Human carbonic anhydrase-II (hCA-II) is the most dominant physiologic isoform amongst the sixteen reported hCA isoforms. Because of its high availability in the different anatomical, and cellular sites of the eye like retina and lens, it plays a more prominent role in the regulation of intraocular pressure than the other twelve catalytically active hCA isoforms. This isoform is also located in the brain, kidney, gastric mucosa, osteoclasts, RBCs, skeletal muscle, testes, pancreas, lungs, etc. Earlier, hCA-II inhibitors were designed based on the sulfonamides e.g. acetazolamide, dichlorphenamide, methazolamide, ethoxzolamide, etc. and they were used systemically in antiglaucoma therapy. Many successful attempts have been made by the researchers in order to design more potent and effective inhibitors by incorporating various moieties in sulphonamides. Some novel scaffolds like chalcones, thiophenes, organotellurium compounds, dithiocarbamate, selenide, and 2-benzylpyrazine, etc. were also designed as hCA-II inhibitors and their inhibitory efficacy was proved in the nanomolar range. In order to obtain relevant information from the insights of their structure-activity relationship, the reported hCA-II inhibitors from the year 1989 to 2019 were critically analysed. It gave a complete insight into the relationship between their structure-activity and hCA-II inhibition. The broad spectrum of our investigation may help researchers to summarize all the crucial structural information required for the development of more potent hCA-II inhibitors for glaucoma.

中文翻译：

---

人类碳酸酐酶II抑制剂的结构活性关系：作为抗青光眼剂的未来发展的详细见解。

人类碳酸酐酶-II（hCA-II）是16种已报道的hCA亚型中最主要的生理亚型。由于它在眼睛的不同解剖结构和细胞位置（如视网膜和晶状体）中的高可用性，因此它在眼内压的调节中比其他十二种具有催化活性的hCA亚型起着更加突出的作用。该同工型也位于脑，肾，胃粘膜，破骨细胞，红细胞，骨骼肌，睾丸，胰腺，肺等中。早期，hCA-II抑制剂是基于磺酰胺设计的，例如乙酰唑胺，二氯苯甲酰胺，甲唑酰胺，乙氧唑酰胺，等等，它们被广泛用于抗青光眼治疗。研究人员已经进行了许多成功的尝试，以便通过在磺酰胺中掺入不同的部分来设计更有效和有效的抑制剂。还设计了一些新颖的支架，如查耳酮，噻吩，有机碲化合物，二硫代氨基甲酸酯，硒化物和2-苄基吡嗪等，作为hCA-II抑制剂，并在纳摩尔范围内证明了其抑制功效。为了从其构效关系的见解中获得相关信息，我们对1989-2019年间报道的hCA-II抑制剂进行了严格分析。它提供了对其结构活性与hCA-II抑制之间的关系的全面了解。