American Journal of Pharmacological Sciences
ISSN (Print): 2327-6711 ISSN (Online): 2327-672X Website: Editor-in-chief: Srinivas NAMMI
Open Access
Journal Browser
American Journal of Pharmacological Sciences. 2015, 3(1), 18-24
DOI: 10.12691/ajps-3-1-4
Open AccessReview Article

Recent Advances in Development of Sulfonamide Derivatives and Their Pharmacological Effects- A Review

Ajeet1, , Arun K. Mishra1 and Arvind Kumar2

1Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, IFTM University, Moradabad Uttar Pradesh, India

2Department of Pharmaceutical Chemistry, S. D. College of Pharmacy and Vocational Studies, Muzaffarnagar, Uttar Pradesh, India

Pub. Date: February 27, 2015

Cite this paper:
Ajeet, Arun K. Mishra and Arvind Kumar. Recent Advances in Development of Sulfonamide Derivatives and Their Pharmacological Effects- A Review. American Journal of Pharmacological Sciences. 2015; 3(1):18-24. doi: 10.12691/ajps-3-1-4


First drugs which were largely used for chemotherapeutically and preventive use were the sulfonamides. Sulfonamides have a wide range of pharmacological activities such as against rheumatoid arthritis, anti-hypertensive, anti-epileptic, anti-bacterial, anti-protozoal, anti-fungal, non-peptidic vasopressin receptor antagonists, anti-inflammatory, and translation initiation inhibitors. These sulfonamides have a variety of synthetic reactions to work with. This review comprises of recent advances related to synthesis and pharmacological effects of sulfonamides especially in concern to anti-epileptic and anti-microbial agents.

sulfonamide anti-epileptic anti-microbial

Creative CommonsThis work is licensed under a Creative Commons Attribution 4.0 International License. To view a copy of this license, visit


