Author(s): Jayalakshmi P M, Sheeba Jasmin TS, Manu Jose


DOI: 10.52711/0974-360X.2021.00923   

Address: Jayalakshmi P M1*, Dr. Sheeba Jasmin TS1, Mr Manu Jose2
1College of Pharmaceutical Sciences, Government Medical College, Thiruvananthapuram, Kerala, India.
2Nirmala College of Pharmacy, Muvattupuzha, Kerala, India.
*Corresponding Author

Published In:   Volume - 14,      Issue - 10,     Year - 2021

1,3,4-Thiadiazole is an important heterocyclic moiety, forms an integral core structural component of different categories of drugs such as antimicrobial, antitubercular, anti-inflammatory, antiepileptic, antiviral, antineoplastics, and analgesic agents. It is a key moiety in current discovery and designing of new drugs. The compounds were synthesised by both conventional method and microwave method. The targeted derivatives can be synthesised in a shorter time under microwave condition than under conventional reaction condition. Their structures were confirmed by FT-IR and NMR Spectroscopy. Antibacterial property of two synthesised analogs were evaluated by Agar well diffusion method against Escherichia coli and Staphylococcus aureus. The results of antibacterial activity showed that both the compounds were active against Staphylococcus aureus and inactive against Escherichia coli. Results of invitro studies showed that modifications in SB-2-PHB and SB-8-PHB will make it as a promising lead molecule for further research.

Cite this article:
Jayalakshmi P M, Sheeba Jasmin TS, Manu Jose. Microwave Assisted Synthesis and Antibacterial Evaluation of 1, 3, 4-Thiadiazole Derivatives. Research Journal of Pharmacy and Technology. 2021; 14(10):5293-6. doi: 10.52711/0974-360X.2021.00923

Jayalakshmi P M, Sheeba Jasmin TS, Manu Jose. Microwave Assisted Synthesis and Antibacterial Evaluation of 1, 3, 4-Thiadiazole Derivatives. Research Journal of Pharmacy and Technology. 2021; 14(10):5293-6. doi: 10.52711/0974-360X.2021.00923   Available on:

