Application of Heterocycles as an Alternative for the Discovery of New Anti-ulcer Compounds: A Mini-Review

Author:

de Lócio Lucas Linhares1ORCID,do Nascimento Agnis Pâmela Simões1ORCID,Santos Mirelly Barbosa1ORCID,Gomes Joilly Nilce Santana1ORCID,de Medeiros e Silva Yvnni Maria Sales1ORCID,Albino Sonaly Lima1ORCID,dos Santos Vanda Lúcia1ORCID,de Moura Ricardo Olímpio1ORCID

Affiliation:

1. Department of Pharmacy, State University of Paraíba, R. Baraúnas, 351, Cidade Universitária, Campina Grande, Paraíba, 58429-500, Brazil

Abstract

ABSTRACT: A peptic ulcer is a lesion located in the esophagus, stomach, and upper intestine, caused by an imbalance between acid secretion and the release of protective mucus. This pathology is prevalent in approximately 14% of the world population and is commonly treated with proton pump inhibitors and type 2 histaminergic receptor antagonists, however, these drugs present concerning side effects that may lead to gastric cancer. In this sense, this research aimed to present the main heterocyclics studied in recent years. The screening method for the choice of articles was based on the selection of publications between 2000 and 2021 present in the Science Direct, Web of Science, Capes, and Scielo databases, by using the descriptors ''new derivatives'', “heterocyclics” “antiulcerogenic”, “gastroprotective” and “antisecretor”. This research showed that the most used rings in the development of anti-ulcer drugs were benzimidazole, quinazoline, thiazole, and thiadiazole. The results also portray several types of modern in silico, in vitro and in vivo assays, as well as the investigation of different mechanisms of action, with emphasis on proton pump inhibition, type 2 histaminergic receptor blockers, potassium competitive acid blockers, type E prostaglandin agonism, anti-secretory activity and anti-oxidant action. Additionally, the review evidenced the presence of the nitrogen atom in the heterocyclic ring as a determinant of the potential of the compound. This research suggests new alternatives for the treatment of gastric lesions, which may be more potent and cause fewer side effects than the currently used, and tend to evolve into more advanced studies in the coming years.

Funder

Programa de Incentivo à Pós-Graduação e Pesquisa

Fundação de Apoio à Pesquisa do Estado da Paraíba

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery,Pharmacology

Reference66 articles.

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2. Bernardo G.O.; Souza S.R.; Bernardo C.O.; Faraco A.J.; Perfil epidemiológico dos pacientes diagnosticados com úlcera gástrica e/ou duodenal em dois serviços de referência do extremo sul catarinense no período de um ano. Arquivos Catarinenses de Medicina 2017,46(3),59-69

3. Torres OJM; Santos OJD; Moura RSD; (2018). Atividade de orbignya phalerata e euterpe edules na prevenção e tratamento da úlcera péptica em ratos. Abcd Arq Bras Cir Dig 2008,31(3)

4. Somensi L.B.; Costa P.; Boeing T.; Gastroprotective properties of Lupeol-derived ester: Pre-clinical evidences of Lupeol-stearate as a potent antiulcer agent. Chem Biol Interact 2020,321

5. Silva T.O.L.D.A.; Gomes K.C.F.; Sales Filho R.; Costa H.F.; Análise histológica da mucosa gástrica saudável e doente com gastrite crônica ou doença ulcerosa péptica. Revista de Ciências da Saúde Nova Esperança 2018,16(3),43-50

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