Design, Synthesis and Evaluation of Thiourea Derivatives as Antimicrobial and Antiviral Agents-Reference-Cited by-同舟云学术

Design, Synthesis and Evaluation of Thiourea Derivatives as Antimicrobial and Antiviral Agents

Published:2019-05-24 Issue:6 Volume:16 Page:618-624
ISSN:1570-1808
Container-title:Letters in Drug Design & Discovery
language:en
Short-container-title:LDDD

Author:

Ravichandran Veerasamy¹,Shalini Sivadasan²,Kumar Krishnan Suresh³,Rajak Harish⁴,Agrawal Ram Kishore⁵

Affiliation:

1. Department of Pharmacy, AIMST University, Semeling 08100, Kedah, Malaysia

2. KMCH College of Pharmacy, Kovai Estate, Kalapatti Road, Coimbatore, India

3. Medicinal Chemistry Research Laboratory, KMCH College of Pharmacy, Coimbatore, India

4. Medicinal Chemistry Research Laboratory, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University, Bilaspur 495 009, India

5. Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar 470003 (M.P.), India

Abstract

Background: The development of drug-resistant by bacteria appears rapidly and thus making the effectiveness of antibiotics severely limited. Methods: A series of thiourea derivatives was synthesized, characterized and evaluated for their in vitro antibacterial, antifungal and antiviral activities. Results: Structures of the newly synthesized compounds were confirmed by elemental and spectral analysis. The biological results showed that some of the target compounds displayed comparable antimicrobial and antiviral activities with reference drugs. Structure-activity relationship studies revealed that the ortho- chloro or fluoro substituted phenyl at Ar1 and substituted pyridinyl at Ar2 positions of the thiourea nucleus are essential for their in vitro antimicrobial and anti-HIV activity. In particular, compounds 8 and 10 showed better activity against the tested bacteria, fungi and viral strains than other synthesized PET derivatives reported in the present study. Conclusion: These results provide an encouraging lead that could be used for the development of new potent antiviral and antimicrobial agents

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery,Pharmaceutical Science,Molecular Medicine

Reference18 articles.

1. Ahgren C, Backro K, Bell FW, Cantrell AS, Clemens M, Colacino JM, Deeter JB, Engelhardt JA, Hogberg M, Jaskunas SR, Johansson NG, Jordan CL, Kasher JS, Kinnick MD, Lind P, Lopez C, Morin JM. Jr.; Muesing, M.A.; Noreen, R.; Oberg, B.; Paget, C.J.; Palkowitz, J.A.; Parrish, C.A.; Pranc, P.; Rippy, M.K.; Rydergard, C.; Sahlberg, C.; Swanson, S.; Ternansky, R.J.; Unge, T.; Vasileff, R.T.; Vrang, L.; West, S.J.; Zhang, H.; Zhou, X.X. The PETT series, a new class of potent nonnucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase.

2. Bell, F.W.; Cantrell, A.S.; Högberg, M.; Jaskunas, S.R.; Johansson, N.G.; Jordan, C.L.; Kinnick, M.D.; Lind, P.; Morin, J.M.; Noréen, R. Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs. J. Med. Chem., 1995, 38, 4929-4936.

3. Cantrell AS, Engelhardt P, Hogberg M, Jaskunas SR, Johansson NG, Jordan CL, Kangasmetsa J, Kinnick MD, Lind P, Morin JM, Muesing MA, Noreen R, Oberg B, Pranc P, Sahlberg C, Ternansky RJ, Vasilef RT, Virang L, West SJ, Zhang H. Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure activity relationship studies of PETT analogs.

4. Zhang H, Vrang L, Backbro K, Lind P, Sahlberg C, Unge T, Oberg B. Inhibition of wild type and mutant reverse transcriptase by the phenyl ethyl thiazolyl thiourea derivatives trovirdine and MSC-127.

5. Uckun, F.M.; Mao, C.; Pendergrass, S.; Maher, D.; Zhu, D.; Tuel-Ahlgren, L.; Venkatachalam, T.K.N. -[2-(1-cyclohexenyl)ethyl]-N′-[2-(5-bromo pyridyl)]-thiourea and N′-[2-(1-cyclohexenyl) ethyl]-N′-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1. Bioorg. Med. Chem. Lett., 1999, 9(18), 2721-2726.

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