1.    Schillaci D, Spano V, Parrino B, Carbone A, Montalbano A, Barraja P, Diana P, Cirrincione G, Cascioferro S. Pharmaceutical Approaches to Target Antibiotic Resistance Mechanisms. J Med Chem. 2017; 60(20): 8268-8297
2.    Sandeep K. Chitale, B. Ramesh, Chetan M. Bhalgat, Jaishree V., Puttaraj C,
D.R. Bharathi. Synthesis and Antioxidant Screening of some Novel 1,3,4- thiadiazole Derivatives. Research J. Pharm. and Tech. 2011; 4(9): 1404- 1408
3.    Sherin A Hameed, Joyamma Varkey, P Jayasekhar. Schiff bases and bicyclic derivatives comprising 1,3,4-thiadiazole moiety-A review on their pharmacological activities. Asian.J.Pharm.Res. 2019; 9(4): 299-306.
4.    Karale B K, Tarkate S J, Salve S P, Zaware B H, Jadhav S S. Synthesis and Biological Screening of novel thiazolyl triazoles and thiadiazoles. Indian J chem. 2014; 53B: 339-344.
5.    Talath S, Gadad A K. Synthesis, antibacterial and antitubercular activities of some 7-[4-(5-amino-[1, 3, 4] thiadiazole-2-sulfonyl)-piperazin-1-yl] fluoroquinolonic derivatives. Eur J Med Chem. 2006; 41(8): 918-92.
6.    Mohammad Shahar Yar, Mohammad Wasim Akhter. Synthesis and Anticonvulsant activity of substituted oxadiazole and thiadiazole derivatives. Acta Poloniae Pharmaceutica-Drug Research. 2009; 66(4): 393- 397.
7.    Adnan A Kadi, Ebtehal S Al Abdullah, Ihsan A Shehata, Elsayed E Habib, Tarek M Ibrahim, Ali A et al. Synthesis, antimicrobial and anti- inflammatory activities of novel 5-(1-adamantyl)-1,3,4-thiadiazole derivatives. European journal of Medicinal Chemistry. 2010; 45(11): 5006- 5011.
8.    Lu Yu, Xiuhai Gan, Dagui Zhou, Fangcheng He, Song Zeng, Deyu Hu. Synthesis and antiviral activity of novel 1, 4-pentadien-3-one derivatives Containing a 1, 3, 4-thiadiazole moiety. Molecules. 2017; 22(4): 658-667.
9.    Subhas S Karki, Kuppusamy Panjamurthy, Sujeet Kumar, Mridula Nambiar, Suresh Babu A, Ramareddy et al. Synthesis and Biological evaluation of novel 2-aralkyl-5-substituted-6-(4’-fluorophenyl)- imidazo[2,1-b][1,3,4] thiadiazole derivatives as potent anticancer agents. European Journal of Medicinal chemistry. 2011; 46(6): 2109-2116.
10.    Mehlika Dilel Altintop, Ozgur Devrim Can, Umide Demir Ozkay, Zafer Asim Kaplancikli. Synthesis and evaluation of new 1, 3, 4-thiadiazole derivatives as nociceptive agents. Molecules. 2016; 21(8): 1004-1014.
11.    Abhishek Kumar Jain, Simant Sharma, AnkurVidya. 1, 3, 4-Thiadiazole and its derivatives as antidiabetic agents. Medicinal Chemistry. 2013; 81: 557-576.
12.    Sandeep k Chitale, B Ramesh, Chetan M Bhalgat, Jaishree V, Puttaraj C, D R Bharathi. Synthesis and antioxidant screening of some novel 1, 3, 4- thiadiazole derivatives. Research J pharm and tech. 2011; 4(9): 1404-1408.
13.    Yogesh Vaishnav, Arvind kumar Jha, Shekhar Verma, Pranita Kashyap, Chanchal Deep kaur. A review on antidiabetic activity of substituted 1, 3, 4- thiadiazole derivatives. Research J Pharm and Tech. 2017; 10(12): 4467- 4470.
14.    Hakan Tahtaci, Hatice Karacik, Abdulilah Ece, Mustafa Er, Mine Gul Seker. Design, Synthesis, SAR and Molecular modelling Studies of novel Imidazo [2, 1-b] [1, 3, 4] Thiadiazole derivatives as Highly potent Antimicrobial Agents. Mol. Inf. 2018; 37(3): 1-15.
15.    L. Pereux and A. Loupy. A tentative rationalisation of microwave effects in organic synthesis according to the reaction medium and mechanistic considerations. Tetrahedron. 2001; 57: 9199-9223.
16.    C.O.Kappe and A. Stadler, Microwaves in organic and medicinal chemistry, Wiley-VCH, Weinheim. 2005.
17.    D. Dallinger and C.O. Kappe. Automated generation of a dihydropyrimidine compound library using microwave assisted processing. Nature Protocols. 2007; 2: 1713
18.    VA Navale, SS Mokle, Archana Y Vibhute, KG Karamunge, SV Khansole, SB Junne, YB Vibhute. Microwave-Assisted Synthesis and Antibacterial Activity of Some New Flavones and 1, 5-Benzothiazepines.Asian J. Research Chem. 2009; 2(4): 472-475.
19.    Amgoth Srinivas Nayak, Neerati Venu Madhav. Rapid Synthesis and Antimicrobial activity of some new 2-amino 5-Alkyl/Aryl-1, 3, 4- thiadiazoles. Actachimica and Pharmaceutica Indica. 2014; 4(1): 63-67
20.    Alshanon Ahmed Fadhil, Firas Hassan, Ayah Abdul Hammed. Synthesis, Characterisation, Antioxidant activity and antitumour of some 2-amino-5- (3-nitrophenyl)-1, 3, 4-thiadiazole derivatives. International Journal of Pharma Sciences. 2015; 5(1): 904-910
21.    Jun Hu, Jianguang Sun, Taoyu Zhou, YanhuaXu. Microwave assisted Synthesis of 1, 3, 4-Thiadiazole Schiff base derivatives. Journal of chemical research. 2011; 35(8): 442-443
22.    Vrushali N Patil, Ameya G Yadav, A S Bobade, S V Athlekar, L S Patil, Abhay Chowdhary. Synthesis and Evaluation of new benzothiazole derivatives as potential antimicrobial agents. Research J. Pharm and Tech. 2010; 3(4): 1044-1046.
23.    Anoop Singh, A C Rana. Synthesis, Spectral characterisation and pharmacological screening of 1-methylene-4-(5-(4-(phenylamino)phenyl)- 1,3,4-Thiadiazol-2-yl)thiosemicarbazide derivatives. Reseach J. Pharm and Tech. 2011; 4(2): 279-285.
24.    Nachiket S. Dighe, Pankaj Shinde, Harshali Anap, Sanjay Bhawar, Deepak S. Musmade. QSAR Study and Synthesis of some new 2, 5-disubstituted 1, 3, 4-oxadiazole derivatives as Anti-microbial and Anti-inflammatory Agents. Asian J. Pharm. Res. 2014; 4(4): 174-179.

Recomonded Articles:

Research Journal of Pharmacy and Technology (RJPT) is an international, peer-reviewed, multidisciplinary journal.... Read more >>>

RNI: CHHENG00387/33/1/2008-TC                     
DOI: 10.5958/0974-360X 

56th percentile
Powered by  Scopus

SCImago Journal & Country Rank

Recent Articles


Not Available