyl/ aryl amino-6-fluro 2- (3 nitro phenyl) Carboxamido (1,3)benzothiazole as anthelmintic agents. J Pharm Res 1(12): 4599.
  • Sarkar S, Dwivedi J, Chauhan R (2013). Synthesis and biological activity of novel azetidinone and thiazolidinone starting from benzothiazole. Ind J Heterocyclic Chem 23: 75-80.
  • Sarkar S, Dwivedi J, Chauhan R (2013). Synthesis of 1-[2 (substituted phenyl)-4-oxothiazolidin-3-yl]-3-(6-fluro-7-chloro-1,3-benzothiazol-2-yl)-ureas as anthelmintic agent. J Pharm Res 5(7): 439-442.
  • Sarkar S (2017). Synthesis and antimicrobial activity of Some azetidinone derivatives Containing Substituted Benzothiazole. Indian J Heterocycl. Chem 69(1): 46-50.

Design, synthesis, and evaluation of antitubercular activity of a novel benzothiazole-containing an azetidinone ring

Year 2018, Volume: 48 Issue: 2, 28 - 31, 31.08.2018

Abstract

Recent studies have demonstrated that
2-amino-substituted benzothiazole derivatives exhibit significant
antitubercular activity. In this study, new compounds of
benzothiazole-containing azetidinone derivatives were designed and synthesized
using substituted benzaldehydeN-(5fluoro-1,3-benzothiazol-2-yl) semicarbazone,
chloroacetyl chloride, and  triethylamine
in DMF. The structures of the synthesized compounds were characterized by TLC,
IR, elemental analysis, and 1H NMR. In vitro screening data revealed that all
the designed and synthesized compounds A6–A10 exhibited the ability to inhibit
the growth of Mycobacterium tuberculosis in terms of MIC. Variable and modest
activity was observed against the investigated strains of bacteria; however,
the compound A6 exhibited significant antitubercular activity against M.
tuberculosis H37Rv (MTCC 200) compared to that of the reference drugs isoniazid
and rifampicin. These experimental data were consistent with our computational
predictions in terms of the compound A6 that exhibited a satisfactory backbone
for the antitubercular activity, perhaps due to an increase in hydrophobicity
resulting in better penetration through the cell wall of M. tuberculosis.

References

  • Patel VR, Patel CN, Sen DJ (2011). Synthesis and Biological evaluation of some 5-[(substituted)-Phenyl]-3-(4-Chlorophenyl)-4,5-Dihydro-1H-Pyrazole-1 Carbathiomide Derivatives. Internationale Pharmaceutica Sciencia 1(1): 133-136.
  • Sarkar S, Pasha TY, Shivakumar B, Reddy VM (2008). Synthesis and Evaluation of Antibacterial and Antiinflammatory Activity of 7-Alkyl/Aryl amino-6-fluoro-2- phenyl Carboxamido-1,3-benzothiazoles. Asian J Chem 20(4): 3227-3230.
  • Sarkar S, Pasha TY, Shivakumar B, Chimkode R (2008). Synthesis of benzothiazole derivatives and study of their anti-fungal activities. Oriantal J Chem 24(2): 705-708.
  • Sarkar S, Pasha TY, Shivakumar B, Chimkode R (2008). Synthesis of new 7-alkyl /aryl amino –6-fluro 2 substituated phenyl carboxamido (1,3 ) benzothiazoles as anthelmintic agents. Indian J Heterocycl. Chem 24(7): 383-388.
  • Sarkar S (2011). Synthesis and Pharmacological evaluation of New 7 alkyl/ aryl amino-6-fluro 2- (3 nitro phenyl) Carboxamido (1,3)benzothiazole as anthelmintic agents. J Pharm Res 1(12): 4599.
  • Sarkar S, Dwivedi J, Chauhan R (2013). Synthesis and biological activity of novel azetidinone and thiazolidinone starting from benzothiazole. Ind J Heterocyclic Chem 23: 75-80.
  • Sarkar S, Dwivedi J, Chauhan R (2013). Synthesis of 1-[2 (substituted phenyl)-4-oxothiazolidin-3-yl]-3-(6-fluro-7-chloro-1,3-benzothiazol-2-yl)-ureas as anthelmintic agent. J Pharm Res 5(7): 439-442.
  • Sarkar S (2017). Synthesis and antimicrobial activity of Some azetidinone derivatives Containing Substituted Benzothiazole. Indian J Heterocycl. Chem 69(1): 46-50.
There are 8 citations in total.

Details

Primary Language English
Subjects Pharmacology and Pharmaceutical Sciences
Journal Section Original Article
Authors

Sibaji Sarkar

Publication Date August 31, 2018
Submission Date July 9, 2017
Published in Issue Year 2018 Volume: 48 Issue: 2

Cite

APA Sarkar, S. (2018). Design, synthesis, and evaluation of antitubercular activity of a novel benzothiazole-containing an azetidinone ring. İstanbul Journal of Pharmacy, 48(2), 28-31.
AMA Sarkar S. Design, synthesis, and evaluation of antitubercular activity of a novel benzothiazole-containing an azetidinone ring. iujp. August 2018;48(2):28-31.
Chicago Sarkar, Sibaji. “Design, Synthesis, and Evaluation of Antitubercular Activity of a Novel Benzothiazole-Containing an Azetidinone Ring”. İstanbul Journal of Pharmacy 48, no. 2 (August 2018): 28-31.
EndNote Sarkar S (August 1, 2018) Design, synthesis, and evaluation of antitubercular activity of a novel benzothiazole-containing an azetidinone ring. İstanbul Journal of Pharmacy 48 2 28–31.
IEEE S. Sarkar, “Design, synthesis, and evaluation of antitubercular activity of a novel benzothiazole-containing an azetidinone ring”, iujp, vol. 48, no. 2, pp. 28–31, 2018.
ISNAD Sarkar, Sibaji. “Design, Synthesis, and Evaluation of Antitubercular Activity of a Novel Benzothiazole-Containing an Azetidinone Ring”. İstanbul Journal of Pharmacy 48/2 (August 2018), 28-31.
JAMA Sarkar S. Design, synthesis, and evaluation of antitubercular activity of a novel benzothiazole-containing an azetidinone ring. iujp. 2018;48:28–31.
MLA Sarkar, Sibaji. “Design, Synthesis, and Evaluation of Antitubercular Activity of a Novel Benzothiazole-Containing an Azetidinone Ring”. İstanbul Journal of Pharmacy, vol. 48, no. 2, 2018, pp. 28-31.
Vancouver Sarkar S. Design, synthesis, and evaluation of antitubercular activity of a novel benzothiazole-containing an azetidinone ring. iujp. 2018;48(2):28-31.