[1]  Uday K., Amandeep K., “An Overview on Some Benzimidazole and Sulfonamide Derivatives with Anti-Microbial Activity”. Research Journal of Pharmaceutical, Biological and Chemical Sciences, 2(4), 1116-1135, 2011.
[2]  Masereel B., Rolin S., Abbate F., Scozzafava A., Supuran C. T., “Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties”. J. Med. Chem., 45(2), 312-320, 2002.
[3]  Barrios I. A., et. al., “Pharmacophoric pattern of anti-epileptic sulfonamides and sulfamates-Theoretical study of the associated requirements”. Journal of Molecular Structure (Theochem), 580, 243-250, 2002.
[4]  Marc A. I., Bernard M., Stephanie R., Andrea S., Gheorghe C., Valentin C., Claudiu T. S., “Carbonic anhydrase inhibitors: aromatic and heterocyclic sulfonamides incorporating adamantyl moieties with strong anticonvulsant activity”. Bioorganic & Medicinal Chemistry, 12, 2717-2726, 2004.
[5]  Chazalette C., Masereel B., Rolin S., Thiry A., Scozzafava A., Innocenti A., Supuran C. T., “Carbonic anhydrase inhibitors. Design of anticonvulsant sulfonamides incorporating indane moieties”. Bioorg. Med. Chem. Lett., 14(23), 5781-5786, 2004.
[6]  Hai Y., Richard B. S., “New substrates and inhibitors of c-aminobutyric acid aminotransferase containing bioisosteres of the carboxylic acid group: Design, synthesis, and biological activity”. Bioorganic & Medicinal Chemistry, 14, 1331-1338, 2006.
[7]  Gregory K., “Current Understanding of Delayed Anticonvulsant Hypersensitivity Reactions”. Epilepsy Currents, 6(2), 33–37, 2006.
[8]  Nadeem S., Surendra Nath P., Suroor A. K., James P. S., Arpana R., Mahfuz A. Md. Faiz A., Mashooq A., “Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain”. Bioorganic & Medicinal Chemistry Letters, 17, 255-259, 2007.
[9]  Jean-Yves W., Anne T., Khaled El C., Jean-Michel D., Jean-Louis M., Daniela V., Andrea S., Bernard M., Claudiu T., Supuran, “Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose–thioureido tails”. Bioorganic & Medicinal Chemistry Letters, 17, 2685-2691, 2007.
[10]  Rosaria Gitto, Stefania Ferro, Stefano Agnello, Laura De Luca, Giovanbattista De Sarro, Emilio Russo, Daniela Vullo, Claudiu T. Supuran, Alba Chimirri, Synthesis and evaluation of pharmacological profile of 1-aryl-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-sulfonamides. Bioorganic & Medicinal Chemistry, 2009, 17, 3659-3664.
[11]  De Simone G., Scozzafava A., Supuran C. T., “Which carbonic anhydrases are targeted by the antiepileptic sulfonamides and sulfamates?”, Chem. Biol. Drug. Des., 74(3),317-321, 2009.
[12]  Naama H., Meir B., Bogdan W., Richard H. F., Boris Y., “Syntheses and Evaluation of Anticonvulsant Profile and Teratogenicity of Novel Amide Derivatives of Branched Aliphatic Carboxylic Acids with 4-Aminobenzensulfonamide”. J. Med. Chem., 53, 4177-4186, 2010.
[13]  Siddiqui N., Arshad M. F., Khan S. A., Ahsan. W., “Sulfonamide derivatives of thiazolidin-4-ones with anticonvulsant activity against two seizure models: synthesis and pharmacological evaluation”. J. Enzyme. Inhib. Med. Chem., 25(4), 485-491, 2010.
[14]  Manuel K., Kurt L., Markus S., Ivan-Toma V., Joerg K., Yves P. A., David A., Carcache, Henri M., Silvi O., David O., Stephan U., “Quinazolinedione sulfonamides: A novel class of competitive AMPA receptor antagonists with oral activity”. Bioorganic & Medicinal Chemistry Letters, 21, 3358-3361, 2011.
[15]  Jahan B. G., Nastaran M., “Docking, CoMFA and CoMSIA studies of a series of sulfonamides derivatives as carbonic anhydrase I inhibitors”. Journal of enzyme inhibition and Medicinal chemistry, 28(2), 320-327, 2013.
[16]  Ajeet, Praveen K., Laxmi T.. “Virtual Screening Tool Based Designing and Evaluation of Novel Sulfonamide Derivatives as Anticonvulsant Agent – A Pharmacophoric Approach”. International Journal of Pharmaceutical and Phytopharmacological Research, 2(3), 202-208, 2012.
[17]  Ajeet, Praveen K., Laxmi T.,QSAR model development for studying sulfonamide derivatives as carbonic anhydrase inhibitors- a MLR approach”. International Journal of Pharmaceutical Research and Technology, 5(1), 74-81, 2013.
[18]  Christophe S., Elise S. G., Ki D. P., Pierre M., Robert S., Erica D., James P. S., Harold K., “Synthesis and Anticonvulsant Activities of (R)-N-(40-Substituted)benzyl 2-Acetamido-3-methoxypropionamides”. J. Med. Chem., 53, 1288-1305, 2010.
[19]  Naama H., Meir B., Boris Y., Alfonso M., Mayank A., Arthur H. R., Robert M., Andrea S., Claudiu T. S., “Anticonvulsant 4-Aminobenzenesulfonamide Derivatives with Branched-Alkylamide Moieties: X-ray Crystallography and Inhibition Studies of Human Carbonic Anhydrase Isoforms I, II, VII, and XIV”. J. Med. Chem., 54, 3977-3981, 2011.
[20]  Claudia B., Milagros A., Andrea M., Dale E. E., “Interactions of Monoamine Oxidases with the Antiepileptic Drug Zonisamide: Specificity of Inhibition and Structure of the Human Monoamine Oxidase B Complex”. J. Med. Chem., 54, 909-912, 2011.
[21]  Narasaiah T., Subba D. R., Venkata Ramana K., Adam S., Naga Raju C., “Synthesis of New Sulfonamide Derivatives of Tryptamine and Their Antimicrobial Activity”. Der Pharma Chemica, 4(4), 1582-1590, 2011.
[22]  Nassir N. A., Yatimah A., Zanariah A., Raied M. S., Ekhlass M. T., Aidil A. H., “Synthesis and Antibacterial Evaluation of Some Novel Imidazole and Benzimidazole Sulfonamides”. Molecules, 18, 11978-11995, 2013.
[23]  Aneta K., Iwona F., Justyna Ł., Danuta B., “Biological activity and synthesis of sulfonamide derivatives: a brief review”, CHEMIK, 68(7), 620-628, 2014.
[24]  Ajeet, Arvind K., “Designing, Proposed Synthesis and Docking Analysis of Novel Sulfonamide Derivatives as Antimicrobial Agents”. American Journal of Pharmacological Sciences, 2(2), 37-41, 2014.
[25]  Ajeet, Laxmi T., Arvind K., “Synthesis, Spectral Characterization, Docking Studies and QSAR Screening of 4-amino-benzenesulfonamides/N-acetyl 4-amino-benzenesulfonamide Derivatives as Antimicrobial Agents”. Journal of Pharmacy and Nutrition Sciences, 4, 135-153, 2014.
[26]  Sapna R., Ajeet, Arvind K., “Designing of Sulfanilamide/Sulfacetamide Derivatives as Human Topoisomerase II Inhibitor: A Docking Approach”. American Journal of Pharmacological Sciences, 2(2), 42-46, 2014.
[27]  Ajeet, Mansi V., Sangeeta R., Arvind K., “In-silico designing and screening of quinazolinedione sulfonamide derivatives as antibacterial agents: a docking approach”. CIBTech Journal of Pharmaceutical Sciences, 3(4), 20-31, 2014.